| Year |
Citation |
Score |
| 2024 |
Ghosh A, Ribeiro-Rodrigues L, Ruffolo G, Alfano V, Domingos C, Rei N, Tosh DK, Rombo DM, Morais TP, Valente CA, Xapelli S, Bordadágua B, Rainha-Campos A, Bentes C, Aronica E, ... ... Jacobson KA, et al. Selective modulation of epileptic tissue by an adenosine A receptor-activating drug. British Journal of Pharmacology. PMID 39300608 DOI: 10.1111/bph.17319 |
0.436 |
|
| 2024 |
Oliva P, Pramanik A, Jung YH, Lewicki SA, Mwendwa JM, Park JH, Jacobson KA. Functionalized Congeners of 2-Chromene P2Y Receptor Antagonists. Cells. 13. PMID 39195256 DOI: 10.3390/cells13161366 |
0.483 |
|
| 2024 |
Tosh DK, Pavan M, Cronin C, Pottie E, Wan TC, Chen E, Lewicki SA, Campbell RG, Gao ZG, Auchampach JA, Stove CP, Liang BT, Jacobson KA. 2-Substituted (N)-Methanocarba A Adenosine Receptor Agonists: In Silico, In Vitro, and In Vivo Characterization. Acs Pharmacology & Translational Science. 7: 2154-2173. PMID 39022354 DOI: 10.1021/acsptsci.4c00223 |
0.837 |
|
| 2024 |
Pradhan B, Pavan M, Fisher CL, Salmaso V, Wan TC, Keyes RF, Rollison N, Suresh RR, Kumar TS, Gao ZG, Smith BC, Auchampach JA, Jacobson KA. Lipid Trolling to Optimize A Adenosine Receptor-Positive Allosteric Modulators (PAMs). Journal of Medicinal Chemistry. PMID 38959401 DOI: 10.1021/acs.jmedchem.4c00944 |
0.692 |
|
| 2024 |
Kim G, Jarhad DB, Lee G, Kim G, Hou X, Yu J, Lee CS, Warnick E, Gao ZG, Ahn SY, Kwak D, Park K, Lee SD, Park TU, Jung SY, ... ... Jacobson KA, et al. Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A Adenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors. Journal of Medicinal Chemistry. PMID 38845345 DOI: 10.1021/acs.jmedchem.4c01003 |
0.808 |
|
| 2024 |
Gao ZG, Haddad M, Jacobson KA. A adenosine receptor signaling and regulation. Purinergic Signalling. PMID 38833181 DOI: 10.1007/s11302-024-10025-y |
0.348 |
|
| 2024 |
Sapio MR, Staedtler ES, King DM, Maric D, Jahanipour J, Ghetti A, Jacobson KA, Mannes AJ, Iadarola MJ. Analgesic candidate adenosine A3 receptors are expressed by perineuronal peripheral macrophages in human dorsal root ganglion and spinal cord microglia. Pain. PMID 38691673 DOI: 10.1097/j.pain.0000000000003242 |
0.379 |
|
| 2024 |
Puhl AC, Lewicki SA, Gao ZG, Pramanik A, Makarov V, Ekins S, Jacobson KA. Machine learning-aided search for ligands of P2Y and other P2Y receptors. Purinergic Signalling. PMID 38526670 DOI: 10.1007/s11302-024-10003-4 |
0.303 |
|
| 2024 |
Kim G, Hou X, Byun WS, Kim G, Jarhad DB, Lee G, Hyun YE, Yu J, Lee CS, Qu S, Warnick E, Gao ZG, Kim JY, Ji S, Shin H, ... ... Jacobson KA, et al. Correction to "Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A/A Adenosine Receptor Antagonists and Their Cancer Immunotherapeutic Activity". Journal of Medicinal Chemistry. PMID 38259147 DOI: 10.1021/acs.jmedchem.3c02442 |
0.797 |
|
| 2024 |
Nikodijević O, Jacobson KA, Daly JW. Effects of Combinations of Methylxanthines and Adenosine Analogs on Locomotor Activity in Control and Chronic Caffeine-Treated Mice. Drug Development Research. 30: 104-110. PMID 38250653 DOI: 10.1002/ddr.430300209 |
0.413 |
|
| 2024 |
Jacobson KA. Probing Adenosine and P2 Receptors: Design of Novel Purines and Nonpurines as Selective Ligands. Drug Development Research. 52: 178-186. PMID 38239932 DOI: 10.1002/ddr.1113 |
0.582 |
|
| 2024 |
Bolego C, Centemeri C, Abbracchio MP, Ceruti S, Cattabeni F, Jacobson KA, Puglisi L, Rovati GE, Burnstock G, Nicosia S. Two Distinct P2Y Receptors Are Involved in Purine- and Pyrimidine-Evoked Ca Elevation in Mammalian Brain Astrocytic Cultures. Drug Development Research. 52: 122-132. PMID 38239931 DOI: 10.1002/ddr.1106 |
0.44 |
|
| 2024 |
Dudley MW, Peet NP, Demeter DA, Weintraub HJR, Ijzerman AP, Nordvall G, van Galen PJM, Jacobson KA. Adenosine A Receptor and Ligand Molecular Modeling. Drug Development Research. 28: 237-243. PMID 38239889 DOI: 10.1002/ddr.430280309 |
0.625 |
|
| 2024 |
Jacobson KA, IJzerman AP, Linden J. 1,3-Dialkylxanthine Derivatives Having High Potency as Antagonists at Human A Adenosine Receptors. Drug Development Research. 47: 45-53. PMID 38239816 DOI: 10.1002/(sici)1098-2299(199905)47:1<45::aid-ddr6>3.0.co;2-u |
0.684 |
|
| 2024 |
Abbracchio MP, Ceruti S, Brambilla R, Barbieri D, Camurri A, Franceschi C, Giammarioli AM, Jacobson KA, Cattabeni F, Malorni W. Adenosine A Receptors and Viability of Astrocytes. Drug Development Research. 45: 379-386. PMID 38239500 DOI: 10.1002/(sici)1098-2299(199811/12)45:3/4<379::aid-ddr38>3.0.co;2-y |
0.393 |
|
| 2024 |
Jacobson KA, Suzuki F. Recent Developments in Selective Agonists and Antagonists Acting at Purine and Pyrimidine Receptors. Drug Development Research. 39: 289-300. PMID 38239267 DOI: 10.1002/(sici)1098-2299(199611/12)39:3/4<289::aid-ddr8>3.0.co;2-n |
0.504 |
|
| 2024 |
Boyer JL, Schachter JB, Sromek SM, Palmer RK, Jacobson KA, Nicholas RA, Harden TK. Avian and Human Homologues of the P2Y Receptor: Pharmacological, Signaling, and Molecular Properties. Drug Development Research. 39: 253-261. PMID 38235168 DOI: 10.1002/(sici)1098-2299(199611/12)39:3/4<253::aid-ddr4>3.0.co;2-q |
0.684 |
|
| 2024 |
Lee JE, Wilcox K, Jacobson KA, Dichter M, Liang BT. Adenosine Receptor Subtypes and Cardioprotection. Drug Development Research. 45: 394-401. PMID 38234711 DOI: 10.1002/(sici)1098-2299(199811/12)45:3/4<394::aid-ddr40>3.0.co;2-j |
0.663 |
|
| 2024 |
Ji XD, von Lubitz D, Olah ME, Stiles GL, Jacobson KA. Species Differences in Ligand Affinity at Central A-Adenosine Receptors. Drug Development Research. 33: 51-59. PMID 38229954 DOI: 10.1002/ddr.430330109 |
0.74 |
|
| 2024 |
Fisher CL, Pavan M, Salmaso V, Keyes RF, Wan TC, Pradhan B, Gao ZG, Smith BC, Jacobson KA, Auchampach JA. Extrahelical binding site for a 1-imidazo[4,5-c]quinolin-4-amine A adenosine receptor positive allosteric modulator on helix 8 and distal portions of transmembrane domains 1 and 7. Molecular Pharmacology. PMID 38182432 DOI: 10.1124/molpharm.123.000784 |
0.694 |
|
| 2023 |
Krols S, Matteucci F, Van Hecke K, Caljon G, Jacobson KA, Van Calenbergh S. Dual /C7-Substituted 7-Deazapurine and Tricyclic Ribonucleosides with Affinity for G Protein-Coupled Receptors. Acs Medicinal Chemistry Letters. 15: 81-86. PMID 38229744 DOI: 10.1021/acsmedchemlett.3c00427 |
0.44 |
|
| 2023 |
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA, Abbracchio MP, Abraham G, Agoulnik A, Alexander W, ... ... Jacobson KA, et al. The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. British Journal of Pharmacology. S23-S144. PMID 38123151 DOI: 10.1111/bph.16177 |
0.686 |
|
| 2023 |
Oliva P, Suresh RR, Pasquini S, Salmaso V, Will EJ, Tosh DK, Gao ZG, Liu N, Gavrilova O, Vincenzi F, Varani K, Jacobson KA. 2-Amino-5-arylethynyl-thiophen-3-yl-(phenyl)methanones as A Adenosine Receptor Positive Allosteric Modulators. Acs Medicinal Chemistry Letters. 14: 1640-1646. PMID 38116442 DOI: 10.1021/acsmedchemlett.3c00315 |
0.436 |
|
| 2023 |
Zhang HJ, Ociepa M, Nassir M, Zheng B, Lewicki SA, Salmaso V, Baburi H, Nagel J, Mirza S, Bueschbell B, Al-Hroub H, Perzanowska O, Lin Z, Schmidt MA, Eastgate MD, ... Jacobson KA, et al. Stereocontrolled access to thioisosteres of nucleoside di- and triphosphates. Nature Chemistry. PMID 37857844 DOI: 10.1038/s41557-023-01347-2 |
0.643 |
|
| 2023 |
Jacobson KA, Pradhan B, Wen Z, Pramanik A. Corrigendum to "New paradigms in purinergic receptor ligand discovery" [Neuropharmacology 230 (2023) 109503]. Neuropharmacology. 241: 109731. PMID 37806912 DOI: 10.1016/j.neuropharm.2023.109731 |
0.4 |
|
| 2023 |
Jacobson KA, Suresh RR, Oliva P. A adenosine receptor agonists, antagonists, inverse agonists and partial agonists. International Review of Neurobiology. 170: 1-27. PMID 37741687 DOI: 10.1016/bs.irn.2023.08.001 |
0.367 |
|
| 2023 |
Tosh DK, Fisher CL, Salmaso V, Wan TC, Campbell RG, Chen E, Gao ZG, Auchampach JA, Jacobson KA. First Potent Macrocyclic A Adenosine Receptor Agonists Reveal G-Protein and β-Arrestin2 Signaling Preferences. Acs Pharmacology & Translational Science. 6: 1288-1305. PMID 37705595 DOI: 10.1021/acsptsci.3c00126 |
0.762 |
|
| 2023 |
Pottie E, Suresh RR, Jacobson KA, Stove CP. Assay-Dependent Inverse Agonism at the A Adenosine Receptor: When Neutral Is Not Neutral. Acs Pharmacology & Translational Science. 6: 1266-1274. PMID 37705594 DOI: 10.1021/acsptsci.3c00071 |
0.372 |
|
| 2023 |
Jacobson KA, Salvemini D. Editorial: Small molecules and biologics for future purinergic therapeutics. Purinergic Signalling. 19: 465-466. PMID 37676356 DOI: 10.1007/s11302-023-09964-9 |
0.571 |
|
| 2023 |
Sánchez-Fernández N, Gómez-Acero L, Sarasola LI, Argerich J, Chevigné A, Jacobson KA, Ciruela F, Fernández-Dueñas V, Aso E. Cannabidiol negatively modulates adenosine A receptor functioning in living cells. Acta Neuropsychiatrica. 1-14. PMID 37605951 DOI: 10.1017/neu.2023.30 |
0.634 |
|
| 2023 |
Kim G, Hou X, Byun WS, Kim G, Jarhad DB, Lee G, Hyun YE, Yu J, Lee CS, Qu S, Warnick E, Gao ZG, Kim JY, Ji S, Shin H, ... ... Jacobson KA, et al. Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A/A Adenosine Receptor Antagonists and Their Cancer Immunotherapeutic Activity. Journal of Medicinal Chemistry. PMID 37603705 DOI: 10.1021/acs.jmedchem.3c00806 |
0.794 |
|
| 2023 |
Tosh DK, Calkins MM, Ivancich MS, Bock HA, Campbell RG, Lewicki SA, Chen E, Gao ZG, McCorvy JD, Jacobson KA. Structure activity relationships of 5-HT and 5-HT serotonin receptor antagonists: N, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives. European Journal of Medicinal Chemistry. 259: 115691. PMID 37562117 DOI: 10.1016/j.ejmech.2023.115691 |
0.357 |
|
| 2023 |
Gao ZG, Levitan IM, Inoue A, Wei Q, Jacobson KA. A adenosine receptor activation and modulation by protein kinase C. Iscience. 26: 107178. PMID 37404375 DOI: 10.1016/j.isci.2023.107178 |
0.301 |
|
| 2023 |
Wen Z, Pramanik A, Lewicki SA, Jung YH, Gao ZG, Randle JCR, Cronin C, Chen Z, Giancotti LA, Whitehead GS, Liang BT, Breton S, Salvemini D, Cook DN, Jacobson KA. Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2Y Receptor Antagonists. Journal of Medicinal Chemistry. PMID 37382926 DOI: 10.1021/acs.jmedchem.3c00664 |
0.745 |
|
| 2023 |
Ciruela F, Jacobson KA. Editorial: Purinergic pharmacology, Volume II. Frontiers in Pharmacology. 14: 1200187. PMID 37261289 DOI: 10.3389/fphar.2023.1200187 |
0.397 |
|
| 2023 |
Jacobson KA, Pradhan B, Wen Z, Pramanik A. New paradigms in purinergic receptor ligand discovery. Neuropharmacology. 230: 109503. PMID 36921890 DOI: 10.1016/j.neuropharm.2023.109503 |
0.401 |
|
| 2023 |
Cherchi F, Venturini M, Magni G, Scortichini M, Jacobson KA, Pugliese AM, Coppi E. Covalently Binding Adenosine A Receptor Agonist ICBM Irreversibly Reduces Voltage-Gated Ca Currents in Dorsal Root Ganglion Neurons. Purinergic Signalling. PMID 36918461 DOI: 10.1007/s11302-023-09929-y |
0.397 |
|
| 2023 |
Thakur N, Ray AP, Sharp L, Jin B, Duong A, Pour NG, Obeng S, Wijesekara AV, Gao ZG, McCurdy CR, Jacobson KA, Lyman E, Eddy MT. Anionic phospholipids control mechanisms of GPCR-G protein recognition. Nature Communications. 14: 794. PMID 36781870 DOI: 10.1038/s41467-023-36425-z |
0.358 |
|
| 2023 |
Thakur N, Ray AP, Sharp L, Jin B, Duong A, Pour NG, Obeng S, Wijesekara AV, Gao ZG, McCurdy CR, Jacobson KA, Lyman E, Eddy MT. Anionic Phospholipids Control Mechanisms of GPCR-G Protein Recognition. Biorxiv : the Preprint Server For Biology. PMID 36711594 DOI: 10.1101/2023.01.11.523010 |
0.368 |
|
| 2022 |
Gao ZG, Auchampach JA, Jacobson KA. Species dependence of A adenosine receptor pharmacology and function. Purinergic Signalling. 1-28. PMID 36538251 DOI: 10.1007/s11302-022-09910-1 |
0.707 |
|
| 2022 |
Fallot LB, Suresh RR, Fisher CL, Salmaso V, O'Connor RD, Kaufman N, Gao ZG, Auchampach JA, Jacobson KA. Structure-Activity Studies of 1-Imidazo[4,5-]quinolin-4-amine Derivatives as A Adenosine Receptor Positive Allosteric Modulators. Journal of Medicinal Chemistry. 65: 15238-15262. PMID 36367749 DOI: 10.1021/acs.jmedchem.2c01170 |
0.728 |
|
| 2022 |
Sgambellone S, Marri S, Catarinicchia S, Pini A, Tosh DK, Jacobson KA, Masini E, Salvemini D, Lucarini L. Adenosine A Receptor (AAR) Agonist for the Treatment of Bleomycin-Induced Lung Fibrosis in Mice. International Journal of Molecular Sciences. 23. PMID 36362112 DOI: 10.3390/ijms232113300 |
0.485 |
|
| 2022 |
Whitehead GS, Karcz TP, Tosh DK, Jung YH, Wen Z, Campbell RG, Gopinatth V, Gao ZG, Jacobson KA, Cook DN. Effects of Purinergic Receptor Deletion or Pharmacologic Modulation on Pulmonary Inflammation in Mice. Acs Pharmacology & Translational Science. 5: 973-984. PMID 36268115 DOI: 10.1021/acsptsci.2c00128 |
0.325 |
|
| 2022 |
Toti KS, Verma R, McGonnigle MJ, Gamiotea Turro D, Wen Z, Lewicki SA, Liang BT, Jacobson KA. Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2-naphtho[1,2-][1,4]diazepine-2,4(3)-diones as P2X4 Receptor Antagonists. Journal of Medicinal Chemistry. PMID 36150180 DOI: 10.1021/acs.jmedchem.2c01197 |
0.635 |
|
| 2022 |
Jung YH, Shah Q, Lewicki SA, Pramanik A, Gopinatth V, Pelletier J, Sévigny J, Iqbal J, Jacobson KA. Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 75: 128981. PMID 36089113 DOI: 10.1016/j.bmcl.2022.128981 |
0.448 |
|
| 2022 |
Fisher CL, Fallot LB, Wan TC, Keyes RF, Suresh RR, Rothwell AC, Gao ZG, McCorvy JD, Smith BC, Jacobson KA, Auchampach JA. Characterization of Dual-Acting A Adenosine Receptor Positive Allosteric Modulators That Preferentially Enhance Adenosine-Induced Gα and Gα Isoprotein Activation. Acs Pharmacology & Translational Science. 5: 625-641. PMID 35983277 DOI: 10.1021/acsptsci.2c00076 |
0.735 |
|
| 2022 |
Shiriaeva A, Park D, Kim G, Lee Y, Hou X, Jarhad DB, Kim G, Yu J, Hyun YE, Kim W, Gao ZG, Jacobson KA, Han GW, Stevens RC, Jeong LS, et al. GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A Adenosine Receptor. Journal of Medicinal Chemistry. PMID 35977382 DOI: 10.1021/acs.jmedchem.2c00462 |
0.849 |
|
| 2022 |
Puhl AC, Gao ZG, Jacobson KA, Ekins S. Machine Learning for Discovery of New ADORA Modulators. Frontiers in Pharmacology. 13: 920643. PMID 35814244 DOI: 10.3389/fphar.2022.920643 |
0.412 |
|
| 2022 |
Jacobson KA, Kim HS, Ravi G, Kim SK, Lee K, Chen A, Chen W, Kim SG, Barak D, Liang BT, Gao ZG. Engineering of A Adenosine and P2Y Nucleotide Receptors and Their Ligands. Drug Development Research. 58: 330-339. PMID 35799977 DOI: 10.1002/ddr.10168 |
0.882 |
|
| 2022 |
Kim YC, Karton Y, Ji XD, Melman N, Linden J, Jacobson KA. Acyl-Hydrazide Derivatives of a Xanthine Carboxylic Congener (XCC) as Selective Antagonists at Human A Adenosine Receptors. Drug Development Research. 47: 178-188. PMID 35790094 DOI: 10.1002/(sici)1098-2299(199908)47:4<178::aid-ddr4>3.0.co;2-l |
0.672 |
|
| 2022 |
Toti KS, Campbell RG, Lee H, Salmaso V, Suresh RR, Gao ZG, Jacobson KA. Fluorescent A and A adenosine receptor antagonists as flow cytometry probes. Purinergic Signalling. PMID 35687212 DOI: 10.1007/s11302-022-09873-3 |
0.391 |
|
| 2022 |
Ciruela F, Jacobson KA. Optical Control of Adenosine A Receptor Signaling: Towards a Multimodal Phototherapy in Psoriasis? Frontiers in Immunology. 13: 904762. PMID 35572558 DOI: 10.3389/fimmu.2022.904762 |
0.552 |
|
| 2022 |
Merighi S, Borea PA, Varani K, Vincenzi F, Travagli A, Nigro M, Pasquini S, Suresh RR, Kim SW, Volkow ND, Jacobson KA, Gessi S. Pathophysiological Role and Medicinal Chemistry of A Adenosine Receptor Antagonists in Alzheimer's Disease. Molecules (Basel, Switzerland). 27. PMID 35566035 DOI: 10.3390/molecules27092680 |
0.369 |
|
| 2022 |
Suresh RR, Gao ZG, Salmaso V, Chen E, Campbell RG, Poe RB, Liston TE, Jacobson KA. Selective A Adenosine Receptor Antagonist Radioligand for Human and Rodent Species. Acs Medicinal Chemistry Letters. 13: 623-631. PMID 35450351 DOI: 10.1021/acsmedchemlett.1c00685 |
0.505 |
|
| 2022 |
Lemmerhirt JP, Isaak A, Liu R, Kock M, Daniliuc CG, Jacobson KA, Heitman LH, Junker A. Development of Bicyclo[3.1.0]hexane-Based A Receptor Ligands: Closing the Gaps in the Structure-Affinity Relationships. Molecules (Basel, Switzerland). 27. PMID 35408685 DOI: 10.3390/molecules27072283 |
0.863 |
|
| 2022 |
Vlachodimou A, de Vries H, Pasoli M, Goudswaard M, Kim SA, Kim YC, Scortichini M, Marshall M, Linden J, Heitman LH, Jacobson KA, IJzerman AP. Kinetic profiling and functional characterization of 8-phenylxanthine derivatives as A adenosine receptor antagonists. Biochemical Pharmacology. 200: 115027. PMID 35395239 DOI: 10.1016/j.bcp.2022.115027 |
0.577 |
|
| 2022 |
Schiller IC, Jacobson KA, Wen Z, Malisetty A, Schmalzing G, Markwardt F. Dihydropyridines Potentiate ATP-Induced Currents Mediated by the Full-Length Human P2X5 Receptor. Molecules (Basel, Switzerland). 27. PMID 35335209 DOI: 10.3390/molecules27061846 |
0.399 |
|
| 2022 |
IJzerman AP, Jacobson KA, Müller CE, Cronstein BN, Cunha RA. International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update. Pharmacological Reviews. 74: 340-372. PMID 35302044 DOI: 10.1124/pharmrev.121.000445 |
0.719 |
|
| 2022 |
Abel B, Murakami M, Tosh DK, Yu J, Lusvarghi S, Campbell RG, Gao ZG, Jacobson KA, Ambudkar SV. Interaction of A adenosine receptor ligands with the human multidrug transporter ABCG2. European Journal of Medicinal Chemistry. 231: 114103. PMID 35152062 DOI: 10.1016/j.ejmech.2022.114103 |
0.759 |
|
| 2022 |
Wen Z, Salmaso V, Jung YH, Phung NB, Gopinatth V, Shah Q, Patterson AT, Randle JCR, Chen Z, Salvemini D, Lieberman DI, Whitehead GS, Karcz TP, Cook DN, Jacobson KA. Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2YR Antagonist. Journal of Medicinal Chemistry. PMID 35113556 DOI: 10.1021/acs.jmedchem.1c01964 |
0.607 |
|
| 2022 |
Singh AK, Mahalingam R, Squillace S, Jacobson KA, Tosh DK, Dharmaraj S, Farr SA, Kavelaars A, Salvemini D, Heijnen CJ. Targeting the A adenosine receptor to prevent and reverse chemotherapy-induced neurotoxicities in mice. Acta Neuropathologica Communications. 10: 11. PMID 35093182 DOI: 10.1186/s40478-022-01315-w |
0.516 |
|
| 2022 |
Scortichini M, Idris RM, Moschütz S, Keim A, Salmaso V, Dobelmann C, Oliva P, Losenkova K, Irjala H, Vaittinen S, Sandholm J, Yegutkin GG, Sträter N, Junker A, Müller CE, ... Jacobson KA, et al. Structure-Activity Relationship of 3-Methylcytidine-5'-α,β-methylenediphosphates as CD73 Inhibitors. Journal of Medicinal Chemistry. PMID 35080883 DOI: 10.1021/acs.jmedchem.1c01852 |
0.794 |
|
| 2021 |
Suresh RR, Poe RB, Lin B, Lv K, Campbell RG, Gao ZG, Liston TE, Toti KS, Jacobson KA. Convergent synthesis of 2-thioether-substituted ()-methanocarba-adenosines as purine receptor agonists. Rsc Advances. 11: 27369-27380. PMID 35480676 DOI: 10.1039/d1ra05096f |
0.435 |
|
| 2021 |
Tosh DK, Salmaso V, Campbell RG, Rao H, Bitant A, Pottie E, Stove CP, Liu N, Gavrilova O, Gao ZG, Auchampach JA, Jacobson KA. A adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity. European Journal of Medicinal Chemistry. 113983. PMID 34844790 DOI: 10.1016/j.ejmech.2021.113983 |
0.733 |
|
| 2021 |
Jacobson KA, Salmaso V, Suresh RR, Tosh DK. Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets. Rsc Medicinal Chemistry. 12: 1808-1825. PMID 34825182 DOI: 10.1039/d1md00167a |
0.442 |
|
| 2021 |
Salmaso V, Jain S, Jacobson KA. Purinergic GPCR transmembrane residues involved in ligand recognition and dimerization. Methods in Cell Biology. 166: 133-159. PMID 34752329 DOI: 10.1016/bs.mcb.2021.06.001 |
0.436 |
|
| 2021 |
Matricon P, Vo DD, Gao ZG, Kihlberg J, Jacobson KA, Carlsson J. Fragment-based design of selective GPCR ligands guided by free energy simulations. Chemical Communications (Cambridge, England). PMID 34734588 DOI: 10.1039/d1cc03202j |
0.652 |
|
| 2021 |
Gao ZG, Suresh RR, Jacobson KA. Pharmacological characterization of DPTN and other selective A adenosine receptor antagonists. Purinergic Signalling. 17: 737-746. PMID 34713378 DOI: 10.1007/s11302-021-09823-5 |
0.386 |
|
| 2021 |
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Southan C, Davies JA, Abbracchio MP, Alexander W, ... ... Jacobson KA, et al. THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors. British Journal of Pharmacology. 178: S27-S156. PMID 34529832 DOI: 10.1111/bph.15538 |
0.685 |
|
| 2021 |
Guo M, Bakhoda A, Gao ZG, Ramsey JM, Li Y, O'Conor KA, Kelleher AC, Eisenberg SM, Kang Y, Yan X, Javdan C, Fowler JS, Rice KC, Hooker JM, Jacobson KA, et al. Discovery of Highly Potent Adenosine A Receptor Agonists: Targeting Positron Emission Tomography Probes. Acs Chemical Neuroscience. PMID 34469110 DOI: 10.1021/acschemneuro.1c00397 |
0.403 |
|
| 2021 |
Lee Y, Hou X, Lee JH, Nayak A, Alexander V, Sharma PK, Chang H, Phan K, Gao ZG, Jacobson KA, Choi S, Jeong LS. Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A Adenosine Receptor Homology Models and Structural Network Analysis Can Predict This Boundary. Journal of Medicinal Chemistry. PMID 34435786 DOI: 10.1021/acs.jmedchem.1c00239 |
0.64 |
|
| 2021 |
Coppi E, Cherchi F, Lucarini E, Ghelardini C, Pedata F, Jacobson KA, Di Cesare Mannelli L, Pugliese AM, Salvemini D. Uncovering the Mechanisms of Adenosine Receptor-Mediated Pain Control: Focus on the A Receptor Subtype. International Journal of Molecular Sciences. 22. PMID 34360719 DOI: 10.3390/ijms22157952 |
0.543 |
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| 2021 |
Bednarska-Szczepaniak K, Mieczkowski A, Kierozalska A, Pavlović Saftić D, Głąbała K, Przygodzki T, Stańczyk L, Karolczak K, Watała C, Rao H, Gao ZG, Jacobson KA, Leśnikowski ZJ. Synthesis and evaluation of adenosine derivatives as A, A, A and A adenosine receptor ligands containing boron clusters as phenyl isosteres and selective A agonists. European Journal of Medicinal Chemistry. 223: 113607. PMID 34171656 DOI: 10.1016/j.ejmech.2021.113607 |
0.456 |
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| 2021 |
López-Cano M, Filgaira I, Nolen EG, Cabré G, Hernando J, Tosh DK, Jacobson KA, Soler C, Ciruela F. Optical control of adenosine A receptor function in psoriasis. Pharmacological Research. 105731. PMID 34157422 DOI: 10.1016/j.phrs.2021.105731 |
0.687 |
|
| 2021 |
Leduc-Pessah H, Xu C, Fan CY, Dalgarno R, Kohro Y, Sparanese S, Burke NN, Jacobson KA, Altier C, Salvemini D, Trang T. Spinal A adenosine receptor activation acutely restores morphine antinociception in opioid tolerant male rats. Journal of Neuroscience Research. PMID 34075613 DOI: 10.1002/jnr.24869 |
0.485 |
|
| 2021 |
Oliva P, Scortichini M, Dobelmann C, Jain S, Gopinatth V, Toti KS, Phung NB, Junker A, Jacobson KA. Structure-Activity Relationships of Pyrimidine Nucleotides Containing a 5'-α,β-Methylene Diphosphonate at the P2Y Receptor. Bioorganic & Medicinal Chemistry Letters. 128137. PMID 34048882 DOI: 10.1016/j.bmcl.2021.128137 |
0.847 |
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| 2021 |
Luongo L, Guida F, Maione S, Jacobson KA, Salvemini D. Adenosine Metabotropic Receptors in Chronic Pain Management. Frontiers in Pharmacology. 12: 651038. PMID 33935761 DOI: 10.3389/fphar.2021.651038 |
0.541 |
|
| 2021 |
Choi H, Jacobson KA, Yu J, Jeong LS. Design and Synthesis of 2,6-Disubstituted-4'-Selenoadenosine-5'-,-Dimethyluronamide Derivatives as Human A Adenosine Receptor Antagonists. Pharmaceuticals (Basel, Switzerland). 14. PMID 33920062 DOI: 10.3390/ph14040363 |
0.81 |
|
| 2021 |
Jung YH, Jain S, Gopinatth V, Phung NB, Gao ZG, Jacobson KA. Structure Activity Relationship of 3-Nitro-2-(trifluoromethyl)-2H-chromene Derivatives as P2Y Receptor Antagonists. Bioorganic & Medicinal Chemistry Letters. 128008. PMID 33831560 DOI: 10.1016/j.bmcl.2021.128008 |
0.445 |
|
| 2021 |
Godoy-Marín H, Duroux R, Jacobson KA, Soler C, Colino-Lage H, Jiménez-Sábado V, Montiel J, Hove-Madsen L, Ciruela F. Adenosine A Receptors Are Upregulated in Peripheral Blood Mononuclear Cells from Atrial Fibrillation Patients. International Journal of Molecular Sciences. 22. PMID 33801676 DOI: 10.3390/ijms22073467 |
0.654 |
|
| 2021 |
Jung YH, Salmaso V, Wen Z, Bennett JM, Phung NB, Lieberman DI, Gopinatth V, Randle JCR, Chen Z, Salvemini D, Karcz TP, Cook DN, Jacobson KA. Structure-Activity Relationship of Heterocyclic P2Y Receptor Antagonists: Removal of the Zwitterionic Character with Piperidine Bioisosteres. Journal of Medicinal Chemistry. PMID 33787273 DOI: 10.1021/acs.jmedchem.1c00164 |
0.695 |
|
| 2021 |
Tosh DK, Brackett CM, Jung YH, Gao ZG, Banerjee M, Blagg BSJ, Jacobson KA. Biological Evaluation of 5'-(-Ethylcarboxamido)adenosine Analogues as Grp94-Selective Inhibitors. Acs Medicinal Chemistry Letters. 12: 373-379. PMID 33738064 DOI: 10.1021/acsmedchemlett.0c00509 |
0.329 |
|
| 2021 |
Durante M, Squillace S, Lauro F, Giancotti LA, Coppi E, Cherchi F, Di Cesare Mannelli L, Ghelardini C, Kolar G, Wahlman C, Opejin A, Xiao C, Reitman ML, Tosh DK, Hawiger D, ... Jacobson KA, et al. Adenosine A3 agonists reverse neuropathic pain via T cell-mediated production of IL-10. The Journal of Clinical Investigation. PMID 33621215 DOI: 10.1172/JCI139299 |
0.506 |
|
| 2021 |
Matricon P, Suresh RR, Gao Z, Panel N, Jacobson KA, Carlsson J. Ligand design by targeting a binding site water Chemical Science. 12: 960-968. DOI: 10.1039/d0sc04938g |
0.573 |
|
| 2020 |
Matricon P, Suresh RR, Gao ZG, Panel N, Jacobson KA, Carlsson J. Ligand design by targeting a binding site water. Chemical Science. 12: 960-968. PMID 34163862 DOI: 10.1039/d0sc04938g |
0.621 |
|
| 2020 |
Sahin Z, Biltekin SN, Yurttas L, Berk B, Özhan Y, Sipahi H, Gao ZG, Jacobson KA, Demirayak Ş. Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition. European Journal of Medicinal Chemistry. 212: 113125. PMID 33422981 DOI: 10.1016/j.ejmech.2020.113125 |
0.357 |
|
| 2020 |
Jain S, Jacobson KA. Purinergic signaling in diabetes and metabolism. Biochemical Pharmacology. 114393. PMID 33359363 DOI: 10.1016/j.bcp.2020.114393 |
0.399 |
|
| 2020 |
An S, Kim G, Kim HJ, Ahn S, Kim HY, Ko H, Hyun YE, Nguyen M, Jeong J, Liu Z, Han J, Choi H, Yu J, Kim JW, Lee HW, ... Jacobson KA, et al. Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPARγ/δ Modulators. Journal of Medicinal Chemistry. PMID 33325691 DOI: 10.1021/acs.jmedchem.0c01874 |
0.806 |
|
| 2020 |
Jacobson KA, IJzerman AP, Müller CE. Medicinal chemistry of P2 and adenosine receptors: Common scaffolds adapted for multiple targets. Biochemical Pharmacology. 114311. PMID 33130128 DOI: 10.1016/j.bcp.2020.114311 |
0.711 |
|
| 2020 |
Liston TE, Hinz S, Müller CE, Holstein DM, Wendling J, Melton RJ, Campbell M, Korinek WS, Suresh RR, Sethre-Hofstad DA, Gao ZG, Tosh DK, Jacobson KA, Lechleiter JD. Nucleotide P2Y receptor agonists are in vitro and in vivo prodrugs of A/A adenosine receptor agonists: implications for roles of P2Y and A/A receptors in physiology and pathology. Purinergic Signalling. PMID 33129204 DOI: 10.1007/s11302-020-09732-z |
0.743 |
|
| 2020 |
Illes P, Müller CE, Jacobson KA, Grutter T, Nicke A, Fountain SJ, Kennedy C, Schmalzing G, Jarvis MF, Stojilkovic SS, King BF, Di Virgilio F. Update of P2X receptor properties and their pharmacology: IUPHAR Review 30. British Journal of Pharmacology. PMID 33125712 DOI: 10.1111/bph.15299 |
0.68 |
|
| 2020 |
Tosh DK, Salmaso V, Rao H, Campbell R, Bitant A, Gao ZG, Auchampach JA, Jacobson KA. Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A Receptor Agonists. Acs Medicinal Chemistry Letters. 11: 1935-1941. PMID 33062176 DOI: 10.1021/Acsmedchemlett.9B00637 |
0.764 |
|
| 2020 |
Jacobson KA, Salmaso V. Purinergic signaling: Impact of GPCR structures on rational drug design. Chemmedchem. PMID 32803849 DOI: 10.1002/cmdc.202000465 |
0.493 |
|
| 2020 |
Jacobson KA. Tribute to Prof. Geoffrey Burnstock: transition of purinergicsignaling to drug discovery. Purinergic Signalling. PMID 32794053 DOI: 10.1007/S11302-020-09717-Y |
0.448 |
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| 2020 |
Jung YH, Yu J, Wen Z, Salmaso V, Karcz TP, Phung NB, Chen Z, Duca S, Bennett JM, Dudas S, Salvemini D, Gao ZG, Cook DN, Jacobson KA. Exploration of Alternative Scaffolds for P2Y Receptor Antagonists Containing a Biaryl Core. Journal of Medicinal Chemistry. PMID 32787142 DOI: 10.1021/Acs.Jmedchem.0C00745 |
0.824 |
|
| 2020 |
Suresh RR, Jain S, Chen Z, Tosh DK, Ma Y, Podszun MC, Rotman Y, Salvemini D, Jacobson KA. Design and in vivo activity of A adenosine receptor agonist prodrugs. Purinergic Signalling. PMID 32720036 DOI: 10.1007/S11302-020-09715-0 |
0.591 |
|
| 2020 |
Abbracchio MP, Jacobson KA, Müller CE, Zimmermann H. Professor Dr. Geoffrey Burnstock (1929-2020). Purinergic Signalling. PMID 32613407 DOI: 10.1007/S11302-020-09709-Y |
0.536 |
|
| 2020 |
Mufti F, Jung YH, Giancotti LA, Yu J, Chen Z, Phung NB, Jacobson KA, Salvemini D. P2Y Receptor Antagonists Reverse Chronic Neuropathic Pain in a Mouse Model. Acs Medicinal Chemistry Letters. 11: 1281-1286. PMID 32551012 DOI: 10.1021/Acsmedchemlett.0C00115 |
0.776 |
|
| 2020 |
Salmaso V, Jacobson KA. In Silico Drug Design for Purinergic GPCRs: Overview on Molecular Dynamics Applied to Adenosine and P2Y Receptors. Biomolecules. 10. PMID 32466404 DOI: 10.3390/biom10060812 |
0.457 |
|
| 2020 |
Doyle TM, Largent-Milnes TM, Chen Z, Staikopoulos V, Esposito E, Delgarno R, Fan C, Tosh DK, Cuzzocrea S, Jacobson KA, Trang T, Hutchinson MR, Bennett GJ, Vanderah TW, Salvemini D.
The Journal of Pharmacology and Experimental Therapeutics. PMID 32434943 DOI: 10.1124/Jpet.120.000004 |
0.573 |
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| 2020 |
Jacobson KA, Gao ZG, Matricon P, Eddy MT, Carlsson J. A adenosine receptor antagonists: From caffeine to selective non-xanthines. British Journal of Pharmacology. PMID 32424811 DOI: 10.1111/Bph.15103 |
0.746 |
|
| 2020 |
Gao ZG, Toti KS, Campbell R, Suresh RR, Yang H, Jacobson KA. Allosteric Antagonism of the A Adenosine Receptor by a Series of Bitopic Ligands. Cells. 9. PMID 32408534 DOI: 10.3390/Cells9051200 |
0.523 |
|
| 2020 |
Lucarini E, Coppi E, Micheli L, Parisio C, Vona A, Cherchi F, Pugliese AM, Pedata F, Failli P, Palomino S, Wahl J, Largent-Milnes TM, Vanderah TW, Tosh DK, Jacobson KA, et al. Acute visceral pain relief mediated by A3AR agonists in rats: involvement of N-type voltage-gated calcium channels. Pain. PMID 32379223 DOI: 10.1097/J.Pain.0000000000001905 |
0.576 |
|
| 2020 |
Jacobson KA, Reitman ML. Adenosine-Related Mechanisms in Non-Adenosine Receptor Drugs. Cells. 9. PMID 32295065 DOI: 10.3390/Cells9040956 |
0.428 |
|
| 2020 |
Srivastava P, Cronin CG, Scranton VL, Jacobson KA, Liang BT, Verma R. Neuroprotective and neuro-rehabilitative effects of acute purinergic receptor P2X4 (P2X4R) blockade after ischemic stroke. Experimental Neurology. 113308. PMID 32289314 DOI: 10.1016/J.Expneurol.2020.113308 |
0.55 |
|
| 2020 |
Tosh DK, Salmaso V, Rao H, Bitant A, Fisher CL, Lieberman DI, Vorbrüggen H, Reitman ML, Gavrilova O, Gao ZG, Auchampach JA, Jacobson KA. Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A Adenosine Receptors: Affinity Enhancement by -(2-Phenylethyl) Substitution. Journal of Medicinal Chemistry. PMID 32271569 DOI: 10.1021/acs.jmedchem.0c00235 |
0.771 |
|
| 2020 |
Pottie E, Tosh DK, Gao ZG, Jacobson KA, Stove CP. Assessment of biased agonism at the A adenosine receptor using β-arrestin and miniGα recruitment assays. Biochemical Pharmacology. 113934. PMID 32224136 DOI: 10.1016/J.Bcp.2020.113934 |
0.52 |
|
| 2020 |
Jacobson KA, Giancotti LA, Lauro F, Mufti F, Salvemini D. Treatment of chronic neuropathic pain: purine receptor modulation. Pain. PMID 32187120 DOI: 10.1097/J.Pain.0000000000001857 |
0.658 |
|
| 2020 |
Lu Y, Qin S, Zhang B, Dai A, Cai X, Ma M, Gao ZG, Yang D, Stevens RC, Jacobson KA, Wang MW, Shui W. Correction to Accelerating the Throughput of Affinity Mass Spectrometry-Based Ligand Screening toward a G Protein-Coupled Receptor. Analytical Chemistry. PMID 32125824 DOI: 10.1021/Acs.Analchem.0C00754 |
0.577 |
|
| 2020 |
Jacobson KA, Delicado EG, Gachet C, Kennedy C, von Kügelgen I, Li B, Miras-Portugal MT, Novak I, Schöneberg T, Perez-Sen R, Thor D, Wu B, Yang Z, Müller CE. Update of P2Y Receptor Pharmacology: IUPHAR Review:"27". British Journal of Pharmacology. PMID 32037507 DOI: 10.1111/Bph.15005 |
0.699 |
|
| 2020 |
Shen JB, Toti KS, Chakraborty S, Kumar TS, Cronin C, Liang BT, Jacobson KA. Prevention and rescue of cardiac dysfunction by methanocarba adenosine monophosphonate derivatives. Purinergic Signalling. PMID 31989534 DOI: 10.1007/S11302-020-09688-0 |
0.57 |
|
| 2020 |
Jacobson KA, Kirk KL. John W. Daly - An Appreciation. Heterocycles. 79: 61-71. PMID 26160996 DOI: 10.3987/COM-08-S(D)Memoire-1 |
0.325 |
|
| 2020 |
Fisher CL, Bitant AA, Rothwell AC, Wan TC, Fallot LB, Suresh RR, Guo-Gao Z, Jacobson KA, Auchampach JA. Identification and Characterization of ‘Biased’ A
3
Adenosine Receptor Allosteric Modulators The Faseb Journal. 34: 1-1. DOI: 10.1096/Fasebj.2020.34.S1.04488 |
0.569 |
|
| 2019 |
Lanznaster D, Massari CM, Marková V, Šimková T, Duroux R, Jacobson KA, Fernández-Dueñas V, Tasca CI, Ciruela F. Adenosine A-A Receptor-Receptor Interaction: Contribution to Guanosine-Mediated Effects. Cells. 8. PMID 31847113 DOI: 10.3390/Cells8121630 |
0.732 |
|
| 2019 |
Federico S, Margiotta E, Moro S, Kozma E, Gao ZG, Jacobson KA, Spalluto G. Conjugable A adenosine receptor antagonists for the development of functionalized ligands and their use in fluorescent probes. European Journal of Medicinal Chemistry. 111886. PMID 31787357 DOI: 10.1016/J.Ejmech.2019.111886 |
0.856 |
|
| 2019 |
Ciancetta A, Rubio P, Lieberman DI, Jacobson KA. A adenosine receptor activation mechanisms: molecular dynamics analysis of inactive, active, and fully active states. Journal of Computer-Aided Molecular Design. PMID 31758354 DOI: 10.1007/S10822-019-00246-4 |
0.461 |
|
| 2019 |
Gao ZG, Jacobson KA. A Adenosine Receptor and Cancer. International Journal of Molecular Sciences. 20. PMID 31627281 DOI: 10.3390/Ijms20205139 |
0.453 |
|
| 2019 |
Stockstill K, Wahlman C, Braden K, Chen Z, Yosten GL, Tosh DK, Jacobson KA, Doyle TM, Samson WK, Salvemini D. Sexually dimorphic therapeutic response in bortezomib-induced neuropathic pain reveals altered pain physiology in female rodents. Pain. PMID 31490328 DOI: 10.1097/J.Pain.0000000000001697 |
0.598 |
|
| 2019 |
Salmaso V, Jacobson KA. Survey of ribose ring pucker of signaling nucleosides and nucleotides. Nucleosides, Nucleotides & Nucleic Acids. 1-20. PMID 31460850 DOI: 10.1080/15257770.2019.1658115 |
0.482 |
|
| 2019 |
Federico S, Margiotta E, Paoletta S, Kachler S, Klotz KN, Jacobson KA, Pastorin G, Moro S, Spalluto G. Pyrazolo[4,3-][1,2,4]triazolo[1,5-]pyrimidines to develop functionalized ligands to target adenosine receptors: fluorescent ligands as an example. Medchemcomm. 10: 1094-1108. PMID 31391881 DOI: 10.1039/C9Md00014C |
0.803 |
|
| 2019 |
Abel B, Tosh DK, Durell SR, Murakami M, Vahedi S, Jacobson KA, Ambudkar SV. Evidence for the Interaction of A Adenosine Receptor Agonists at the Drug-Binding Site(s) of Human P-glycoprotein (ABCB1). Molecular Pharmacology. PMID 31127007 DOI: 10.1124/Mol.118.115295 |
0.384 |
|
| 2019 |
Lu Y, Qin S, Zhang B, Dai A, Cai X, Ma M, Gao ZG, Yang D, Stevens RC, Jacobson KA, Wang MW, Shui W. Accelerating the Throughput of Affinity Mass Spectrometry-Based Ligand Screening towards a G Protein-Coupled Receptor. Analytical Chemistry. PMID 31094506 DOI: 10.1021/Acs.Analchem.9B00477 |
0.611 |
|
| 2019 |
Carmona-Rivera C, Khaznadar SS, Shwin KW, Irizarry-Caro JA, O'Neil LJ, Liu Y, Jacobson KA, Ombrello AK, Stone DL, Tsai WL, Kastner DL, Aksentijevich I, Kaplan MJ, Grayson PC. Deficiency of adenosine deaminase 2 triggers adenosine-mediated NETosis and TNF production in patients with DADA2. Blood. PMID 31015188 DOI: 10.1182/Blood.2018892752 |
0.411 |
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| 2019 |
Coppi E, Cherchi F, Fusco I, Failli P, Vona A, Dettori I, Gaviano L, Lucarini E, Jacobson KA, Tosh DK, Salvemini D, Ghelardini C, Pedata F, Di Cesare Mannelli L, Pugliese AM. Adenosine A3 receptor activation inhibits pronociceptive N-type Ca2+ currents and cell excitability in dorsal root ganglion neurons. Pain. 160: 1103-1118. PMID 31008816 DOI: 10.1097/J.Pain.0000000000001488 |
0.587 |
|
| 2019 |
Jacobson KA, Tosh DK, Jain S, Gao ZG. Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development. Frontiers in Cellular Neuroscience. 13: 124. PMID 30983976 DOI: 10.3389/fncel.2019.00124 |
0.374 |
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| 2019 |
Coppi E, Cherchi F, Fusco I, Failli P, Vona A, Dettori I, Gaviano L, Lucarini E, Jacobson KA, Tosh DK, Salvemini D, Ghelardini C, Pedata F, Di Cesare Mannelli L, Pugliese AM. Title: Adenosine A3 receptor activation inhibits pro-nociceptive N-type Ca2+ currents and cell excitability in dorsal root ganglion neurons. Pain. PMID 30938716 DOI: 10.1097/j.pain.0000000000001488 |
0.535 |
|
| 2019 |
Junker A, Renn C, Dobelmann C, Namasivayam V, Jain S, Losenkova K, Irjala H, Duca S, Balasubramanian R, Chakraborty S, Börgel F, Zimmermann H, Yegutkin GG, Müller CE, Jacobson KA. Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors. Journal of Medicinal Chemistry. PMID 30895781 DOI: 10.1021/Acs.Jmedchem.9B00164 |
0.805 |
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| 2019 |
Xiao C, Liu N, Jacobson KA, Gavrilova O, Reitman ML. Physiology and effects of nucleosides in mice lacking all four adenosine receptors. Plos Biology. 17: e3000161. PMID 30822301 DOI: 10.1371/Journal.Pbio.3000161 |
0.387 |
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| 2019 |
Cacciari B, Crepaldi P, Cheng CY, Bossi E, Spalluto G, Federico S, Jacobson KA, Cattaneo M. Structure Activity Relationship of 4-Amino-2-thiopyrimidine Derivatives as Platelet Aggregation Inhibitors. Medicinal Chemistry (Shariqah (United Arab Emirates)). PMID 30734681 DOI: 10.2174/1573406415666190208124534 |
0.538 |
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| 2019 |
Ciruela F, Jacobson KA. Editorial: Purinergic Pharmacology. Frontiers in Pharmacology. 10: 21. PMID 30728779 DOI: 10.3389/Fphar.2019.00021 |
0.685 |
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| 2019 |
Tosh DK, Rao H, Bitant A, Salmaso V, Mannes P, Lieberman DI, Vaughan KL, Mattison JA, Rothwell AC, Auchampach JA, Ciancetta A, Liu N, Cui Z, Gao ZG, Reitman ML, ... ... Jacobson KA, et al. Design and in Vivo Characterization of A Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series. Journal of Medicinal Chemistry. PMID 30605331 DOI: 10.1021/acs.jmedchem.8b01662 |
0.741 |
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| 2019 |
Jacobson KA, Tchilibon S, Joshi BV, Gao ZG. Chapter 13. A Adenosine Receptors. Annual Reports in Medicinal Chemistry. 38: 121-130. PMID 26640305 DOI: 10.1016/S0065-7743(03)38014-5 |
0.591 |
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| 2019 |
Zimmet J, Järlebark L, Hammarberg T, van Galen PJ, Jacobson KA, Heilbronn E. SYNTHESIS AND BIOLOGICAL ACTIVITY OF NOVEL 2-THIO DERIVATIVES OF ATP. Nucleosides & Nucleotides. 12: 1-20. PMID 25181577 DOI: 10.1080/07328319308016190 |
0.354 |
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| 2019 |
Kim HO, Hawes C, Towers P, Jacobson KA. RADIOLABELING AND EFFICIENT SYNTHESIS OF TRITIATED 2-CHLORO--(3-IODOBENZYL)ADENOSINE-5'--METHYLURON-AMIDE, A POTENT, SELECTIVE A ADENOSINE RECEPTOR AGONIST. Journal of Labelled Compounds & Radiopharmaceuticals. 38: 547-560. PMID 23598401 DOI: 10.1002/(Sici)1099-1344(199606)38:6<547::Aid-Jlcr870>3.0.Co;2-Y |
0.538 |
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| 2019 |
van Rhee AM, Jacobson KA. Molecular Architecture of G Protein-Coupled Receptors. Drug Development Research. 37: 1-38. PMID 21921973 DOI: 10.1002/(Sici)1098-2299(199601)37:1<1::Aid-Ddr1>3.0.Co;2-S |
0.508 |
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| 2019 |
JAIN S, TOSH DK, REITMAN M, JACOBSON KA. 280-LB: Role of A1 and A3 Adenosine Receptors in Whole Body Glucose Metabolism Diabetes. 68: 280-LB. DOI: 10.2337/DB19-280-LB |
0.322 |
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| 2019 |
Abbracchio M, Boeynaems J, Boyer JL, Burnstock G, Ceruti S, Fumagalli M, Gachet C, Hills R, Humphries RG, Inoue K, Jacobson KA, Kennedy C, King BF, Lecca D, Müller CE, et al. P2Y receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database Iuphar/Bps Guide to Pharmacology Cite. 2019. DOI: 10.2218/gtopdb/f52/2019.4 |
0.502 |
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| 2019 |
Fredholm BB, Frenguelli BG, Hills R, IJzerman AP, Jacobson KA, Klotz K, Linden J, Müller CE, Schwabe U, Stiles GL. Adenosine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database Iuphar/Bps Guide to Pharmacology Cite. 2019. DOI: 10.2218/gtopdb/f3/2019.4 |
0.839 |
|
| 2019 |
Xiao C, Liu N, Jacobson K, Gavrilova O, Reitman M. SAT-038 Physiology of Mice Lacking All Four Adenosine Receptors Journal of the Endocrine Society. 3. DOI: 10.1210/JS.2019-SAT-038 |
0.373 |
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| 2019 |
Verma R, Srivastava P, Cronin CG, Scranton V, Jacobson KA, Liang BT. Abstract WP143: Acute Treatment With Purinergic Receptor P2X4 Inhibitors Show Neuroprotective and Neuro-Rehabilitation Potential in Ischemic Stroke Stroke. 50. DOI: 10.1161/Str.50.Suppl_1.Wp143 |
0.534 |
|
| 2018 |
Yu J, Mannes P, Jung YH, Ciancetta A, Bitant A, Lieberman DI, Khaznadar S, Auchampach JA, Gao ZG, Jacobson KA. Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A adenosine receptor antagonists. Medchemcomm. 9: 1920-1932. PMID 30568760 DOI: 10.1039/C8Md00317C |
0.862 |
|
| 2018 |
Tosh DK, Ciancetta A, Mannes P, Warnick E, Janowsky A, Eshleman AJ, Gizewski E, Brust TF, Bohn LM, Auchampach JA, Gao ZG, Jacobson KA. Repurposing of a Nucleoside Scaffold from Adenosine Receptor Agonists to Opioid Receptor Antagonists. Acs Omega. 3: 12658-12678. PMID 30411015 DOI: 10.1021/acsomega.8b01237 |
0.772 |
|
| 2018 |
Guo M, Gao ZG, Tyler R, Stodden T, Li Y, Ramsey J, Zhao WJ, Wang GJ, Wiers CE, Fowler JS, Rice KC, Jacobson KA, Kim SW, Volkow ND. Preclinical evaluation of the first adenosine A receptor partial agonist radioligand for positron emission tomography (PET) imaging. Journal of Medicinal Chemistry. PMID 30359014 DOI: 10.1021/Acs.Jmedchem.8B01009 |
0.325 |
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| 2018 |
Storme J, Tosh DK, Gao ZG, Jacobson KA, Stove CP. Probing Structure-Activity Relationship in β-Arrestin2 Recruitment of Diversely Substituted Adenosine Derivatives. Biochemical Pharmacology. PMID 30292756 DOI: 10.1016/J.Bcp.2018.10.003 |
0.577 |
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| 2018 |
Liu X, Gao ZG, Wu Y, Stevens RC, Jacobson KA, Zhao S. Author Correction: Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y and P2Y receptors. Scientific Reports. 8: 11380. PMID 30038283 DOI: 10.1038/S41598-018-29406-6 |
0.562 |
|
| 2018 |
Yang C, Larin A, McKenna JT, Jacobson KA, Winston S, Strecker RE, Kalinchuk A, Basheer R, Brown RE. Activation of basal forebrain purinergic P2 receptors promotes wakefulness in mice. Scientific Reports. 8: 10730. PMID 30013200 DOI: 10.1038/S41598-018-29103-4 |
0.368 |
|
| 2018 |
Eddy MT, Gao ZG, Mannes P, Patel N, Jacobson KA, Katritch V, Stevens RC, Wüthrich K. Extrinsic Tryptophans as NMR Probes of Allosteric Coupling in Membrane Proteins: Application to the A2A Adenosine Receptor. Journal of the American Chemical Society. PMID 29874058 DOI: 10.1021/Jacs.8B03805 |
0.601 |
|
| 2018 |
Taura J, Nolen EG, Cabré G, Hernando J, Squarcialupi L, López-Cano M, Jacobson KA, Fernández-Dueñas V, Ciruela F. Remote control of movement disorders using a photoactive adenosine A receptor antagonist. Journal of Controlled Release : Official Journal of the Controlled Release Society. PMID 29859955 DOI: 10.1016/J.Jconrel.2018.05.033 |
0.752 |
|
| 2018 |
Liu X, Gao ZG, Wu Y, Stevens RC, Jacobson KA, Zhao S. Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y and P2Y receptors. Scientific Reports. 8: 8084. PMID 29795391 DOI: 10.1038/S41598-018-26577-0 |
0.655 |
|
| 2018 |
Yu J, Ciancetta A, Dudas S, Duca S, Lottermoser J, Jacobson KA. Structure-Guided Modification of Heterocyclic Antagonists of the P2Y Receptor. Journal of Medicinal Chemistry. PMID 29767967 DOI: 10.1021/Acs.Jmedchem.8B00168 |
0.782 |
|
| 2018 |
Carlin JL, Jain S, Duroux R, Suresh RR, Xiao C, Auchampach JA, Jacobson KA, Gavrilova O, Reitman ML. Activation of adenosine Aor Areceptors causes hypothermia in mice. Neuropharmacology. PMID 29548686 DOI: 10.1016/J.Neuropharm.2018.02.035 |
0.714 |
|
| 2018 |
Wahlman C, Doyle TM, Little JW, Luongo L, Janes K, Chen Z, Esposito E, Tosh DK, Cuzzocrea S, Jacobson KA, Salvemini D. Chemotherapy-induced pain is promoted by enhanced spinal adenosine kinase levels via astrocyte-dependent mechanisms. Pain. PMID 29419652 DOI: 10.1097/J.Pain.0000000000001177 |
0.581 |
|
| 2018 |
White KL, Eddy MT, Gao ZG, Han GW, Lian T, Deary A, Patel N, Jacobson KA, Katritch V, Stevens RC. Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling. Structure (London, England : 1993). PMID 29395784 DOI: 10.1016/J.Str.2017.12.013 |
0.585 |
|
| 2018 |
Xia L, Kyrizaki A, Tosh DK, van Duijl TT, Cornelia Roorda J, Jacobson KA, IJzerman AP, Heitman LH. A Binding Kinetics Study of Human Adenosine A3 Receptor Agonists. Biochemical Pharmacology. PMID 29305857 DOI: 10.1016/J.Bcp.2017.12.026 |
0.698 |
|
| 2018 |
Ciancetta A, Jacobson KA. Breakthrough in GPCR Crystallography and Its Impact on Computer-Aided Drug Design. Methods in Molecular Biology (Clifton, N.J.). 1705: 45-72. PMID 29188558 DOI: 10.1007/978-1-4939-7465-8_3 |
0.553 |
|
| 2018 |
Squillace S, Durante M, Opejin A, Hawiger D, Tosh D, Jacobson K, Salvemini D. CD4 + T cells and IL-10 are required for the beneficial effects exerted by A 3 AR agonists in neuropathic pain The Journal of Pain. 19: S81-S82. DOI: 10.1016/J.Jpain.2017.12.197 |
0.45 |
|
| 2017 |
Toti KS, Jain S, Ciancetta A, Balasubramanian R, Chakraborty S, Surujdin R, Shi ZD, Jacobson KA. Pyrimidine Nucleotides Containing a (S)-Methanocarba Ring as P2Y6 Receptor Agonists. Medchemcomm. 8: 1897-1908. PMID 29423136 DOI: 10.1039/C7Md00397H |
0.499 |
|
| 2017 |
Gao ZG, Jacobson KA. Purinergic Signaling in Mast Cell Degranulation and Asthma. Frontiers in Pharmacology. 8: 947. PMID 29311944 DOI: 10.3389/Fphar.2017.00947 |
0.508 |
|
| 2017 |
Eddy MT, Lee MY, Gao ZG, White KL, Didenko T, Horst R, Audet M, Stanczak P, McClary KM, Han GW, Jacobson KA, Stevens RC, Wüthrich K. Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor. Cell. PMID 29290469 DOI: 10.1016/J.Cell.2017.12.004 |
0.578 |
|
| 2017 |
Duroux R, Ciancetta A, Mannes P, Yu J, Boyapati S, Gizewski E, Yous S, Ciruela F, Auchampach JA, Gao ZG, Jacobson KA. Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners. Medchemcomm. 8: 1659-1667. PMID 29250307 DOI: 10.1039/C7Md00247E |
0.861 |
|
| 2017 |
Gao ZG, Inoue A, Jacobson KA. On the G protein-coupling selectivity of the native A2B adenosine receptor. Biochemical Pharmacology. PMID 29225130 DOI: 10.1016/J.Bcp.2017.12.003 |
0.378 |
|
| 2017 |
Ciancetta A, O'Connor RD, Paoletta S, Jacobson KA. Demystifying P2Y1 Receptor Ligand Recognition through Docking and Molecular Dynamics Analyses. Journal of Chemical Information and Modeling. PMID 29182323 DOI: 10.1021/Acs.Jcim.7B00528 |
0.486 |
|
| 2017 |
Du L, Gao ZG, Paoletta S, Wan TC, Gizewski ET, Barbour S, van Veldhoven JPD, IJzerman AP, Jacobson KA, Auchampach JA. Species differences and mechanism of action of A3 adenosine receptor allosteric modulators. Purinergic Signalling. PMID 29170977 DOI: 10.1007/S11302-017-9592-1 |
0.809 |
|
| 2017 |
Burnstock G, Jacobson KA, Christofi FL. Purinergic drug targets for gastrointestinal disorders. Current Opinion in Pharmacology. 37: 131-141. PMID 29149731 DOI: 10.1016/J.Coph.2017.10.011 |
0.432 |
|
| 2017 |
Gao ZG, Jacobson KA. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor. Molecular Pharmacology. PMID 28864555 DOI: 10.1124/Mol.117.109660 |
0.456 |
|
| 2017 |
Yu J, Ahn S, Kim HJ, Lee M, Ahn S, Kim J, Jin SH, Lee E, Kim G, Cheong JH, Jacobson KA, Jeong LS, Noh M. Polypharmacology of N6-(3-iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPAR δ Antagonist Activity Suggests Their Anti-diabetic Potential. Journal of Medicinal Chemistry. PMID 28799755 DOI: 10.1021/Acs.Jmedchem.7B00805 |
0.816 |
|
| 2017 |
Jacobson KA, Tosh DK, Toti KS, Ciancetta A. Polypharmacology of conformationally locked methanocarba nucleosides. Drug Discovery Today. PMID 28781163 DOI: 10.1016/J.Drudis.2017.07.013 |
0.454 |
|
| 2017 |
Matricon P, Ranganathan A, Warnick E, Gao ZG, Rudling A, Lambertucci C, Marucci G, Ezzati A, Jaiteh M, Dal Ben D, Jacobson KA, Carlsson J. Fragment optimization for GPCRs by molecular dynamics free energy calculations: Probing druggable subpockets of the A 2A adenosine receptor binding site. Scientific Reports. 7: 6398. PMID 28743961 DOI: 10.1038/S41598-017-04905-0 |
0.676 |
|
| 2017 |
Jacobson KA, Merighi S, Varani K, Borea PA, Baraldi S, Aghazadeh Tabrizi M, Romagnoli R, Baraldi PG, Ciancetta A, Tosh DK, Gao ZG, Gessi S. A3 Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy. Medicinal Research Reviews. PMID 28682469 DOI: 10.1002/Med.21456 |
0.495 |
|
| 2017 |
Salvemini D, Jacobson KA. Highly selective A3 adenosine receptor agonists relieve chronic neuropathic pain. Expert Opinion On Therapeutic Patents. PMID 28604241 DOI: 10.1080/13543776.2017.1341018 |
0.66 |
|
| 2017 |
Petrelli R, Scortichini M, Kachler S, Boccella S, Cerchia C, Torquati I, Del Bello F, Salvemini D, Novellino E, Luongo L, Maione S, Jacobson KA, Lavecchia A, Klotz KN, Cappellacci L. Exploring the role of N(6)-substituents in potent dual acting 5'-C-ethyl-tetrazolyl-adenosine derivatives: synthesis, binding, functional assays and antinociceptive effects in mice. Journal of Medicinal Chemistry. PMID 28447789 DOI: 10.1021/Acs.Jmedchem.7B00291 |
0.714 |
|
| 2017 |
Yu J, Zhao LX, Park J, Lee HW, Sahu PK, Cui M, Moss SM, Hammes E, Warnick E, Gao ZG, Noh M, Choi S, Ahn HC, Choi J, Jacobson KA, et al. N6-Substituted-5'-N-Methylcarbamoyl-4'-selenoadenosines as Potent and Selective A3 Adenosine Receptor Agonists with Unusual Sugar Puckering and Nucleobase Orientation. Journal of Medicinal Chemistry. PMID 28380296 DOI: 10.1021/Acs.Jmedchem.7B00241 |
0.811 |
|
| 2017 |
Tosh DK, Janowsky A, Eshleman AJ, Warnick E, Gao ZG, Chen Z, Gizewski E, Auchampach JA, Salvemini D, Jacobson KA. Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. Journal of Medicinal Chemistry. PMID 28319392 DOI: 10.1021/Acs.Jmedchem.7B00141 |
0.79 |
|
| 2017 |
Ciancetta A, Jacobson KA. Structural Probing and Molecular Modeling of the A₃ Adenosine Receptor: A Focus on Agonist Binding. Molecules (Basel, Switzerland). 22. PMID 28287473 DOI: 10.3390/Molecules22030449 |
0.58 |
|
| 2017 |
Durante M, Squillace S, Stockstill K, Wahlman C, Masini E, Tosh D, Jacobson K, Salvemini D. (193) Contribution of IL-10 and T cells in beneficial effects exerted by A 3 adenosine receptor agonists in blocking and reversing neuropathic pain The Journal of Pain. 18: S24. DOI: 10.1016/J.Jpain.2017.02.100 |
0.604 |
|
| 2017 |
Zhang H, Doyle T, Grenald S, Jacobson K, Salvemini D, Vanderah T. (192) Targeting A3 adenosine receptor in HIV-1 gp120-induced neuropathic pain The Journal of Pain. 18: S24. DOI: 10.1016/J.Jpain.2017.02.099 |
0.604 |
|
| 2016 |
Tosh DK, Ciancetta A, Warnick E, Crane S, Gao ZG, Jacobson KA. Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT2B/5HT2C Serotonin Receptor Antagonists. Journal of Medicinal Chemistry. PMID 27933810 DOI: 10.1021/Acs.Jmedchem.6B01183 |
0.64 |
|
| 2016 |
Carlin JL, Jain S, Gizewski E, Wan TC, Tosh DK, Xiao C, Auchampach JA, Jacobson KA, Gavrilova O, Reitman ML. Hypothermia in mouse is caused by adenosine A1 and A3 receptor agonists and AMP via three distinct mechanisms. Neuropharmacology. PMID 27914963 DOI: 10.1016/J.Neuropharm.2016.11.026 |
0.766 |
|
| 2016 |
Jacobson KA, Civan MM. Ocular Purine Receptors as Drug Targets in the Eye. Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association For Ocular Pharmacology and Therapeutics. PMID 27574786 DOI: 10.1089/Jop.2016.0090 |
0.688 |
|
| 2016 |
Lecchi A, Femia EA, Paoletta S, Dupuis A, Ohlmann P, Gachet C, Jacobson KA, Machura K, Podda GM, Zieger B, Cattaneo M. Inherited dysfunctional platelet P2Y12 receptor mutations associated with bleeding disorders. Hamostaseologie. 36. PMID 27487748 DOI: 10.5482/Hamo-16-03-0010 |
0.464 |
|
| 2016 |
Rodriguez D, Chakraborty S, Warnick E, Crane S, Gao ZG, O'Connor RD, Jacobson KA, Carlsson J. Structure-based screening of unchartered chemical space for atypical adenosine receptor agonists. Acs Chemical Biology. PMID 27439119 DOI: 10.1021/Acschembio.6B00357 |
0.705 |
|
| 2016 |
Sesma JI, Weitzer CD, Livraghi-Butrico A, Dang H, Donaldson S, Alexis NE, Jacobson KA, Harden TK, Lazarowski ER. UDP-glucose promotes neutrophil recruitment in the lung. Purinergic Signalling. PMID 27421735 DOI: 10.1007/S11302-016-9524-5 |
0.512 |
|
| 2016 |
Toti KS, Osborne D, Ciancetta A, Boison D, Jacobson KA. South (S)- and North (N)-Methanocarba-7-Deazaadenosine Analogues as Inhibitors of Human Adenosine Kinase. Journal of Medicinal Chemistry. PMID 27410258 DOI: 10.1021/Acs.Jmedchem.6B00689 |
0.378 |
|
| 2016 |
Junker A, Balasubramanian R, Ciancetta A, Uliassi E, Kiselev E, Martiriggiano C, Trujillo K, Mtchedlidze G, Birdwell L, Brown KA, Harden TK, Jacobson KA. Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists. Journal of Medicinal Chemistry. PMID 27331270 DOI: 10.1021/Acs.Jmedchem.6B00044 |
0.847 |
|
| 2016 |
Baltos JA, Paoletta S, Nguyen AT, Gregory KJ, Tosh DK, Christopoulos A, Jacobson KA, May LT. Structure-Activity Analysis of Biased Agonism at the Human Adenosine A3 Receptor. Molecular Pharmacology. PMID 27136943 DOI: 10.1124/Mol.116.103283 |
0.533 |
|
| 2016 |
Gao ZG, Jacobson KA. On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin. Biochemical Pharmacology. PMID 26954502 DOI: 10.1016/J.Bcp.2016.03.003 |
0.43 |
|
| 2016 |
Tosh DK, Ciancetta A, Warnick E, O'Connor R, Chen Z, Gizewski E, Crane S, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA. Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists. Journal of Medicinal Chemistry. PMID 26890707 DOI: 10.1021/Acs.Jmedchem.5B01998 |
0.806 |
|
| 2016 |
Janowsky A, Tosh DK, Eshleman AJ, Jacobson KA. Rigid adenine nucleoside derivatives as novel modulators of the human sodium symporters for dopamine and other neurotransmitters. The Journal of Pharmacology and Experimental Therapeutics. PMID 26813929 DOI: 10.1124/Jpet.115.229666 |
0.456 |
|
| 2016 |
Janes K, Symons-Liguori AM, Jacobson KA, Salvemini D. Identification of A3 adenosine receptor agonists as novel non-narcotic analgesics. British Journal of Pharmacology. PMID 26804983 DOI: 10.1111/Bph.13446 |
0.672 |
|
| 2015 |
Jacobson KA, Müller CE. Medicinal Chemistry of Adenosine, P2Y and P2X Receptors. Neuropharmacology. PMID 26686393 DOI: 10.1016/J.Neuropharm.2015.12.001 |
0.733 |
|
| 2015 |
Carlin JL, Tosh DK, Xiao C, Pinol RA, Chen Z, Salvemini D, Gavrilova O, Jacobson KA, Reitman ML. Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice that is Dependent on Central Histamine H1 Receptors. The Journal of Pharmacology and Experimental Therapeutics. PMID 26606937 DOI: 10.1124/Jpet.115.229872 |
0.682 |
|
| 2015 |
Kiselev E, Balasubramanian R, Uliassi E, Brown KA, Trujillo K, Katritch V, Hammes E, Stevens RC, Harden TK, Jacobson KA. Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y14 receptor. Bioorganic & Medicinal Chemistry Letters. 25: 4733-9. PMID 26303895 DOI: 10.1016/J.Bmcl.2015.08.021 |
0.854 |
|
| 2015 |
Jacobson KA. New paradigms in GPCR drug discovery. Biochemical Pharmacology. PMID 26265138 DOI: 10.1016/J.Bcp.2015.08.085 |
0.421 |
|
| 2015 |
Serchov T, Clement HW, Schwarz MK, Iasevoli F, Tosh DK, Idzko M, Jacobson KA, de Bartolomeis A, Normann C, Biber K, van Calker D. Increased Signaling via Adenosine A1 Receptors, Sleep Deprivation, Imipramine, and Ketamine Inhibit Depressive-like Behavior via Induction of Homer1a. Neuron. 87: 549-62. PMID 26247862 DOI: 10.1016/J.Neuron.2015.07.010 |
0.342 |
|
| 2015 |
Tosh DK, Paoletta S, Chen Z, Crane S, Lloyd J, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA. Structure-Based Design, Synthesis by Click Chemistry and in Vivo Activity of Highly Selective A3 Adenosine Receptor Agonists. Medchemcomm. 6: 555-563. PMID 26236460 DOI: 10.1039/C4Md00571F |
0.817 |
|
| 2015 |
Fang ZZ, Tosh DK, Tanaka N, Wang H, Krausz KW, O'Connor R, Jacobson KA, Gonzalez FJ. Metabolic mapping of A3 adenosine receptor agonist MRS5980. Biochemical Pharmacology. PMID 26212548 DOI: 10.1016/J.Bcp.2015.07.007 |
0.338 |
|
| 2015 |
Paoletta S, Sabbadin D, von Kügelgen I, Hinz S, Katritch V, Hoffmann K, Abdelrahman A, Straßburger J, Baqi Y, Zhao Q, Stevens RC, Moro S, Müller CE, Jacobson KA. Modeling ligand recognition at the P2Y12 receptor in light of X-ray structural information. Journal of Computer-Aided Molecular Design. PMID 26194851 DOI: 10.1007/S10822-015-9858-Z |
0.81 |
|
| 2015 |
Tosh DK, Crane S, Chen Z, Paoletta S, Gao ZG, Gizewski E, Auchampach JA, Salvemini D, Jacobson KA. Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy. Acs Medicinal Chemistry Letters. 6: 804-8. PMID 26191370 DOI: 10.1021/Acsmedchemlett.5B00150 |
0.84 |
|
| 2015 |
Tosh DK, Padia J, Salvemini D, Jacobson KA. Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain. Purinergic Signalling. PMID 26111639 DOI: 10.1007/S11302-015-9459-2 |
0.611 |
|
| 2015 |
Jacobson KA, Gao ZG, Paoletta S, Kiselev E, Chakraborty S, Jayasekara PS, Balasubramanian R, Tosh DK. John Daly Lecture: Structure-guided Drug Design for Adenosine and P2Y Receptors. Computational and Structural Biotechnology Journal. 13: 286-98. PMID 25973142 DOI: 10.1016/J.Csbj.2014.10.004 |
0.608 |
|
| 2015 |
Ciruela F, Fernández-Dueñas V, Jacobson KA. Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands. Neuropharmacology. PMID 25890205 DOI: 10.1016/J.Neuropharm.2015.04.001 |
0.741 |
|
| 2015 |
Ford A, Castonguay A, Cottet M, Little JW, Chen Z, Symons-Liguori AM, Doyle T, Egan TM, Vanderah TW, De Konnick Y, Tosh DK, Jacobson KA, Salvemini D. Engagement of the GABA to KCC2 signaling pathway contributes to the analgesic effects of A3AR agonists in neuropathic pain. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 35: 6057-67. PMID 25878279 DOI: 10.1523/Jneurosci.4495-14.2015 |
0.543 |
|
| 2015 |
Trujillo K, Paoletta S, Kiselev E, Jacobson KA. Molecular modeling of the human P2Y14 receptor: A template for structure-based design of selective agonist ligands. Bioorganic & Medicinal Chemistry. 23: 4056-64. PMID 25868749 DOI: 10.1016/J.Bmc.2015.03.042 |
0.53 |
|
| 2015 |
Jacobson KA, Paoletta S, Katritch V, Wu B, Gao ZG, Zhao Q, Stevens RC, Kiselev E. Nucleotides Acting at P2Y Receptors: Connecting Structure and Function. Molecular Pharmacology. 88: 220-30. PMID 25837834 DOI: 10.1124/Mol.114.095711 |
0.656 |
|
| 2015 |
Zhang D, Gao ZG, Zhang K, Kiselev E, Crane S, Wang J, Paoletta S, Yi C, Ma L, Zhang W, Han GW, Liu H, Cherezov V, Katritch V, Jiang H, ... ... Jacobson KA, et al. Two disparate ligand-binding sites in the human P2Y1 receptor. Nature. 520: 317-21. PMID 25822790 DOI: 10.1038/Nature14287 |
0.637 |
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| 2015 |
Azroyan A, Cortez-Retamozo V, Bouley R, Liberman R, Ruan YC, Kiselev E, Jacobson KA, Pittet MJ, Brown D, Breton S. Renal intercalated cells sense and mediate inflammation via the P2Y14 receptor. Plos One. 10: e0121419. PMID 25799465 DOI: 10.1371/Journal.Pone.0121419 |
0.333 |
|
| 2015 |
Yang R, Beqiri D, Shen JB, Redden JM, Dodge-Kafka K, Jacobson KA, Liang BT. P2X4 receptor-eNOS signaling pathway in cardiac myocytes as a novel protective mechanism in heart failure. Computational and Structural Biotechnology Journal. 13: 1-7. PMID 25750695 DOI: 10.1016/J.Csbj.2014.11.002 |
0.63 |
|
| 2015 |
Rodríguez D, Gao ZG, Moss SM, Jacobson KA, Carlsson J. Molecular docking screening using agonist-bound GPCR structures: probing the A2A adenosine receptor. Journal of Chemical Information and Modeling. 55: 550-63. PMID 25625646 DOI: 10.1021/Ci500639G |
0.744 |
|
| 2015 |
Lecchi A, Razzari C, Paoletta S, Dupuis A, Nakamura L, Ohlmann P, Gachet C, Jacobson KA, Zieger B, Cattaneo M. Identification of a new dysfunctional platelet P2Y12 receptor variant associated with bleeding diathesis. Blood. 125: 1006-13. PMID 25428217 DOI: 10.1182/Blood-2013-07-517896 |
0.497 |
|
| 2015 |
Little JW, Ford A, Symons-Liguori AM, Chen Z, Janes K, Doyle T, Xie J, Luongo L, Tosh DK, Maione S, Bannister K, Dickenson AH, Vanderah TW, Porreca F, Jacobson KA, et al. Endogenous adenosine A3 receptor activation selectively alleviates persistent pain states. Brain : a Journal of Neurology. 138: 28-35. PMID 25414036 DOI: 10.1093/Brain/Awu330 |
0.573 |
|
| 2015 |
Janes K, Wahlman C, Little JW, Doyle T, Tosh DK, Jacobson KA, Salvemini D. Spinal neuroimmune activation is independent of T-cell infiltration and attenuated by A3 adenosine receptor agonists in a model of oxaliplatin-induced peripheral neuropathy. Brain, Behavior, and Immunity. 44: 91-9. PMID 25220279 DOI: 10.1016/J.Bbi.2014.08.010 |
0.562 |
|
| 2015 |
Tosh DK, Paoletta S, Chen Z, Crane S, Lloyd J, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA. Structure-based design, synthesis by click chemistry and in vivo activity of highly selective A3 adenosine receptor agonists Medchemcomm. 6: 555-563. DOI: 10.1039/c4md00571f |
0.679 |
|
| 2015 |
Little J, Janes K, Chen Z, Wahlman C, Tosh D, Jacobson K, Salvemini D. (326) Supraspinal adenosine A3 receptor (A3AR) activation reverses chemotherapy-induced neuropathic pain through an IL-10 dependent mechanism The Journal of Pain. 16: S57. DOI: 10.1016/J.Jpain.2015.01.244 |
0.619 |
|
| 2015 |
Tosh DK, Padia J, Salvemini D, Jacobson KA. Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain Purinergic Signalling. DOI: 10.1007/s11302-015-9459-2 |
0.606 |
|
| 2014 |
Balasubramanian R, Robaye B, Boeynaems JM, Jacobson KA. Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists. Plos One. 9: e116203. PMID 25549240 DOI: 10.1371/Journal.Pone.0116203 |
0.327 |
|
| 2014 |
Jacobson KA, Costanzi S, Paoletta S. Computational studies to predict or explain G protein coupled receptor polypharmacology. Trends in Pharmacological Sciences. 35: 658-63. PMID 25458540 DOI: 10.1016/J.Tips.2014.10.009 |
0.744 |
|
| 2014 |
Tosh DK, Finley A, Paoletta S, Moss SM, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA. In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists. Journal of Medicinal Chemistry. 57: 9901-14. PMID 25422861 DOI: 10.1021/Jm501021N |
0.819 |
|
| 2014 |
Cohen S, Barer F, Bar-Yehuda S, IJzerman AP, Jacobson KA, Fishman P. A₃ adenosine receptor allosteric modulator induces an anti-inflammatory effect: in vivo studies and molecular mechanism of action. Mediators of Inflammation. 2014: 708746. PMID 25374446 DOI: 10.1155/2014/708746 |
0.567 |
|
| 2014 |
Kiselev E, Barrett MO, Katritch V, Paoletta S, Weitzer CD, Brown KA, Hammes E, Yin AL, Zhao Q, Stevens RC, Harden TK, Jacobson KA. Exploring a 2-naphthoic acid template for the structure-based design of P2Y14 receptor antagonist molecular probes. Acs Chemical Biology. 9: 2833-42. PMID 25299434 DOI: 10.1021/Cb500614P |
0.773 |
|
| 2014 |
Fernández-Dueñas V, Gómez-Soler M, López-Cano M, Taura JJ, Ledent C, Watanabe M, Jacobson KA, Vilardaga JP, Ciruela F. Uncovering caffeine's adenosine A2A receptor inverse agonism in experimental parkinsonism. Acs Chemical Biology. 9: 2496-501. PMID 25268872 DOI: 10.1021/Cb5005383 |
0.714 |
|
| 2014 |
Bahamonde MI, Taura J, Paoletta S, Gakh AA, Chakraborty S, Hernando J, Fernández-Dueñas V, Jacobson KA, Gorostiza P, Ciruela F. Photomodulation of G protein-coupled adenosine receptors by a novel light-switchable ligand. Bioconjugate Chemistry. 25: 1847-54. PMID 25248077 DOI: 10.1021/Bc5003373 |
0.817 |
|
| 2014 |
Janes K, Esposito E, Doyle T, Cuzzocrea S, Tosh DK, Jacobson KA, Salvemini D. A3 adenosine receptor agonist prevents the development of paclitaxel-induced neuropathic pain by modulating spinal glial-restricted redox-dependent signaling pathways. Pain. 155: 2560-7. PMID 25242567 DOI: 10.1016/J.Pain.2014.09.016 |
0.563 |
|
| 2014 |
Moss SM, Jayasekara PS, Paoletta S, Gao ZG, Jacobson KA. Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor. Acs Medicinal Chemistry Letters. 5: 1043-8. PMID 25221664 DOI: 10.1021/Ml5002486 |
0.562 |
|
| 2014 |
Dix AV, Moss SM, Phan K, Hoppe T, Paoletta S, Kozma E, Gao ZG, Durell SR, Jacobson KA, Appella DH. Programmable nanoscaffolds that control ligand display to a G-protein-coupled receptor in membranes to allow dissection of multivalent effects. Journal of the American Chemical Society. 136: 12296-303. PMID 25116377 DOI: 10.1021/Ja504288S |
0.833 |
|
| 2014 |
Ciruela F, Jacobson KA, Fernández-Dueñas V. Portraying G protein-coupled receptors with fluorescent ligands. Acs Chemical Biology. 9: 1918-28. PMID 25010291 DOI: 10.1021/Cb5004042 |
0.713 |
|
| 2014 |
Tosh DK, Paoletta S, Chen Z, Moss SM, Gao ZG, Salvemini D, Jacobson KA. Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor. Bioorganic & Medicinal Chemistry Letters. 24: 3302-6. PMID 24969016 DOI: 10.1016/J.Bmcl.2014.06.006 |
0.711 |
|
| 2014 |
Toti KS, Moss SM, Paoletta S, Gao ZG, Jacobson KA, Van Calenbergh S. Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators. Bioorganic & Medicinal Chemistry. 22: 4257-68. PMID 24931275 DOI: 10.1016/J.Bmc.2014.05.036 |
0.434 |
|
| 2014 |
Ochoa-Cortes F, Liñán-Rico A, Jacobson KA, Christofi FL. Potential for developing purinergic drugs for gastrointestinal diseases. Inflammatory Bowel Diseases. 20: 1259-87. PMID 24859298 DOI: 10.1097/Mib.0000000000000047 |
0.393 |
|
| 2014 |
Paoletta S, Tosh DK, Salvemini D, Jacobson KA. Structural probing of off-target G protein-coupled receptor activities within a series of adenosine/adenine congeners. Plos One. 9: e97858. PMID 24859150 DOI: 10.1371/Journal.Pone.0097858 |
0.729 |
|
| 2014 |
Gao ZG, Balasubramanian R, Kiselev E, Wei Q, Jacobson KA. Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor. Biochemical Pharmacology. 90: 297-306. PMID 24853985 DOI: 10.1016/J.Bcp.2014.05.008 |
0.475 |
|
| 2014 |
Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Müller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, et al. Agonist-bound structure of the human P2Y12 receptor. Nature. 509: 119-22. PMID 24784220 DOI: 10.1038/Nature13288 |
0.689 |
|
| 2014 |
Jayasekara PS, Barrett MO, Ball CB, Brown KA, Hammes E, Balasubramanian R, Harden TK, Jacobson KA. 4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors. Journal of Medicinal Chemistry. 57: 3874-83. PMID 24712832 DOI: 10.1021/Jm500367E |
0.692 |
|
| 2014 |
Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Müller CE, Yang H, Jiang H, ... ... Jacobson KA, et al. Structure of the human P2Y12 receptor in complex with an antithrombotic drug. Nature. 509: 115-8. PMID 24670650 DOI: 10.1038/Nature13083 |
0.669 |
|
| 2014 |
Yang T, Shen JB, Yang R, Redden J, Dodge-Kafka K, Grady J, Jacobson KA, Liang BT. Novel protective role of endogenous cardiac myocyte P2X4 receptors in heart failure. Circulation. Heart Failure. 7: 510-8. PMID 24622244 DOI: 10.1161/Circheartfailure.113.001023 |
0.601 |
|
| 2014 |
Leung CT, Li A, Banerjee J, Gao ZG, Kambayashi T, Jacobson KA, Civan MM. The role of activated adenosine receptors in degranulation of human LAD2 mast cells. Purinergic Signalling. 10: 465-75. PMID 24595664 DOI: 10.1007/S11302-014-9409-4 |
0.681 |
|
| 2014 |
Nayak A, Chandra G, Hwang I, Kim K, Hou X, Kim HO, Sahu PK, Roy KK, Yoo J, Lee Y, Cui M, Choi S, Moss SM, Phan K, Gao ZG, ... ... Jacobson KA, et al. Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N(6)-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists. Journal of Medicinal Chemistry. 57: 1344-54. PMID 24456490 DOI: 10.1021/Jm4015313 |
0.644 |
|
| 2014 |
Fernández-Dueñas V, Jacobson K, Ciruela F. Adenosine A2A Receptor Ligand Binding Experiments by Using Real-time Single-cell FRET Bio-Protocol. 4. DOI: 10.21769/bioprotoc.1070 |
0.725 |
|
| 2014 |
Jacobson K, Ciruela F. Synthesis of the Adenosine A2A Receptor Fluorescent Agonist MRS5424 Bio-Protocol. 4. DOI: 10.21769/BIOPROTOC.1069 |
0.751 |
|
| 2014 |
Maloy C, Janes K, Bryant L, Tosh D, Jacobson K, Salvemini D. (336) A3 adenosine receptor agonists reverse established oxaliplatin-induced neuropathic pain through an IL-10 mediated mechanism of action in spinal cord The Journal of Pain. 15: S60. DOI: 10.1016/J.Jpain.2014.01.246 |
0.607 |
|
| 2014 |
Little J, Chen Z, Ford A, Janes K, Doyle T, Tosh D, Jacobson K, Salvemini D. (297) Central adenosine A3 receptor (A3AR) activation reverses neuropathic pain The Journal of Pain. 15: S50. DOI: 10.1016/J.Jpain.2014.01.207 |
0.606 |
|
| 2013 |
Jayasekara PS, Barrett MO, Ball CB, Brown KA, Kozma E, Costanzi S, Squarcialupi L, Balasubramanian R, Maruoka H, Jacobson KA. 4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2Y6 receptor. Medchemcomm. 4: 1156-1165. PMID 26161252 DOI: 10.1039/C3Md00132F |
0.858 |
|
| 2013 |
Tosh DK, Jacobson KA. Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches. Medchemcomm. 2013: 619-630. PMID 26161251 DOI: 10.1039/C2Md20348K |
0.564 |
|
| 2013 |
Jacobson KA. Crystal structures of the A2A adenosine receptor and their use in medicinal chemistry. In Silico Pharmacology. 1: 22. PMID 24660138 DOI: 10.1186/2193-9616-1-22 |
0.426 |
|
| 2013 |
Gao ZG, Jacobson KA. Allosteric modulation and functional selectivity of G protein-coupled receptors. Drug Discovery Today. Technologies. 10: e237-43. PMID 24050274 DOI: 10.1016/J.Ddtec.2012.08.004 |
0.497 |
|
| 2013 |
Hochhauser E, Cohen R, Waldman M, Maksin A, Isak A, Aravot D, Jayasekara PS, Müller CE, Jacobson KA, Shainberg A. P2Y2 receptor agonist with enhanced stability protects the heart from ischemic damage in vitro and in vivo. Purinergic Signalling. 9: 633-42. PMID 23828651 DOI: 10.1007/S11302-013-9374-3 |
0.44 |
|
| 2013 |
Paoletta S, Tosh DK, Finley A, Gizewski ET, Moss SM, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA. Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain. Journal of Medicinal Chemistry. 56: 5949-63. PMID 23789857 DOI: 10.1021/Jm4007966 |
0.805 |
|
| 2013 |
Fernández-Dueñas V, Gómez-Soler M, Morató X, Núñez F, Das A, Kumar TS, Jaumà S, Jacobson KA, Ciruela F. Dopamine D(2) receptor-mediated modulation of adenosine A(2A) receptor agonist binding within the A(2A)R/D(2)R oligomer framework. Neurochemistry International. 63: 42-6. PMID 23619397 DOI: 10.1016/J.Neuint.2013.04.006 |
0.747 |
|
| 2013 |
Jacobson KA. Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates. Journal of Medicinal Chemistry. 56: 3749-67. PMID 23597047 DOI: 10.1021/Jm400422S |
0.546 |
|
| 2013 |
Barrett MO, Sesma JI, Ball CB, Jayasekara PS, Jacobson KA, Lazarowski ER, Harden TK. A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils. Molecular Pharmacology. 84: 41-9. PMID 23592514 DOI: 10.1124/Mol.113.085654 |
0.689 |
|
| 2013 |
Zhou S, Yang T, Jacobson KA, Liang BT. The therapeutic effect of 2-cyclohexylthio-AMP in heart failure. Journal of Cardiovascular Pharmacology. 61: 553-9. PMID 23474842 DOI: 10.1097/Fjc.0B013E31828E8758 |
0.562 |
|
| 2013 |
Kozma E, Gizewski ET, Tosh DK, Squarcialupi L, Auchampach JA, Jacobson KA. Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor. Biochemical Pharmacology. 85: 1171-81. PMID 23376019 DOI: 10.1016/J.Bcp.2013.01.021 |
0.847 |
|
| 2013 |
Balasubramanian R, Maruoka H, Jayasekara PS, Gao ZG, Jacobson KA. AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells. Biochemical Pharmacology. 85: 991-8. PMID 23333427 DOI: 10.1016/J.Bcp.2012.11.029 |
0.377 |
|
| 2013 |
Jacobson KA, Costanzi S, Deflorian F. Probing GPCR structure: adenosine and P2Y nucleotide receptors. Methods in Enzymology. 520: 199-217. PMID 23332701 DOI: 10.1016/B978-0-12-391861-1.00009-5 |
0.729 |
|
| 2013 |
Wei Q, Costanzi S, Balasubramanian R, Gao ZG, Jacobson KA. A2B adenosine receptor blockade inhibits growth of prostate cancer cells. Purinergic Signalling. 9: 271-80. PMID 23315335 DOI: 10.1007/S11302-012-9350-3 |
0.661 |
|
| 2013 |
Kumar TS, Yang T, Mishra S, Cronin C, Chakraborty S, Shen JB, Liang BT, Jacobson KA. 5'-Phosphate and 5'-phosphonate ester derivatives of (N)-methanocarba adenosine with in vivo cardioprotective activity. Journal of Medicinal Chemistry. 56: 902-14. PMID 23286881 DOI: 10.1021/Jm301372C |
0.614 |
|
| 2013 |
Kozma E, Jayasekara PS, Squarcialupi L, Paoletta S, Moro S, Federico S, Spalluto G, Jacobson KA. Fluorescent ligands for adenosine receptors. Bioorganic & Medicinal Chemistry Letters. 23: 26-36. PMID 23200243 DOI: 10.1016/J.Bmcl.2012.10.112 |
0.819 |
|
| 2013 |
Jayasekara PS, Phan K, Tosh DK, Kumar TS, Moss SM, Zhang G, Barchi JJ, Gao ZG, Jacobson KA. Modulation of G protein-coupled adenosine receptors by strategically functionalized agonists and antagonists immobilized on gold nanoparticles. Purinergic Signalling. 9: 183-98. PMID 23179047 DOI: 10.1007/S11302-012-9338-Z |
0.534 |
|
| 2013 |
Gao ZG, Wei Q, Jayasekara MP, Jacobson KA. The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells. Purinergic Signalling. 9: 31-40. PMID 22825617 DOI: 10.1007/S11302-012-9325-4 |
0.342 |
|
| 2013 |
Jayasekara PS, Barrett MO, Ball CB, Brown KA, Kozma E, Costanzi S, Squarcialupi L, Balasubramanian R, Maruoka H, Jacobson KA. 4-Alkyloxyimino-cytosine nucleotides: Tethering approaches to molecular probes for the P2Y6 receptor Medchemcomm. 4: 1156-1165. DOI: 10.1039/c3md00132f |
0.845 |
|
| 2013 |
Tosh DK, Jacobson KA. Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: Synthetic approaches Medchemcomm. 4: 619-630. DOI: 10.1039/c2md20348k |
0.345 |
|
| 2012 |
Carlsson J, Tosh DK, Phan K, Gao ZG, Jacobson KA. Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists. Acs Medicinal Chemistry Letters. 3: 715-720. PMID 23342198 DOI: 10.1021/Ml300097G |
0.747 |
|
| 2012 |
Jacobson KA, Jayasekara MP, Costanzi S. Molecular Structure of P2Y Receptors: Mutagenesis, Modeling, and Chemical Probes. Wiley Interdisciplinary Reviews. Membrane Transport and Signaling. 1. PMID 23336097 DOI: 10.1002/wmts.68 |
0.722 |
|
| 2012 |
Kolb P, Phan K, Gao ZG, Marko AC, Sali A, Jacobson KA. Limits of ligand selectivity from docking to models: in silico screening for A(1) adenosine receptor antagonists. Plos One. 7: e49910. PMID 23185482 DOI: 10.1371/Journal.Pone.0049910 |
0.55 |
|
| 2012 |
Tosh DK, Paoletta S, Phan K, Gao ZG, Jacobson KA. Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions. Acs Medicinal Chemistry Letters. 3: 596-601. PMID 23145215 DOI: 10.1021/Ml300107E |
0.499 |
|
| 2012 |
Fernández-Dueñas V, Gómez-Soler M, Jacobson KA, Kumar ST, Fuxe K, Borroto-Escuela DO, Ciruela F. Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R. Journal of Neurochemistry. 123: 373-84. PMID 22924752 DOI: 10.1111/J.1471-4159.2012.07956.X |
0.726 |
|
| 2012 |
Tosh DK, Paoletta S, Deflorian F, Phan K, Moss SM, Gao ZG, Jiang X, Jacobson KA. Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity. Journal of Medicinal Chemistry. 55: 8075-90. PMID 22921089 DOI: 10.1021/Jm300965A |
0.579 |
|
| 2012 |
Costanzi S, Santhosh Kumar T, Balasubramanian R, Kendall Harden T, Jacobson KA. Virtual screening leads to the discovery of novel non-nucleotide P2Yâ‚ receptor antagonists. Bioorganic & Medicinal Chemistry. 20: 5254-61. PMID 22831801 DOI: 10.1016/J.Bmc.2012.06.044 |
0.741 |
|
| 2012 |
Jacobson KA, Costanzi S. New insights for drug design from the X-ray crystallographic structures of G-protein-coupled receptors. Molecular Pharmacology. 82: 361-71. PMID 22695719 DOI: 10.1124/Mol.112.079335 |
0.719 |
|
| 2012 |
Högberg C, Gidlöf O, Deflorian F, Jacobson KA, Abdelrahman A, Müller CE, Olde B, Erlinge D. Farnesyl pyrophosphate is an endogenous antagonist to ADP-stimulated P2Yâ‚â‚‚ receptor-mediated platelet aggregation. Thrombosis and Haemostasis. 108: 119-32. PMID 22628078 DOI: 10.1160/Th11-10-0749 |
0.482 |
|
| 2012 |
Tosh DK, Deflorian F, Phan K, Gao ZG, Wan TC, Gizewski E, Auchampach JA, Jacobson KA. Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions. Journal of Medicinal Chemistry. 55: 4847-60. PMID 22559880 DOI: 10.1021/Jm300396N |
0.78 |
|
| 2012 |
Tosh DK, Phan K, Gao ZG, Gakh AA, Xu F, Deflorian F, Abagyan R, Stevens RC, Jacobson KA, Katritch V. Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening. Journal of Medicinal Chemistry. 55: 4297-308. PMID 22486652 DOI: 10.1021/Jm300095S |
0.675 |
|
| 2012 |
Kozma E, Kumar TS, Federico S, Phan K, Balasubramanian R, Gao ZG, Paoletta S, Moro S, Spalluto G, Jacobson KA. Novel fluorescent antagonist as a molecular probe in A(3) adenosine receptor binding assays using flow cytometry. Biochemical Pharmacology. 83: 1552-61. PMID 22402302 DOI: 10.1016/J.Bcp.2012.02.019 |
0.853 |
|
| 2012 |
Van Poecke S, Barrett MO, Santhosh Kumar T, Sinnaeve D, Martins JC, Jacobson KA, Kendall Harden T, Van Calenbergh S. Synthesis and P2Yâ‚‚ receptor agonist activities of uridine 5'-phosphonate analogues. Bioorganic & Medicinal Chemistry. 20: 2304-15. PMID 22386981 DOI: 10.1016/J.Bmc.2012.02.012 |
0.611 |
|
| 2012 |
Jacobson KA, Balasubramanian R, Deflorian F, Gao ZG. G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions. Purinergic Signalling. 8: 419-36. PMID 22371149 DOI: 10.1007/S11302-012-9294-7 |
0.554 |
|
| 2012 |
Chen Z, Janes K, Chen C, Doyle T, Bryant L, Tosh DK, Jacobson KA, Salvemini D. Controlling murine and rat chronic pain through A3 adenosine receptor activation. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 26: 1855-65. PMID 22345405 DOI: 10.1096/Fj.11-201541 |
0.647 |
|
| 2012 |
Tosh DK, Phan K, Deflorian F, Wei Q, Yoo LS, Gao ZG, Jacobson KA. Click modification in the N6 region of A3 adenosine receptor-selective carbocyclic nucleosides for dendrimeric tethering that preserves pharmacophore recognition. Bioconjugate Chemistry. 23: 232-47. PMID 22175234 DOI: 10.1021/Bc200526C |
0.539 |
|
| 2012 |
Chanyshev B, Shainberg A, Isak A, Litinsky A, Chepurko Y, Tosh DK, Phan K, Gao ZG, Hochhauser E, Jacobson KA. Anti-ischemic effects of multivalent dendrimeric A₃ adenosine receptor agonists in cultured cardiomyocytes and in the isolated rat heart. Pharmacological Research : the Official Journal of the Italian Pharmacological Society. 65: 338-46. PMID 22154845 DOI: 10.1016/J.Phrs.2011.11.013 |
0.469 |
|
| 2012 |
Hou X, Majik MS, Kim K, Pyee Y, Lee Y, Alexander V, Chung HJ, Lee HW, Chandra G, Lee JH, Park SG, Choi WJ, Kim HO, Phan K, Gao ZG, ... Jacobson KA, et al. Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A₂A and A₃ adenosine receptor ligands. Journal of Medicinal Chemistry. 55: 342-56. PMID 22142423 DOI: 10.1021/Jm201229J |
0.657 |
|
| 2012 |
Deflorian F, Kumar TS, Phan K, Gao ZG, Xu F, Wu H, Katritch V, Stevens RC, Jacobson KA. Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound Aâ‚‚A adenosine receptor. Journal of Medicinal Chemistry. 55: 538-52. PMID 22104008 DOI: 10.1021/Jm201461Q |
0.703 |
|
| 2012 |
Fishman P, Bar-Yehuda S, Liang BT, Jacobson KA. Pharmacological and therapeutic effects of A3 adenosine receptor agonists. Drug Discovery Today. 17: 359-66. PMID 22033198 DOI: 10.1016/J.Drudis.2011.10.007 |
0.715 |
|
| 2012 |
Du L, Gao ZG, Nithipatikom K, Ijzerman AP, Veldhoven JP, Jacobson KA, Gross GJ, Auchampach JA. Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor. The Journal of Pharmacology and Experimental Therapeutics. 340: 210-7. PMID 22011434 DOI: 10.1124/Jpet.111.187559 |
0.744 |
|
| 2012 |
Kaszas K, Keller JM, Coddou C, Mishra SK, Hoon MA, Stojilkovic S, Jacobson KA, Iadarola MJ. Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH. The Journal of Pharmacology and Experimental Therapeutics. 340: 152-60. PMID 22005042 DOI: 10.1124/Jpet.111.183053 |
0.391 |
|
| 2012 |
Ji XD, Stiles GL, Jacobson KA. [(3)H]XAC (xanthine amine congener) is a radioligand for A(2)-adenosine receptors in rabbit striatum. Neurochemistry International. 18: 207-13. PMID 20504695 DOI: 10.1016/0197-0186(91)90187-I |
0.786 |
|
| 2011 |
Lee HW, Choi WJ, Jacobson KA, Jeong LS. Synthesis and Binding Affinity of Homologated Adenosine Analogues as A3 Adenosine Receptor Ligands. Bulletin of the Korean Chemical Society. 32: 1620-1624. PMID 26120223 DOI: 10.5012/Bkcs.2011.32.5.1620 |
0.703 |
|
| 2011 |
Gao ZG, Jacobson KA. Emerging adenosine receptor agonists: an update. Expert Opinion On Emerging Drugs. 16: 597-602. PMID 22148938 DOI: 10.1517/14728214.2011.644786 |
0.515 |
|
| 2011 |
Wan TC, Tosh DK, Du L, Gizewski ET, Jacobson KA, Auchampach JA. Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts. Bmc Pharmacology. 11: 11. PMID 22039965 DOI: 10.1186/1471-2210-11-11 |
0.731 |
|
| 2011 |
Choi MJ, Chandra G, Lee HW, Hou X, Choi WJ, Phan K, Jacobson KA, Jeong LS. Regio- and stereoselective synthesis of truncated 3'-aminocarbanucleosides and their binding affinity at the A3 adenosine receptor. Organic & Biomolecular Chemistry. 9: 6955-62. PMID 21860878 DOI: 10.1039/C1Ob05853C |
0.672 |
|
| 2011 |
Tosh DK, Phan K, Deflorian F, Wei Q, Gao ZG, Jacobson KA. Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element. Acs Medicinal Chemistry Letters. 2: 626-631. PMID 21858244 DOI: 10.1021/Ml200114Q |
0.566 |
|
| 2011 |
Bhattacharjee AK, Lang L, Jacobson O, Shinkre B, Ma Y, Niu G, Trenkle WC, Jacobson KA, Chen X, Kiesewetter DO. Striatal adenosine A(2A) receptor-mediated positron emission tomographic imaging in 6-hydroxydopamine-lesioned rats using [(18)F]-MRS5425. Nuclear Medicine and Biology. 38: 897-906. PMID 21843786 DOI: 10.1016/J.Nucmedbio.2011.01.009 |
0.408 |
|
| 2011 |
Gao ZG, Verzijl D, Zweemer A, Ye K, Göblyös A, Ijzerman AP, Jacobson KA. Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers. Biochemical Pharmacology. 82: 658-68. PMID 21718691 DOI: 10.1016/J.Bcp.2011.06.017 |
0.631 |
|
| 2011 |
Cohen S, Stemmer SM, Zozulya G, Ochaion A, Patoka R, Barer F, Bar-Yehuda S, Rath-Wolfson L, Jacobson KA, Fishman P. CF102 an A3 adenosine receptor agonist mediates anti-tumor and anti-inflammatory effects in the liver. Journal of Cellular Physiology. 226: 2438-47. PMID 21660967 DOI: 10.1002/Jcp.22593 |
0.356 |
|
| 2011 |
Wei Q, Costanzi S, Liu QZ, Gao ZG, Jacobson KA. Activation of the P2Y1 receptor induces apoptosis and inhibits proliferation of prostate cancer cells. Biochemical Pharmacology. 82: 418-25. PMID 21632028 DOI: 10.1016/J.Bcp.2011.05.013 |
0.702 |
|
| 2011 |
Jacobson KA, Gao ZG, Göblyös A, Ijzerman AP. Allosteric modulation of purine and pyrimidine receptors. Advances in Pharmacology (San Diego, Calif.). 61: 187-220. PMID 21586360 DOI: 10.1016/B978-0-12-385526-8.00007-2 |
0.69 |
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| 2011 |
Jacobson KA, Linden J. Pharmacology of purine and pyrimidine receptors. Preface. Advances in Pharmacology (San Diego, Calif.). 61: xv-xvi. PMID 21586353 DOI: 10.1016/B978-0-12-385526-8.00020-5 |
0.59 |
|
| 2011 |
Kecskés A, Tosh DK, Wei Q, Gao ZG, Jacobson KA. GPCR ligand dendrimer (GLiDe) conjugates: adenosine receptor interactions of a series of multivalent xanthine antagonists. Bioconjugate Chemistry. 22: 1115-27. PMID 21539392 DOI: 10.1021/Bc1005812 |
0.598 |
|
| 2011 |
Maruoka H, Jayasekara MP, Barrett MO, Franklin DA, de Castro S, Kim N, Costanzi S, Harden TK, Jacobson KA. Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor. Journal of Medicinal Chemistry. 54: 4018-33. PMID 21528910 DOI: 10.1021/Jm101591J |
0.827 |
|
| 2011 |
Kim SK, Riley L, Abrol R, Jacobson KA, Goddard WA. Predicted structures of agonist and antagonist bound complexes of adenosine A3 receptor. Proteins. 79: 1878-97. PMID 21488099 DOI: 10.1002/Prot.23012 |
0.684 |
|
| 2011 |
Jacobson KA, Deflorian F, Mishra S, Costanzi S. Pharmacochemistry of the platelet purinergic receptors. Purinergic Signalling. 7: 305-24. PMID 21484092 DOI: 10.1007/S11302-011-9216-0 |
0.783 |
|
| 2011 |
Deflorian F, Jacobson KA. Comparison of three GPCR structural templates for modeling of the P2Y12 nucleotide receptor. Journal of Computer-Aided Molecular Design. 25: 329-38. PMID 21461952 DOI: 10.1007/S10822-011-9423-3 |
0.572 |
|
| 2011 |
Xu F, Wu H, Katritch V, Han GW, Jacobson KA, Gao ZG, Cherezov V, Stevens RC. Structure of an agonist-bound human A2A adenosine receptor. Science (New York, N.Y.). 332: 322-7. PMID 21393508 DOI: 10.1126/Science.1202793 |
0.702 |
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| 2011 |
Fredholm BB, IJzerman AP, Jacobson KA, Linden J, Müller CE. International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. Pharmacological Reviews. 63: 1-34. PMID 21303899 DOI: 10.1124/Pr.110.003285 |
0.755 |
|
| 2011 |
Federico S, Paoletta S, Cheong SL, Pastorin G, Cacciari B, Stragliotto S, Klotz KN, Siegel J, Gao ZG, Jacobson KA, Moro S, Spalluto G. Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility. Journal of Medicinal Chemistry. 54: 877-89. PMID 21214204 DOI: 10.1021/Jm101349U |
0.781 |
|
| 2011 |
Müller CE, Jacobson KA. Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochimica Et Biophysica Acta. 1808: 1290-308. PMID 21185259 DOI: 10.1016/J.Bbamem.2010.12.017 |
0.54 |
|
| 2011 |
Kumar TS, Mishra S, Deflorian F, Yoo LS, Phan K, Kecskés M, Szabo A, Shinkre B, Gao ZG, Trenkle W, Jacobson KA. Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold. Bioorganic & Medicinal Chemistry Letters. 21: 2740-5. PMID 21185184 DOI: 10.1016/J.Bmcl.2010.11.082 |
0.56 |
|
| 2011 |
Müller CE, Jacobson KA. Xanthines as adenosine receptor antagonists. Handbook of Experimental Pharmacology. 151-99. PMID 20859796 DOI: 10.1007/978-3-642-13443-2_6 |
0.596 |
|
| 2011 |
Lee HW, Choi WJ, Jacobson KA, Jeong LS. Synthesis and binding affinity of homologated adenosine analogues as A3 adenosine receptor ligands Bulletin of the Korean Chemical Society. 32: 1620-1624. DOI: 10.5012/bkcs.2011.32.5.1620 |
0.663 |
|
| 2011 |
Poecke SV, Barrett M, Jacobson KA, Harden TK, Calenbergh SV. Synthesis of base-substituted uridine 5'-phosphonate analogues as potential P2Y2 receptor ligands Collection of Czechoslovak Chemical Communications. 12: 485-486. DOI: 10.1135/Css201112485 |
0.741 |
|
| 2010 |
Hou X, Kim HO, Alexander V, Kim K, Choi S, Park SG, Lee JH, Yoo LS, Gao ZG, Jacobson KA, Jeong LS. Discovery of New Human A(2A) Adenosine Receptor Agonists: Design, Synthesis, and Binding Mode of Truncated 2-Hexynyl-4'-thioadenosine. Acs Medicinal Chemistry Letters. 2010: 516-520. PMID 21286238 DOI: 10.1021/ml1001823 |
0.608 |
|
| 2010 |
Jacobson KA. GPCR ligand-dendrimer (GLiDe) conjugates: future smart drugs? Trends in Pharmacological Sciences. 31: 575-9. PMID 20961625 DOI: 10.1016/J.Tips.2010.09.002 |
0.5 |
|
| 2010 |
Ding Y, Gao ZG, Jacobson KA, Suffredini AF. Dexamethasone enhances ATP-induced inflammatory responses in endothelial cells. The Journal of Pharmacology and Experimental Therapeutics. 335: 693-702. PMID 20826566 DOI: 10.1124/Jpet.110.171975 |
0.337 |
|
| 2010 |
Lee HW, Kim HO, Choi WJ, Choi S, Lee JH, Park SG, Yoo L, Jacobson KA, Jeong LS. Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptors. Bioorganic & Medicinal Chemistry. 18: 7015-21. PMID 20826090 DOI: 10.1016/J.Bmc.2010.08.018 |
0.721 |
|
| 2010 |
Gao ZG, Ding Y, Jacobson KA. P2Y(13) receptor is responsible for ADP-mediated degranulation in RBL-2H3 rat mast cells. Pharmacological Research : the Official Journal of the Italian Pharmacological Society. 62: 500-5. PMID 20813187 DOI: 10.1016/J.Phrs.2010.08.003 |
0.57 |
|
| 2010 |
Shinkre BA, Kumar TS, Gao ZG, Deflorian F, Jacobson KA, Trenkle WC. Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. Bioorganic & Medicinal Chemistry Letters. 20: 5690-4. PMID 20801028 DOI: 10.1016/J.Bmcl.2010.08.021 |
0.507 |
|
| 2010 |
Hu H, Lu W, Zhang M, Zhang X, Argall AJ, Patel S, Lee GE, Kim YC, Jacobson KA, Laties AM, Mitchell CH. Stimulation of the P2X7 receptor kills rat retinal ganglion cells in vivo. Experimental Eye Research. 91: 425-32. PMID 20599962 DOI: 10.1016/J.Exer.2010.06.017 |
0.615 |
|
| 2010 |
Ohlmann P, de Castro S, Brown GG, Gachet C, Jacobson KA, Harden TK. Quantification of recombinant and platelet P2Y(1) receptors utilizing a [(125)I]-labeled high-affinity antagonist 2-iodo-N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate ([(125)I]MRS2500). Pharmacological Research : the Official Journal of the Italian Pharmacological Society. 62: 344-51. PMID 20594939 DOI: 10.1016/J.Phrs.2010.05.007 |
0.704 |
|
| 2010 |
Jacobson KA, Boeynaems JM. P2Y nucleotide receptors: promise of therapeutic applications. Drug Discovery Today. 15: 570-8. PMID 20594935 DOI: 10.1016/J.Drudis.2010.05.011 |
0.533 |
|
| 2010 |
de Castro S, Maruoka H, Hong K, Kilbey SM, Costanzi S, Hechler B, Brown GG, Gachet C, Harden TK, Jacobson KA. Functionalized congeners of P2Y1 receptor antagonists: 2-alkynyl (N)-methanocarba 2'-deoxyadenosine 3',5'-bisphosphate analogues and conjugation to a polyamidoamine (PAMAM) dendrimer carrier. Bioconjugate Chemistry. 21: 1190-205. PMID 20565071 DOI: 10.1021/Bc900569U |
0.819 |
|
| 2010 |
Das A, Sanjayan GJ, Kecskés M, Yoo L, Gao ZG, Jacobson KA. Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2A adenosine receptor agonists. Journal of Nanobiotechnology. 8: 11. PMID 20478037 DOI: 10.1186/1477-3155-8-11 |
0.502 |
|
| 2010 |
Maruoka H, Barrett MO, Ko H, Tosh DK, Melman A, Burianek LE, Balasubramanian R, Berk B, Costanzi S, Harden TK, Jacobson KA. Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications. Journal of Medicinal Chemistry. 53: 4488-501. PMID 20446735 DOI: 10.1021/Jm100287T |
0.881 |
|
| 2010 |
Kecskés M, Kumar TS, Yoo L, Gao ZG, Jacobson KA. Novel Alexa Fluor-488 labeled antagonist of the A(2A) adenosine receptor: Application to a fluorescence polarization-based receptor binding assay. Biochemical Pharmacology. 80: 506-11. PMID 20438717 DOI: 10.1016/J.Bcp.2010.04.027 |
0.53 |
|
| 2010 |
Carlsson J, Yoo L, Gao ZG, Irwin JJ, Shoichet BK, Jacobson KA. Structure-based discovery of A2A adenosine receptor ligands. Journal of Medicinal Chemistry. 53: 3748-55. PMID 20405927 DOI: 10.1021/Jm100240H |
0.745 |
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| 2010 |
Keene AM, Balasubramanian R, Lloyd J, Shainberg A, Jacobson KA. Multivalent dendrimeric and monomeric adenosine agonists attenuate cell death in HL-1 mouse cardiomyocytes expressing the A(3) receptor. Biochemical Pharmacology. 80: 188-96. PMID 20346920 DOI: 10.1016/J.Bcp.2010.03.020 |
0.529 |
|
| 2010 |
Pastorin G, Federico S, Paoletta S, Corradino M, Cateni F, Cacciari B, Klotz KN, Gao ZG, Jacobson KA, Spalluto G, Moro S. Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand-receptor recognition process. Bioorganic & Medicinal Chemistry. 18: 2524-36. PMID 20304654 DOI: 10.1016/J.Bmc.2010.02.039 |
0.793 |
|
| 2010 |
Zhou SY, Mamdani M, Qanud K, Shen JB, Pappano AJ, Kumar TS, Jacobson KA, Hintze T, Recchia FA, Liang BT. Treatment of heart failure by a methanocarba derivative of adenosine monophosphate: implication for a role of cardiac purinergic P2X receptors. The Journal of Pharmacology and Experimental Therapeutics. 333: 920-8. PMID 20200116 DOI: 10.1124/Jpet.109.164376 |
0.647 |
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| 2010 |
Kumar TS, Zhou SY, Joshi BV, Balasubramanian R, Yang T, Liang BT, Jacobson KA. Structure-activity relationship of (N)-Methanocarba phosphonate analogues of 5'-AMP as cardioprotective agents acting through a cardiac P2X receptor. Journal of Medicinal Chemistry. 53: 2562-76. PMID 20192270 DOI: 10.1021/Jm9018542 |
0.684 |
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| 2010 |
Tosh DK, Yoo LS, Chinn M, Hong K, Kilbey SM, Barrett MO, Fricks IP, Harden TK, Gao ZG, Jacobson KA. Polyamidoamine (PAMAM) dendrimer conjugates of "clickable" agonists of the A3 adenosine receptor and coactivation of the P2Y14 receptor by a tethered nucleotide. Bioconjugate Chemistry. 21: 372-84. PMID 20121074 DOI: 10.1021/Bc900473V |
0.735 |
|
| 2010 |
Balasubramanian R, Ruiz de Azua I, Wess J, Jacobson KA. Activation of distinct P2Y receptor subtypes stimulates insulin secretion in MIN6 mouse pancreatic beta cells. Biochemical Pharmacology. 79: 1317-26. PMID 20067775 DOI: 10.1016/J.Bcp.2009.12.026 |
0.481 |
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| 2010 |
Tosh DK, Chinn M, Yoo LS, Kang DW, Luecke H, Gao ZG, Jacobson KA. 2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists. Bioorganic & Medicinal Chemistry. 18: 508-17. PMID 20036562 DOI: 10.1016/J.Bmc.2009.12.018 |
0.589 |
|
| 2010 |
Auchampach JA, Gizewski ET, Wan TC, de Castro S, Brown GG, Jacobson KA. Synthesis and pharmacological characterization of [(125)I]MRS5127, a high affinity, selective agonist radioligand for the A3 adenosine receptor. Biochemical Pharmacology. 79: 967-73. PMID 19917269 DOI: 10.1016/J.Bcp.2009.11.009 |
0.762 |
|
| 2010 |
Das A, Ko H, Burianek LE, Barrett MO, Harden TK, Jacobson KA. Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups. Journal of Medicinal Chemistry. 53: 471-80. PMID 19902968 DOI: 10.1021/Jm901432G |
0.813 |
|
| 2010 |
Gao ZG, Ding Y, Jacobson KA. UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation. Biochemical Pharmacology. 79: 873-9. PMID 19896471 DOI: 10.1016/J.Bcp.2009.10.024 |
0.573 |
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| 2010 |
Wang Z, Do CW, Avila MY, Peterson-Yantorno K, Stone RA, Gao ZG, Joshi B, Besada P, Jeong LS, Jacobson KA, Civan MM. Nucleoside-derived antagonists to A3 adenosine receptors lower mouse intraocular pressure and act across species. Experimental Eye Research. 90: 146-54. PMID 19878673 DOI: 10.1016/J.Exer.2009.10.001 |
0.849 |
|
| 2010 |
Zhang M, Hu H, Zhang X, Lu W, Lim J, Eysteinsson T, Jacobson KA, Laties AM, Mitchell CH. The A3 adenosine receptor attenuates the calcium rise triggered by NMDA receptors in retinal ganglion cells. Neurochemistry International. 56: 35-41. PMID 19723551 DOI: 10.1016/J.Neuint.2009.08.011 |
0.535 |
|
| 2010 |
Kaszas K, Keller J, Alvarez CC, Jacobson K, Iadarola M. Allosteric modulation of the vanilloid receptor The Journal of Pain. 11: S24. DOI: 10.1016/J.Jpain.2010.01.104 |
0.533 |
|
| 2010 |
Moro S, Morizzo E, Jacobson KA. Molecular modeling and reengineering of A3 adenosine receptors A3 Adenosine Receptors From Cell Biology to Pharmacology and Therapeutics. 149-161. DOI: 10.1007/978-90-481-3144-0_8 |
0.44 |
|
| 2010 |
Jacobson KA, Gao ZG, Tosh DK, Sanjayan GJ, De Castro S. A3 adenosine receptor agonists: History and future perspectives A3 Adenosine Receptors From Cell Biology to Pharmacology and Therapeutics. 93-120. DOI: 10.1007/978-90-481-3144-0_6 |
0.484 |
|
| 2010 |
Liang BT, Urso M, Zambraski E, Jacobson KA. Adenosine A3 receptors in muscle protection A3 Adenosine Receptors From Cell Biology to Pharmacology and Therapeutics. 257-280. DOI: 10.1007/978-90-481-3144-0_13 |
0.376 |
|
| 2010 |
Lee K, Ravi G, Ji X, Marquez VE, Jacobson KA. ChemInform Abstract: Ring-Constrained (N)-Methanocarba Nucleosides as Adenosine Receptor Agonists: Independent 5′-Uronamide and 2′-Deoxy Modifications. Cheminform. 32: no-no. DOI: 10.1002/CHIN.200137209 |
0.463 |
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| 2010 |
Kim Y, Gallo-Rodriguez C, Jang S, Nandanan E, Adams M, Harden TK, Boyer JL, Jacobson KA. ChemInform Abstract: Acyclic Analogues of Deoxyadenosine 3′,5′-Bisphosphates as P2Y1 Receptor Antagonists. Cheminform. 31: no-no. DOI: 10.1002/CHIN.200023160 |
0.478 |
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| 2010 |
DE ZWART M, LINK R, VON FRIJTAG DRABBE KUENZEL JK, CRISTALLI G, JACOBSON KA, TOWNSEND-NICHOLSON A, IJZERMAN AP. ChemInform Abstract: A Functional Screening of Adenosine Analogues at the Adenosine A2B Receptor: A Search for Potent Agonists. Cheminform. 29: no-no. DOI: 10.1002/chin.199837252 |
0.622 |
|
| 2010 |
BRIDSON PK, LIN X, MELMAN N, JI X, JACOBSON KA. ChemInform Abstract: Synthesis and Adenosine Receptor Affinity of 7-β-D-Ribofuranosylxanthine. Cheminform. 29: no-no. DOI: 10.1002/CHIN.199829289 |
0.359 |
|
| 2010 |
HA SB, MELMAN N, JACOBSON KA, NAIR V. ChemInform Abstract: New Base-Altered Adenosine Analogues: Synthesis and Affinity at Adenosine A1 and A2A Receptors. Cheminform. 29: no-no. DOI: 10.1002/CHIN.199817238 |
0.478 |
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| 2010 |
JIANG J, VAN RHEE AM, MELMAN N, JI X, JACOBSON KA. ChemInform Abstract: 6-Phenyl-1,4-dihydropyridine Derivatives as Potent and Selective A3 Adenosine Receptor Antagonists. Cheminform. 28: no-no. DOI: 10.1002/CHIN.199708139 |
0.508 |
|
| 2010 |
KARTON Y, JIANG J, JI X, MELMAN N, OLAH ME, STILES GL, JACOBSON KA. ChemInform Abstract: Synthesis and Biological Activities of Flavonoid Derivatives as A3 Adenosine Receptor Antagonists. Cheminform. 27: no-no. DOI: 10.1002/CHIN.199638149 |
0.744 |
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| 2010 |
BARALDI PG, CACCIARI B, SPALLUTO G, JI X, OLAH ME, STILES G, DIONISOTTI S, ZOCCHI C, ONGINI E, JACOBSON KA. ChemInform Abstract: Novel N6-(Substituted-phenylcarbamoyl)adenosine-5′-uronamides as Potent Agonists for A3 Adenosine Receptors. Cheminform. 27: no-no. DOI: 10.1002/CHIN.199621237 |
0.821 |
|
| 2009 |
Fredholm BB, Jacobson KA. Adenosine Receptors: The Contributions by John W. Daly. Heterocycles. 79: 73-83. PMID 26113768 DOI: 10.3987/Com-08-S(D)Memoire-2 |
0.67 |
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| 2009 |
Costanzi S, Siegel J, Tikhonova IG, Jacobson KA. Rhodopsin and the others: a historical perspective on structural studies of G protein-coupled receptors. Current Pharmaceutical Design. 15: 3994-4002. PMID 20028316 DOI: 10.2174/138161209789824795 |
0.728 |
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| 2009 |
Choi WJ, Lee HW, Kim HO, Chinn M, Gao ZG, Patel A, Jacobson KA, Moon HR, Jung YH, Jeong LS. Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists. Bioorganic & Medicinal Chemistry. 17: 8003-11. PMID 19879151 DOI: 10.1016/J.Bmc.2009.10.011 |
0.689 |
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| 2009 |
Kim Y, Hechler B, Gao ZG, Gachet C, Jacobson KA. PEGylated dendritic unimolecular micelles as versatile carriers for ligands of G protein-coupled receptors. Bioconjugate Chemistry. 20: 1888-98. PMID 19785401 DOI: 10.1021/Bc9001689 |
0.823 |
|
| 2009 |
Carter RL, Fricks IP, Barrett MO, Burianek LE, Zhou Y, Ko H, Das A, Jacobson KA, Lazarowski ER, Harden TK. Quantification of Gi-mediated inhibition of adenylyl cyclase activity reveals that UDP is a potent agonist of the human P2Y14 receptor. Molecular Pharmacology. 76: 1341-8. PMID 19759354 DOI: 10.1124/Mol.109.058578 |
0.835 |
|
| 2009 |
Jacobson KA, Klutz AM, Tosh DK, Ivanov AA, Preti D, Baraldi PG. Medicinal chemistry of the A3 adenosine receptor: agonists, antagonists, and receptor engineering. Handbook of Experimental Pharmacology. 123-59. PMID 19639281 DOI: 10.1007/978-3-540-89615-9_5 |
0.772 |
|
| 2009 |
Jacobson KA. Introduction to adenosine receptors as therapeutic targets. Handbook of Experimental Pharmacology. 1-24. PMID 19639277 DOI: 10.1007/978-3-540-89615-9_1 |
0.547 |
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| 2009 |
Das A, Zhou Y, Ivanov AA, Carter RL, Harden TK, Jacobson KA. Enhanced potency of nucleotide-dendrimer conjugates as agonists of the P2Y14 receptor: multivalent effect in G protein-coupled receptor recognition. Bioconjugate Chemistry. 20: 1650-9. PMID 19572637 DOI: 10.1021/Bc900206G |
0.825 |
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| 2009 |
Ko H, Das A, Carter RL, Fricks IP, Zhou Y, Ivanov AA, Melman A, Joshi BV, Kovác P, Hajduch J, Kirk KL, Harden TK, Jacobson KA. Molecular recognition in the P2Y(14) receptor: Probing the structurally permissive terminal sugar moiety of uridine-5'-diphosphoglucose. Bioorganic & Medicinal Chemistry. 17: 5298-311. PMID 19502066 DOI: 10.1016/J.Bmc.2009.05.024 |
0.857 |
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| 2009 |
Tosh DK, Chinn M, Ivanov AA, Klutz AM, Gao ZG, Jacobson KA. Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system. Journal of Medicinal Chemistry. 52: 7580-92. PMID 19499950 DOI: 10.1021/Jm900426G |
0.763 |
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| 2009 |
Cosyn L, Van Calenbergh S, Joshi BV, Ko H, Carter RL, Kendall Harden T, Jacobson KA. Synthesis and P2Y receptor activity of nucleoside 5'-phosphonate derivatives. Bioorganic & Medicinal Chemistry Letters. 19: 3002-5. PMID 19419868 DOI: 10.1016/J.Bmcl.2009.04.027 |
0.815 |
|
| 2009 |
Jacobson KA. Functionalized congener approach to the design of ligands for G protein-coupled receptors (GPCRs). Bioconjugate Chemistry. 20: 1816-35. PMID 19405524 DOI: 10.1021/Bc9000596 |
0.573 |
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| 2009 |
Ivanov AA, Barak D, Jacobson KA. Evaluation of homology modeling of G-protein-coupled receptors in light of the A(2A) adenosine receptor crystallographic structure. Journal of Medicinal Chemistry. 52: 3284-92. PMID 19402631 DOI: 10.1021/Jm801533X |
0.764 |
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| 2009 |
Pal S, Choi WJ, Choe SA, Heller CL, Gao ZG, Chinn M, Jacobson KA, Hou X, Lee SK, Kim HO, Jeong LS. Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists. Bioorganic & Medicinal Chemistry. 17: 3733-8. PMID 19375920 DOI: 10.1016/J.Bmc.2009.03.034 |
0.693 |
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| 2009 |
Kim Y, de Castro S, Gao ZG, Ijzerman AP, Jacobson KA. Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor. Journal of Medicinal Chemistry. 52: 2098-108. PMID 19284749 DOI: 10.1021/Jm801659W |
0.834 |
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| 2009 |
Kiesewetter DO, Lang L, Ma Y, Bhattacharjee AK, Gao ZG, Joshi BV, Melman A, de Castro S, Jacobson KA. Synthesis and characterization of [76Br]-labeled high-affinity A3 adenosine receptor ligands for positron emission tomography. Nuclear Medicine and Biology. 36: 3-10. PMID 19181263 DOI: 10.1016/J.Nucmedbio.2008.10.003 |
0.501 |
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| 2009 |
Jacobson KA, Zablocki J, Bhagwat S. Preface: special issue on medicinal chemistry of purines. Purinergic Signalling. 5: 1. PMID 18604595 DOI: 10.1007/S11302-008-9120-4 |
0.446 |
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| 2009 |
Jacobson KA, Ivanov AA, de Castro S, Harden TK, Ko H. Development of selective agonists and antagonists of P2Y receptors. Purinergic Signalling. 5: 75-89. PMID 18600475 DOI: 10.1007/S11302-008-9106-2 |
0.885 |
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| 2009 |
Kim Y, Klutz AM, Hechler B, Gao ZG, Gachet C, Jacobson KA. Application of the functionalized congener approach to dendrimer-based signaling agents acting through A(2A) adenosine receptors. Purinergic Signalling. 5: 39-50. PMID 18600474 DOI: 10.1007/S11302-008-9113-3 |
0.815 |
|
| 2009 |
Gao ZG, Teng B, Wu H, Joshi BV, Griffiths GL, Jacobson KA. Synthesis and pharmacological characterization of [(125)I]MRS1898, a high-affinity, selective radioligand for the rat A(3) adenosine receptor. Purinergic Signalling. 5: 31-7. PMID 18528782 DOI: 10.1007/S11302-008-9107-1 |
0.522 |
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| 2009 |
Costanzi S, Tikhonova IG, Harden TK, Jacobson KA. Ligand and structure-based methodologies for the prediction of the activity of G protein-coupled receptor ligands. Journal of Computer-Aided Molecular Design. 23: 747-54. PMID 18483766 DOI: 10.1007/S10822-008-9218-3 |
0.743 |
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| 2009 |
Fredholm BB, Jacobson KA. Adenosine receptors: The contributions by John W. Daly Heterocycles. 79: 73-83. DOI: 10.3987/COM-08-S(D)Memoire-2 |
0.64 |
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| 2009 |
Jacobson KA, Kirk KL. John W. Daly - An appreciation Heterocycles. 79: 61-71. DOI: 10.3987/Com-08-S(D)Memoire-1 |
0.437 |
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| 2009 |
Tosh DK, Jacobson KA, Jeong LS. Nucleoside-based adenosine A3 receptor antagonists as drug candidates Drugs of the Future. 34: 43-52. DOI: 10.1358/Dof.2009.034.01.1286494 |
0.678 |
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| 2009 |
Lee GE, Joshi BV, Chen W, Jeong LS, Moon HR, Jacobson KA, Kim YC. Corrigendum to "Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor" [Bioorg. Med. Chem. Lett. 18 (2008) 571-575] (DOI:10.1016/j.bmcl.2007.11.077) Bioorganic and Medicinal Chemistry Letters. 19: 556. DOI: 10.1016/J.Bmcl.2008.05.108 |
0.853 |
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| 2008 |
Gao ZG, Ye K, Göblyös A, Ijzerman AP, Jacobson KA. Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000. Bmc Pharmacology. 8: 20. PMID 19077268 DOI: 10.1186/1471-2210-8-20 |
0.699 |
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| 2008 |
Klutz AM, Gao ZG, Lloyd J, Shainberg A, Jacobson KA. Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates. Journal of Nanobiotechnology. 6: 12. PMID 18947419 DOI: 10.1186/1477-3155-6-12 |
0.598 |
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| 2008 |
Wess J, Han SJ, Kim SK, Jacobson KA, Li JH. Conformational changes involved in G-protein-coupled-receptor activation. Trends in Pharmacological Sciences. 29: 616-25. PMID 18838178 DOI: 10.1016/J.Tips.2008.08.006 |
0.665 |
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| 2008 |
Melman A, Zhong M, Marquez VE, Jacobson KA. Synthesis of enantiomerically pure (S)-methanocarbaribo uracil nucleoside derivatives for use as antiviral agents and P2Y receptor ligands. The Journal of Organic Chemistry. 73: 8085-8. PMID 18811198 DOI: 10.1021/Jo801224J |
0.318 |
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| 2008 |
Jeong LS, Pal S, Choe SA, Choi WJ, Jacobson KA, Gao ZG, Klutz AM, Hou X, Kim HO, Lee HW, Lee SK, Tosh DK, Moon HR. Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists. Journal of Medicinal Chemistry. 51: 6609-13. PMID 18811138 DOI: 10.1021/Jm8008647 |
0.648 |
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| 2008 |
Roh EJ, Keller JM, Olah Z, Iadarola MJ, Jacobson KA. Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1). Bioorganic & Medicinal Chemistry. 16: 9349-58. PMID 18809334 DOI: 10.1016/J.Bmc.2008.08.048 |
0.641 |
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| 2008 |
Mamedova LK, Wang R, Besada P, Liang BT, Jacobson KA. Attenuation of apoptosis in vitro and ischemia/reperfusion injury in vivo in mouse skeletal muscle by P2Y6 receptor activation. Pharmacological Research : the Official Journal of the Italian Pharmacological Society. 58: 232-9. PMID 18805489 DOI: 10.1016/J.Phrs.2008.08.004 |
0.835 |
|
| 2008 |
Ohtani M, Suzuki J, Jacobson KA, Oka T. Evidence for the possible involvement of the P2Y(6) receptor in Ca (2+) mobilization and insulin secretion in mouse pancreatic islets. Purinergic Signalling. 4: 365-75. PMID 18784987 DOI: 10.1007/S11302-008-9122-2 |
0.416 |
|
| 2008 |
Choi WJ, Lee HW, Hou X, Kim HO, Jacobson KA, Jeong LS. Synthesis of 2-chloro-N6-substituted-4'-thioadenosine-5'-N, N-dialkyluronamides as potent and selective A3 adenosine receptor antagonists. Nucleic Acids Symposium Series (2004). 645-6. PMID 18776545 DOI: 10.1093/nass/nrn326 |
0.697 |
|
| 2008 |
Hou X, Pal S, Choi WJ, Kim HO, Tipnis A, Jacobson KA, Jeong LS. Design and synthesis of truncated 4'-thioadenosine derivatives as potent and selective A3 adenosine receptor antagonists. Nucleic Acids Symposium Series (2004). 641-2. PMID 18776543 DOI: 10.1093/nass/nrn324 |
0.675 |
|
| 2008 |
Melman A, Wang B, Joshi BV, Gao ZG, Castro Sd, Heller CL, Kim SK, Jeong LS, Jacobson KA. Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system. Bioorganic & Medicinal Chemistry. 16: 8546-56. PMID 18752961 DOI: 10.1016/J.Bmc.2008.08.007 |
0.867 |
|
| 2008 |
Houston D, Costanzi S, Jacobson KA, Harden TK. Development of selective high affinity antagonists, agonists, and radioligands for the P2Y1 receptor. Combinatorial Chemistry & High Throughput Screening. 11: 410-9. PMID 18673269 DOI: 10.2174/138620708784911474 |
0.832 |
|
| 2008 |
Sonin D, Zhou SY, Cronin C, Sonina T, Wu J, Jacobson KA, Pappano A, Liang BT. Role of P2X purinergic receptors in the rescue of ischemic heart failure. American Journal of Physiology. Heart and Circulatory Physiology. 295: H1191-H1197. PMID 18641271 DOI: 10.1152/Ajpheart.00577.2008 |
0.639 |
|
| 2008 |
Ivanov AA, Jacobson KA. Molecular modeling of a PAMAM-CGS21680 dendrimer bound to an A2A adenosine receptor homodimer. Bioorganic & Medicinal Chemistry Letters. 18: 4312-5. PMID 18639453 DOI: 10.1016/J.Bmcl.2008.06.087 |
0.786 |
|
| 2008 |
Kim Y, Klutz AM, Jacobson KA. Systematic investigation of polyamidoamine dendrimers surface-modified with poly(ethylene glycol) for drug delivery applications: synthesis, characterization, and evaluation of cytotoxicity. Bioconjugate Chemistry. 19: 1660-72. PMID 18610944 DOI: 10.1021/Bc700483S |
0.718 |
|
| 2008 |
Brand F, Klutz AM, Jacobson KA, Fredholm BB, Schulte G. Adenosine A(2A) receptor dynamics studied with the novel fluorescent agonist Alexa488-APEC. European Journal of Pharmacology. 590: 36-42. PMID 18603240 DOI: 10.1016/J.Ejphar.2008.05.036 |
0.703 |
|
| 2008 |
Ochaion A, Bar-Yehuda S, Cohen S, Amital H, Jacobson KA, Joshi BV, Gao ZG, Barer F, Patoka R, Del Valle L, Perez-Liz G, Fishman P. The A3 adenosine receptor agonist CF502 inhibits the PI3K, PKB/Akt and NF-kappaB signaling pathway in synoviocytes from rheumatoid arthritis patients and in adjuvant-induced arthritis rats. Biochemical Pharmacology. 76: 482-94. PMID 18602896 DOI: 10.1016/J.Bcp.2008.05.032 |
0.42 |
|
| 2008 |
Cappellacci L, Franchetti P, Petrelli R, Vita P, Jacobson KA, Maddileti S, Harden TK, Grifantini M. ATP-mimetics derived from 2 '(3 ')-C-methyladenosine as human P2Y2 agonists Purinergic Signalling. 4. PMID 18553155 DOI: 10.1007/S11302-008-9116-0 |
0.381 |
|
| 2008 |
Ko H, Carter RL, Cosyn L, Petrelli R, de Castro S, Besada P, Zhou Y, Cappellacci L, Franchetti P, Grifantini M, Van Calenbergh S, Harden TK, Jacobson KA. Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists. Bioorganic & Medicinal Chemistry. 16: 6319-32. PMID 18514530 DOI: 10.1016/J.Bmc.2008.05.013 |
0.884 |
|
| 2008 |
Gao ZG, Jacobson KA. Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways. Pharmacological Research : the Official Journal of the Italian Pharmacological Society. 57: 303-11. PMID 18424164 DOI: 10.1016/J.Phrs.2008.02.008 |
0.521 |
|
| 2008 |
Melman A, Gao ZG, Kumar D, Wan TC, Gizewski E, Auchampach JA, Jacobson KA. Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorganic & Medicinal Chemistry Letters. 18: 2813-9. PMID 18424135 DOI: 10.1016/J.Bmcl.2008.04.001 |
0.752 |
|
| 2008 |
Chun MW, Choi SW, Kang TK, Choi WJ, Kim HO, Gao ZG, Jacobson KA, Jeong LS. Synthesis of 3'-acetamidoadenosine derivatives as potential A3 adenosine receptor agonists. Nucleosides, Nucleotides & Nucleic Acids. 27: 408-20. PMID 18404574 DOI: 10.1080/15257770801944436 |
0.681 |
|
| 2008 |
Ivanov AA, Wang B, Klutz AM, Chen VL, Gao ZG, Jacobson KA. Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists. Journal of Medicinal Chemistry. 51: 2088-99. PMID 18321038 DOI: 10.1021/Jm701442D |
0.74 |
|
| 2008 |
Joshi BV, Melman A, Mackman RL, Jacobson KA. Synthesis of ethyl (1S,2R,3S,4S,5S)-2,3-O-(isopropylidene)-4-hydroxy-bicyclo[3.1.0]hexane-carboxylate from L-ribose: a versatile chiral synthon for preparation of adenosine and P2 receptor ligands. Nucleosides, Nucleotides & Nucleic Acids. 27: 279-91. PMID 18260011 DOI: 10.1080/15257770701845253 |
0.409 |
|
| 2008 |
Jeong LS, Lee HW, Kim HO, Tosh DK, Pal S, Choi WJ, Gao ZG, Patel AR, Williams W, Jacobson KA, Kim HD. Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 18: 1612-6. PMID 18255292 DOI: 10.1016/J.Bmcl.2008.01.070 |
0.619 |
|
| 2008 |
Fricks IP, Maddileti S, Carter RL, Lazarowski ER, Nicholas RA, Jacobson KA, Harden TK. UDP is a competitive antagonist at the human P2Y14 receptor. The Journal of Pharmacology and Experimental Therapeutics. 325: 588-94. PMID 18252808 DOI: 10.1124/Jpet.108.136309 |
0.648 |
|
| 2008 |
Li JH, Hamdan FF, Kim SK, Jacobson KA, Zhang X, Han SJ, Wess J. Ligand-specific changes in M3 muscarinic acetylcholine receptor structure detected by a disulfide scanning strategy. Biochemistry. 47: 2776-88. PMID 18247581 DOI: 10.1021/Bi7019113 |
0.695 |
|
| 2008 |
Gao ZG, Hechler B, Besada P, Gachet C, Jacobson KA. Caged agonist of P2Y1 and P2Y12 receptors for light-directed facilitation of platelet aggregation. Biochemical Pharmacology. 75: 1341-7. PMID 18199424 DOI: 10.1016/J.Bcp.2007.10.037 |
0.778 |
|
| 2008 |
Kim Y, Hechler B, Klutz AM, Gachet C, Jacobson KA. Toward multivalent signaling across G protein-coupled receptors from poly(amidoamine) dendrimers. Bioconjugate Chemistry. 19: 406-11. PMID 18176997 DOI: 10.1021/Bc700327U |
0.793 |
|
| 2008 |
Lee GE, Joshi BV, Chen W, Jeong LS, Moon HR, Jacobson KA, Kim YC. Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor. Bioorganic & Medicinal Chemistry Letters. 18: 571-5. PMID 18078749 DOI: 10.1016/J.Bmcl.2007.11.077 |
0.862 |
|
| 2008 |
Lee HW, Shin DH, Jung JY, Kim HO, Chun MW, Melman N, Gao Z-, Jacobson K, Jeong LS. Erratum Nucleosides, Nucleotides and Nucleic Acids. 27: 101-101. DOI: 10.1080/15257770701761864 |
0.361 |
|
| 2008 |
Kim AY, Kim HO, Kim MJ, Chun MW, Lee KM, Jacobson KA, Jeong LS. ChemInform Abstract: Synthesis of 3′-(Ureido)adenosine Derivatives and Their High Binding Affinity at the Mutant A3 Adenosine Receptor Cheminform. 39. DOI: 10.1002/CHIN.200829254 |
0.649 |
|
| 2008 |
Jeong LS, Gunaga P, Kim HO, Tosh DK, Lee HW, Choe SA, Moon HR, Gao Z, Jacobson KA, Chun MW. ChemInform Abstract: Stereoselective Synthesis of 1′-Functionalized-4′-thionucleosides Cheminform. 39. DOI: 10.1002/CHIN.200811260 |
0.397 |
|
| 2008 |
Jeong LS, Choe SA, Kim AY, Kim HO, Gao Z, Jacobson KA, Chun MW, Moon HR. ChemInform Abstract: Synthesis of N6-Substituted 3′-Ureidoadenosine Derivatives as Highly Potent Agonists at the Mutant A3Adenosine Receptor Cheminform. 39. DOI: 10.1002/CHIN.200811239 |
0.633 |
|
| 2008 |
Jacobson KA, Joshi BV, Wang B, Klutz A, Kim Y, Ivanov AA, Melman A, Gao ZG. Modified Nucleosides as Selective Modulators of Adenosine Receptors for Therapeutic Use Modified Nucleosides: in Biochemistry, Biotechnology and Medicine. 433-449. DOI: 10.1002/9783527623112.ch17 |
0.734 |
|
| 2007 |
Jeong LS, Choe SA, Kim AY, Kim HO, Gao ZG, Jacobson KA, Chun MW, Moon HR. Synthesis of N6-substituted 3'-ureidoadenosine derivatives as highly potent agonists at the mutant A3 adenosine receptor. Nucleosides, Nucleotides & Nucleic Acids. 26: 717-9. PMID 18066887 DOI: 10.1080/15257770701493161 |
0.694 |
|
| 2007 |
Jeong LS, Lee HW, Kim HO, Jung JY, Gunaga P, Lee SK, Lee EJ, Chun MW, Gao ZG, Jacobson KA, Moon HR. Design, synthesis, and anti-tumor activity of 4'-thionucleosides as potent and selective agonists at the human A3 adenosine receptor. Nucleosides, Nucleotides & Nucleic Acids. 26: 1565-8. PMID 18066827 DOI: 10.1080/15257770701547107 |
0.69 |
|
| 2007 |
Jeong LS, Gunaga P, Kim HO, Tosh DK, Lee HW, Choe SA, Moon HR, Gao ZG, Jacobson KA, Chun MW. Stereoselective synthesis of 1'-functionalized-4'-thionucleosides. Nucleosides, Nucleotides & Nucleic Acids. 26: 1011-4. PMID 18058527 DOI: 10.1080/15257770701508588 |
0.488 |
|
| 2007 |
Zheng J, Wang R, Zambraski E, Wu D, Jacobson KA, Liang BT. Protective roles of adenosine A1, A2A, and A3 receptors in skeletal muscle ischemia and reperfusion injury. American Journal of Physiology. Heart and Circulatory Physiology. 293: H3685-91. PMID 17921328 DOI: 10.1152/Ajpheart.00819.2007 |
0.747 |
|
| 2007 |
Gao ZG, Jacobson KA. Emerging adenosine receptor agonists. Expert Opinion On Emerging Drugs. 12: 479-92. PMID 17874974 DOI: 10.1517/14728214.12.3.479 |
0.519 |
|
| 2007 |
Pugliese AM, Coppi E, Volpini R, Cristalli G, Corradetti R, Jeong LS, Jacobson KA, Pedata F. Role of adenosine A3 receptors on CA1 hippocampal neurotransmission during oxygen-glucose deprivation episodes of different duration. Biochemical Pharmacology. 74: 768-79. PMID 17626785 DOI: 10.1016/J.Bcp.2007.06.003 |
0.658 |
|
| 2007 |
Li JH, Han SJ, Hamdan FF, Kim SK, Jacobson KA, Bloodworth LM, Zhang X, Wess J. Distinct structural changes in a G protein-coupled receptor caused by different classes of agonist ligands. The Journal of Biological Chemistry. 282: 26284-93. PMID 17623649 DOI: 10.1074/Jbc.M704875200 |
0.712 |
|
| 2007 |
Costanzi S, Tikhonova IG, Ohno M, Roh EJ, Joshi BV, Colson AO, Houston D, Maddileti S, Harden TK, Jacobson KA. P2Y1 antagonists: combining receptor-based modeling and QSAR for a quantitative prediction of the biological activity based on consensus scoring. Journal of Medicinal Chemistry. 50: 3229-41. PMID 17564423 DOI: 10.1021/Jm0700971 |
0.818 |
|
| 2007 |
Jeong LS, Choe SA, Gunaga P, Kim HO, Lee HW, Lee SK, Tosh DK, Patel A, Palaniappan KK, Gao ZG, Jacobson KA, Moon HR. Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists. Journal of Medicinal Chemistry. 50: 3159-62. PMID 17555308 DOI: 10.1021/Jm070259T |
0.68 |
|
| 2007 |
Palaniappan KK, Gao ZG, Ivanov AA, Greaves R, Adachi H, Besada P, Kim HO, Kim AY, Choe SA, Jeong LS, Jacobson KA. Probing the binding site of the A1 adenosine receptor reengineered for orthogonal recognition by tailored nucleosides. Biochemistry. 46: 7437-48. PMID 17542617 DOI: 10.1021/Bi7001828 |
0.859 |
|
| 2007 |
Wang Z, Do CW, Avila MY, Stone RA, Jacobson KA, Civan MM. Barrier qualities of the mouse eye to topically applied drugs. Experimental Eye Research. 85: 105-12. PMID 17490649 DOI: 10.1016/J.Exer.2007.03.006 |
0.564 |
|
| 2007 |
Koizumi S, Shigemoto-Mogami Y, Nasu-Tada K, Shinozaki Y, Ohsawa K, Tsuda M, Joshi BV, Jacobson KA, Kohsaka S, Inoue K. UDP acting at P2Y6 receptors is a mediator of microglial phagocytosis. Nature. 446: 1091-5. PMID 17410128 DOI: 10.1038/Nature05704 |
0.472 |
|
| 2007 |
Ko H, Fricks I, Ivanov AA, Harden TK, Jacobson KA. Structure-activity relationship of uridine 5'-diphosphoglucose analogues as agonists of the human P2Y14 receptor. Journal of Medicinal Chemistry. 50: 2030-9. PMID 17407275 DOI: 10.1021/Jm061222W |
0.873 |
|
| 2007 |
Adachi H, Palaniappan KK, Ivanov AA, Bergman N, Gao ZG, Jacobson KA. Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor. Journal of Medicinal Chemistry. 50: 1810-27. PMID 17378544 DOI: 10.1021/Jm061278Q |
0.846 |
|
| 2007 |
Kimand SK, Jacobson KA. Three-dimensional quantitative structure-activity relationship of nucleosides acting at the A3 adenosine receptor: analysis of binding and relative efficacy. Journal of Chemical Information and Modeling. 47: 1225-33. PMID 17338510 DOI: 10.1021/Ci600501Z |
0.571 |
|
| 2007 |
Ivanov AA, Ko H, Cosyn L, Maddileti S, Besada P, Fricks I, Costanzi S, Harden TK, Calenbergh SV, Jacobson KA. Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate. Journal of Medicinal Chemistry. 50: 1166-76. PMID 17302398 DOI: 10.1021/Jm060903O |
0.872 |
|
| 2007 |
Olivecrona GK, Götberg M, Harnek J, Jacobson KA, Jern S, Erlinge D. The ADP receptor P2Y(1) mediates t-PA release in pigs during cardiac ischemia. Journal of Thrombosis and Thrombolysis. 24: 115-22. PMID 17294140 DOI: 10.1007/S11239-007-0010-3 |
0.41 |
|
| 2007 |
Jacobson KA, Gao ZG, Liang BT. Neoceptors: reengineering GPCRs to recognize tailored ligands. Trends in Pharmacological Sciences. 28: 111-6. PMID 17280720 DOI: 10.1016/J.Tips.2007.01.006 |
0.727 |
|
| 2007 |
Li B, Scarselli M, Knudsen CD, Kim SK, Jacobson KA, McMillin SM, Wess J. Rapid identification of functionally critical amino acids in a G protein-coupled receptor. Nature Methods. 4: 169-74. PMID 17206152 DOI: 10.1038/Nmeth990 |
0.623 |
|
| 2007 |
Ivanov AA, Fricks I, Kendall Harden T, Jacobson KA. Molecular dynamics simulation of the P2Y14 receptor. Ligand docking and identification of a putative binding site of the distal hexose moiety. Bioorganic & Medicinal Chemistry Letters. 17: 761-6. PMID 17088057 DOI: 10.1016/J.Bmcl.2006.10.081 |
0.756 |
|
| 2007 |
Shen JB, Cronin C, Sonin D, Joshi BV, Gongora Nieto M, Harrison D, Jacobson KA, Liang BT. P2X purinergic receptor-mediated ionic current in cardiac myocytes of calsequestrin model of cardiomyopathy: implications for the treatment of heart failure. American Journal of Physiology. Heart and Circulatory Physiology. 292: H1077-84. PMID 17040972 DOI: 10.1152/Ajpheart.00515.2006 |
0.642 |
|
| 2007 |
Fishman P, Jacobson KA, Ochaion A, Cohen S, Bar-Yehuda S. The Anti-Cancer Effect of A3 Adenosine Receptor Agonists: A Novel, Targeted Therapy Immunology‚ Endocrine & Metabolic Agents in Medicinal Chemistry. 7: 298-303. DOI: 10.2174/187152207781369878 |
0.492 |
|
| 2007 |
Li JH, Han S, Hamdan FF, Kim S, Jacobson KA, Bloodworth LM, Zhang X, Wess J. Identification of distinct, ligand‐specific structural changes in a G protein‐coupled receptor The Faseb Journal. 21. DOI: 10.1096/Fasebj.21.5.A425-C |
0.635 |
|
| 2007 |
Fricks IP, Maddileti S, Lazarowski ER, Nicholas RA, Jacobson KA, Harden TK. UDP is an antagonist at the hP2Y14 receptor The Faseb Journal. 21. DOI: 10.1096/Fasebj.21.5.A424-C |
0.719 |
|
| 2006 |
Besada P, Mamedova LK, Palaniappan KK, Gao ZG, Joshi BV, Jeong LS, Civan MM, Jacobson KA. NUCLEOSIDE PRODRUGS OF A ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS. Collection of Czechoslovak Chemical Communications. 71: 912-928. PMID 34815583 DOI: 10.1135/cccc20060912 |
0.849 |
|
| 2006 |
Cosyn L, Palaniappan KK, Kim SK, Duong HT, Gao ZG, Jacobson KA, Van Calenbergh S. 2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. Journal of Medicinal Chemistry. 49: 7373-83. PMID 17149867 DOI: 10.1021/Jm0608208 |
0.719 |
|
| 2006 |
Jacobson KA, Costanzi S, Kim SK, Roh E, Joshi BV, Tchilibon S, Duong HT, Gao ZG. Action of nucleosides and nucleotides at 7 transmembrane-spanning receptors. Nucleosides, Nucleotides & Nucleic Acids. 25: 1425-36. PMID 17067963 DOI: 10.1080/15257770600919027 |
0.878 |
|
| 2006 |
Ivanov AA, Costanzi S, Jacobson KA. Defining the nucleotide binding sites of P2Y receptors using rhodopsin-based homology modeling. Journal of Computer-Aided Molecular Design. 20: 417-26. PMID 17016747 DOI: 10.1007/S10822-006-9054-2 |
0.836 |
|
| 2006 |
Abbracchio MP, Burnstock G, Boeynaems JM, Barnard EA, Boyer JL, Kennedy C, Knight GE, Fumagalli M, Gachet C, Jacobson KA, Weisman GA. International Union of Pharmacology LVIII: update on the P2Y G protein-coupled nucleotide receptors: from molecular mechanisms and pathophysiology to therapy. Pharmacological Reviews. 58: 281-341. PMID 16968944 DOI: 10.1124/Pr.58.3.3 |
0.654 |
|
| 2006 |
Besada P, Shin DH, Costanzi S, Ko H, Mathé C, Gagneron J, Gosselin G, Maddileti S, Harden TK, Jacobson KA. Structure-activity relationships of uridine 5'-diphosphate analogues at the human P2Y6 receptor. Journal of Medicinal Chemistry. 49: 5532-43. PMID 16942026 DOI: 10.1021/Jm060485N |
0.868 |
|
| 2006 |
Mamedova LK, Gao ZG, Jacobson KA. Regulation of death and survival in astrocytes by ADP activating P2Y1 and P2Y12 receptors. Biochemical Pharmacology. 72: 1031-41. PMID 16934758 DOI: 10.1016/J.Bcp.2006.07.017 |
0.826 |
|
| 2006 |
Jacobson KA, Costanzi S, Joshi BV, Besada P, Shin DH, Ko H, Ivanov AA, Mamedova L. Agonists and antagonists for P2 receptors. Novartis Foundation Symposium. 276: 58-68; discussion 68. PMID 16805423 DOI: 10.1002/9780470032244.Ch6 |
0.883 |
|
| 2006 |
Kim SK, Gao ZG, Jeong LS, Jacobson KA. Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor. Journal of Molecular Graphics & Modelling. 25: 562-77. PMID 16793299 DOI: 10.1016/J.Jmgm.2006.05.004 |
0.79 |
|
| 2006 |
Kim SK, Jacobson KA. Computational prediction of homodimerization of the A3 adenosine receptor. Journal of Molecular Graphics & Modelling. 25: 549-61. PMID 16781879 DOI: 10.1016/J.Jmgm.2006.03.003 |
0.6 |
|
| 2006 |
Hu J, Jiang J, Costanzi S, Thomas C, Yang W, Feyen JH, Jacobson KA, Spiegel AM. A missense mutation in the seven-transmembrane domain of the human Ca2+ receptor converts a negative allosteric modulator into a positive allosteric modulator. The Journal of Biological Chemistry. 281: 21558-65. PMID 16735501 DOI: 10.1074/Jbc.M603682200 |
0.713 |
|
| 2006 |
Göblyös A, Gao ZG, Brussee J, Connestari R, Santiago SN, Ye K, Ijzerman AP, Jacobson KA. Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor. Journal of Medicinal Chemistry. 49: 3354-61. PMID 16722654 DOI: 10.1021/Jm060086S |
0.693 |
|
| 2006 |
Gao ZG, Duong HT, Sonina T, Kim SK, Van Rompaey P, Van Calenbergh S, Mamedova L, Kim HO, Kim MJ, Kim AY, Liang BT, Jeong LS, Jacobson KA. Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists. Journal of Medicinal Chemistry. 49: 2689-702. PMID 16640329 DOI: 10.1021/Jm050968B |
0.88 |
|
| 2006 |
Bourdon DM, Mahanty SK, Jacobson KA, Boyer JL, Harden TK. (N)-methanocarba-2MeSADP (MRS2365) is a subtype-specific agonist that induces rapid desensitization of the P2Y1 receptor of human platelets. Journal of Thrombosis and Haemostasis : Jth. 4: 861-8. PMID 16634757 DOI: 10.1111/J.1538-7836.2006.01866.X |
0.714 |
|
| 2006 |
Matot I, Weiniger CF, Zeira E, Galun E, Joshi BV, Jacobson KA. A3 adenosine receptors and mitogen-activated protein kinases in lung injury following in vivo reperfusion. Critical Care (London, England). 10: R65. PMID 16623960 DOI: 10.1186/Cc4893 |
0.463 |
|
| 2006 |
Jeong LS, Lee HW, Kim HO, Jung JY, Gao ZG, Duong HT, Rao S, Jacobson KA, Shin DH, Lee JA, Gunaga P, Lee SK, Jin DZ, Chun MW, Moon HR. Design, synthesis, and biological activity of N6-substituted-4'-thioadenosines at the human A3 adenosine receptor. Bioorganic & Medicinal Chemistry. 14: 4718-30. PMID 16603368 DOI: 10.1016/J.Bmc.2006.03.030 |
0.709 |
|
| 2006 |
Gao ZG, Jacobson KA. Keynote review: allosterism in membrane receptors. Drug Discovery Today. 11: 191-202. PMID 16580596 DOI: 10.1016/S1359-6446(05)03689-5 |
0.566 |
|
| 2006 |
Wihlborg AK, Balogh J, Wang L, Borna C, Dou Y, Joshi BV, Lazarowski E, Jacobson KA, Arner A, Erlinge D. Positive inotropic effects by uridine triphosphate (UTP) and uridine diphosphate (UDP) via P2Y2 and P2Y6 receptors on cardiomyocytes and release of UTP in man during myocardial infarction. Circulation Research. 98: 970-6. PMID 16543499 DOI: 10.1161/01.Res.0000217402.73402.Cd |
0.501 |
|
| 2006 |
Jacobson KA, Gao ZG. Adenosine receptors as therapeutic targets. Nature Reviews. Drug Discovery. 5: 247-64. PMID 16518376 DOI: 10.1038/Nrd1983 |
0.533 |
|
| 2006 |
Jeong LS, Lee HW, Jacobson KA, Kim HO, Shin DH, Lee JA, Gao ZG, Lu C, Duong HT, Gunaga P, Lee SK, Jin DZ, Chun MW, Moon HR. Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor. Journal of Medicinal Chemistry. 49: 273-81. PMID 16392812 DOI: 10.1021/Jm050595E |
0.713 |
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| 2006 |
Moro S, Gao ZG, Jacobson KA, Spalluto G. Progress in the pursuit of therapeutic adenosine receptor antagonists. Medicinal Research Reviews. 26: 131-59. PMID 16380972 DOI: 10.1002/Med.20048 |
0.816 |
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| 2006 |
Jacobson KA, Costanzi S, Ivanov AA, Tchilibon S, Besada P, Gao ZG, Maddileti S, Harden TK. Structure activity and molecular modeling analyses of ribose- and base-modified uridine 5'-triphosphate analogues at the human P2Y2 and P2Y4 receptors. Biochemical Pharmacology. 71: 540-9. PMID 16359641 DOI: 10.1016/J.Bcp.2005.11.010 |
0.884 |
|
| 2006 |
Houston D, Ohno M, Nicholas RA, Jacobson KA, Harden TK. [32P]2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate ([32P]MRS2500), a novel radioligand for quantification of native P2Y1 receptors. British Journal of Pharmacology. 147: 459-67. PMID 16299552 DOI: 10.1038/Sj.Bjp.0706453 |
0.718 |
|
| 2006 |
Gao ZG, Joshi BV, Klutz AM, Kim SK, Lee HW, Kim HO, Jeong LS, Jacobson KA. Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety. Bioorganic & Medicinal Chemistry Letters. 16: 596-601. PMID 16289820 DOI: 10.1016/J.Bmcl.2005.10.054 |
0.757 |
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| 2006 |
Cosyn L, Gao ZG, Van Rompaey P, Lu C, Jacobson KA, Van Calenbergh S. Synthesis of hypermodified adenosine derivatives as selective adenosine A3 receptor ligands. Bioorganic & Medicinal Chemistry. 14: 1403-12. PMID 16266807 DOI: 10.1016/J.Bmc.2005.09.062 |
0.556 |
|
| 2006 |
Hechler B, Nonne C, Roh EJ, Cattaneo M, Cazenave JP, Lanza F, Jacobson KA, Gachet C. MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice. The Journal of Pharmacology and Experimental Therapeutics. 316: 556-63. PMID 16236815 DOI: 10.1124/Jpet.105.094037 |
0.747 |
|
| 2006 |
Kim S, Jacobson KA, Kim HS. New Synthetic Approach to the Bicyclo[3.1.0]hexane Ring System from (+)-(1R,4R)-4-(Benzyloxymethyl)-4-(hydroxymethyl)cyclopent-2-enol. Cheminform. 37. DOI: 10.5012/Bkcs.2005.26.10.1503 |
0.446 |
|
| 2006 |
Besada P, Mamedova LK, Palaniappan KK, Gao ZG, Joshi BV, Jeong LS, Civan MM, Jacobson KA. Nucleoside prodrugs of A3 adenosine receptor agonists and antagonists Collection of Czechoslovak Chemical Communications. 71: 912-928. DOI: 10.1135/Cccc20060912 |
0.853 |
|
| 2006 |
Gao Z, Joshi BV, Klutz AM, Kim S, Lee HW, Kim HO, Jeong LS, Jacobson KA. Conversion of A3 Adenosine Receptor Agonists into Selective Antagonists by Modification of the 5′-Ribofuran-uronamide Moiety. Cheminform. 37. DOI: 10.1002/CHIN.200618207 |
0.77 |
|
| 2005 |
Kim SA, Jacobson KA, Kim HS. New Synthetic Approach to the Bicyclo[3.1.0]hexane Ring System from (+)-(1,4)-4-(Benzyloxymethyl)-4-(hydroxymethyl)cyclopent-2-enol. Bulletin of the Korean Chemical Society. 26: 1503-1504. PMID 34824486 DOI: 10.5012/bkcs.2005.26.10.1503 |
0.384 |
|
| 2005 |
Kim AY, Kim HO, Kim MJ, Chun MW, Lee KM, Jacobson KA, Jeong LS. Synthesis of 3'-ureidoadenosines and their high binding affinity at the mutant A3 adenosine receptor. Nucleic Acids Symposium Series (2004). 105-6. PMID 17150655 DOI: 10.1093/nass/49.1.105 |
0.611 |
|
| 2005 |
Jeong LS, Lee HW, Jacobson KA, Lee SK, Chun MW. Development of potent and selective human A3 adenosine receptor agonists. Nucleic Acids Symposium Series (2004). 31-2. PMID 17150618 DOI: 10.1093/nass/49.1.31 |
0.686 |
|
| 2005 |
Niebauer RT, Gao ZG, Li B, Wess J, Jacobson KA. Signaling of the Human P2Y(1) Receptor Measured by a Yeast Growth Assay with Comparisons to Assays of Phospholipase C and Calcium Mobilization in 1321N1 Human Astrocytoma Cells. Purinergic Signalling. 1: 241-7. PMID 16467903 DOI: 10.1007/S11302-005-6310-1 |
0.564 |
|
| 2005 |
Duong HT, Gao ZG, Jacobson KA. Nucleoside modification and concerted mutagenesis of the human A3 adenosine receptor to probe interactions between the 2-position of adenosine analogs and Gln167 in the second extracellular loop. Nucleosides, Nucleotides & Nucleic Acids. 24: 1507-17. PMID 16438031 DOI: 10.1080/15257770500265778 |
0.576 |
|
| 2005 |
Costanzi S, Joshi BV, Maddileti S, Mamedova L, Gonzalez-Moa MJ, Marquez VE, Harden TK, Jacobson KA. Human P2Y(6) receptor: molecular modeling leads to the rational design of a novel agonist based on a unique conformational preference. Journal of Medicinal Chemistry. 48: 8108-11. PMID 16366591 DOI: 10.1021/Jm050911P |
0.865 |
|
| 2005 |
Jacobson KA, Gao ZG, Tchilibon S, Duong HT, Joshi BV, Sonin D, Liang BT. Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection. Journal of Medicinal Chemistry. 48: 8103-7. PMID 16366590 DOI: 10.1021/Jm050726B |
0.758 |
|
| 2005 |
Joshi BV, Jacobson KA. Purine derivatives as ligands for A3 adenosine receptors. Current Topics in Medicinal Chemistry. 5: 1275-95. PMID 16305531 DOI: 10.2174/156802605774463079 |
0.653 |
|
| 2005 |
Mamedova L, Capra V, Accomazzo MR, Gao ZG, Ferrario S, Fumagalli M, Abbracchio MP, Rovati GE, Jacobson KA. CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors. Biochemical Pharmacology. 71: 115-25. PMID 16280122 DOI: 10.1016/J.Bcp.2005.10.003 |
0.841 |
|
| 2005 |
Chun MW, Lee HW, Kim AY, Kim MJ, Kim HO, Gao ZG, Jacobson KA, Jeong LS. Synthesis of 3'-ureidoadenosine analogues and their binding affinity to the A3 adenosine receptor. Nucleosides, Nucleotides & Nucleic Acids. 24: 1119-21. PMID 16248104 DOI: 10.1081/Ncn-200060079 |
0.712 |
|
| 2005 |
Lee HW, Shin DH, Jeong JY, Kim HO, Chun MW, Melman N, Gao ZG, Jacobson KA, Jeong LS. D-4'-thioadenosine derivatives as highly potent and selective agonists at the human A3 adenosine receptor. Nucleosides, Nucleotides & Nucleic Acids. 24: 607-9. PMID 16247997 DOI: 10.1081/NCN-200061827 |
0.671 |
|
| 2005 |
Berk B, Akgün H, Erol K, Sirmagül B, Gao ZG, Jacobson KA. New 8-substituted xanthiene derivatives as potent bronchodilators. Farmaco (Societã Chimica Italiana : 1989). 60: 974-80. PMID 16243321 DOI: 10.1016/J.Farmac.2005.08.011 |
0.536 |
|
| 2005 |
Yang H, Avila MY, Peterson-Yantorno K, Coca-Prados M, Stone RA, Jacobson KA, Civan MM. The cross-species A3 adenosine-receptor antagonist MRS 1292 inhibits adenosine-triggered human nonpigmented ciliary epithelial cell fluid release and reduces mouse intraocular pressure. Current Eye Research. 30: 747-54. PMID 16146920 DOI: 10.1080/02713680590953147 |
0.671 |
|
| 2005 |
Han SJ, Hamdan FF, Kim SK, Jacobson KA, Bloodworth LM, Li B, Wess J. Identification of an agonist-induced conformational change occurring adjacent to the ligand-binding pocket of the M(3) muscarinic acetylcholine receptor. The Journal of Biological Chemistry. 280: 34849-58. PMID 16093246 DOI: 10.1074/Jbc.M506711200 |
0.707 |
|
| 2005 |
Perreira M, Jiang JK, Klutz AM, Gao ZG, Shainberg A, Lu C, Thomas CJ, Jacobson KA. "Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. Journal of Medicinal Chemistry. 48: 4910-8. PMID 16033270 DOI: 10.1021/Jm050221L |
0.566 |
|
| 2005 |
Gao ZG, Kim SK, Ijzerman AP, Jacobson KA. Allosteric modulation of the adenosine family of receptors. Mini Reviews in Medicinal Chemistry. 5: 545-53. PMID 15974932 DOI: 10.2174/1389557054023242 |
0.759 |
|
| 2005 |
Lee JA, Moon HR, Kim HO, Kim KR, Lee KM, Kim BT, Hwang KJ, Chun MW, Jacobson KA, Jeong LS. Synthesis of novel apio carbocyclic nucleoside analogues as selective a(3) adenosine receptor agonists. The Journal of Organic Chemistry. 70: 5006-13. PMID 15960499 DOI: 10.1021/Jo0503207 |
0.72 |
|
| 2005 |
Kim YC, Lee JS, Sak K, Marteau F, Mamedova L, Boeynaems JM, Jacobson KA. Synthesis of pyridoxal phosphate derivatives with antagonist activity at the P2Y13 receptor. Biochemical Pharmacology. 70: 266-74. PMID 15913566 DOI: 10.1016/J.Bcp.2005.04.021 |
0.866 |
|
| 2005 |
Balogh J, Wihlborg AK, Isackson H, Joshi BV, Jacobson KA, Arner A, Erlinge D. Phospholipase C and cAMP-dependent positive inotropic effects of ATP in mouse cardiomyocytes via P2Y11-like receptors. Journal of Molecular and Cellular Cardiology. 39: 223-30. PMID 15893764 DOI: 10.1016/J.Yjmcc.2005.03.007 |
0.564 |
|
| 2005 |
Besada P, Mamedova L, Thomas CJ, Costanzi S, Jacobson KA. Design and synthesis of new bicyclic diketopiperazines as scaffolds for receptor probes of structurally diverse functionality. Organic & Biomolecular Chemistry. 3: 2016-25. PMID 15889186 DOI: 10.1039/B416349D |
0.867 |
|
| 2005 |
Han SJ, Hamdan FF, Kim SK, Jacobson KA, Brichta L, Bloodworth LM, Li JH, Wess J. Pronounced conformational changes following agonist activation of the M(3) muscarinic acetylcholine receptor. The Journal of Biological Chemistry. 280: 24870-9. PMID 15870064 DOI: 10.1074/Jbc.M500379200 |
0.691 |
|
| 2005 |
Jacobson KA, Mamedova L, Joshi BV, Besada P, Costanzi S. Molecular recognition at adenine nucleotide (P2) receptors in platelets. Seminars in Thrombosis and Hemostasis. 31: 205-16. PMID 15852224 DOI: 10.1055/S-2005-869526 |
0.882 |
|
| 2005 |
Yitzhaki S, Shneyvays V, Jacobson KA, Shainberg A. Involvement of uracil nucleotides in protection of cardiomyocytes from hypoxic stress. Biochemical Pharmacology. 69: 1215-23. PMID 15794942 DOI: 10.1016/J.Bcp.2005.01.018 |
0.464 |
|
| 2005 |
Tchilibon S, Joshi BV, Kim SK, Duong HT, Gao ZG, Jacobson KA. (N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists. Journal of Medicinal Chemistry. 48: 1745-58. PMID 15771421 DOI: 10.1021/Jm049580R |
0.661 |
|
| 2005 |
Erdmann AA, Gao ZG, Jung U, Foley J, Borenstein T, Jacobson KA, Fowler DH. Activation of Th1 and Tc1 cell adenosine A2A receptors directly inhibits IL-2 secretion in vitro and IL-2-driven expansion in vivo. Blood. 105: 4707-14. PMID 15746085 DOI: 10.1182/Blood-2004-04-1407 |
0.381 |
|
| 2005 |
Jacobson KA, Ohno M, Duong HT, Kim SK, Tchilibon S, Cesnek M, Holý A, Gao ZG. A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists. Chemistry & Biology. 12: 237-47. PMID 15734651 DOI: 10.1016/J.Chembiol.2004.12.010 |
0.699 |
|
| 2005 |
Shneyvays V, Leshem D, Zinman T, Mamedova LK, Jacobson KA, Shainberg A. Role of adenosine A1 and A3 receptors in regulation of cardiomyocyte homeostasis after mitochondrial respiratory chain injury. American Journal of Physiology. Heart and Circulatory Physiology. 288: H2792-801. PMID 15681707 DOI: 10.1152/Ajpheart.01157.2004 |
0.764 |
|
| 2005 |
Van Rompaey P, Jacobson KA, Gross AS, Gao ZG, Van Calenbergh S. Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety. Bioorganic & Medicinal Chemistry. 13: 973-83. PMID 15670905 DOI: 10.1016/J.Bmc.2004.11.044 |
0.565 |
|
| 2005 |
Joshi BV, Moon HR, Fettinger JC, Marquez VE, Jacobson KA. A new synthetic route to (North)-methanocarba nucleosides designed as A3 adenosine receptor agonists. The Journal of Organic Chemistry. 70: 439-47. PMID 15651784 DOI: 10.1021/Jo0487606 |
0.556 |
|
| 2005 |
Moro S, Spalluto G, Jacobson KA. Techniques: Recent developments in computer-aided engineering of GPCR ligands using the human adenosine A3 receptor as an example. Trends in Pharmacological Sciences. 26: 44-51. PMID 15629204 DOI: 10.1016/J.Tips.2004.11.006 |
0.762 |
|
| 2005 |
Abbracchio MP, Burnstock G, Boeynaems JM, Barnard EA, Boyer JL, Kennedy C, Miras-Portugal MT, King BF, Gachet C, Jacobson KA, Weisman GA. The recently deorphanized GPR80 (GPR99) proposed to be the P2Y15 receptor is not a genuine P2Y receptor. Trends in Pharmacological Sciences. 26: 8-9. PMID 15629198 DOI: 10.1016/J.Tips.2004.10.010 |
0.65 |
|
| 2005 |
Hu J, McLarnon SJ, Mora S, Jiang J, Thomas C, Jacobson KA, Spiegel AM. A region in the seven-transmembrane domain of the human Ca2+ receptor critical for response to Ca2+. The Journal of Biological Chemistry. 280: 5113-20. PMID 15591042 DOI: 10.1074/Jbc.M413403200 |
0.358 |
|
| 2005 |
Li B, Nowak NM, Kim SK, Jacobson KA, Bagheri A, Schmidt C, Wess J. Random mutagenesis of the M3 muscarinic acetylcholine receptor expressed in yeast: identification of second-site mutations that restore function to a coupling-deficient mutant M3 receptor. The Journal of Biological Chemistry. 280: 5664-75. PMID 15572356 DOI: 10.1074/Jbc.M411623200 |
0.678 |
|
| 2005 |
Cosyn L, Jacobson KA, Calenbergh SV. 2-(1,2,3-Triazol-1-yl) N 6 -CH 3 -substituted adenosine derivatives: Highly potent and selective A 3 receptor ligands Collection of Czechoslovak Chemical Communications. 7: 393-394. DOI: 10.1135/Css200507393 |
0.505 |
|
| 2004 |
Dunn PM, Kim HS, Jacobson KA, Burnstock G. Northern Ring Conformation of Methanocarba-Adenosine 5'-Triphosphate Required for Activation of P2X Receptors. Drug Development Research. 61: 227-232. PMID 22833693 DOI: 10.1002/Ddr.10381 |
0.735 |
|
| 2004 |
Ji XD, Gallo-Rodriguez C, Jacobson KA. 8-(3-Isothiocyanatostyryl)caffeine Is a Selective, Irreversible Inhibitor of Striatal A(2)-Adenosine Receptors. Drug Development Research. 29: 292-298. PMID 22787287 DOI: 10.1002/Ddr.430290407 |
0.804 |
|
| 2004 |
Olivecrona GK, Gotberg M, Harnek J, Wang L, Jacobson KA, Erlinge D. Coronary artery reperfusion: The ADP receptor P2Y(1) mediates early reactive hyperemia in vivo in pigs. Purinergic Signalling. 1: 59-65. PMID 18404401 DOI: 10.1007/S11302-004-4742-7 |
0.331 |
|
| 2004 |
Jacobson KA, Kim SK, Costanzi S, Gao ZG. Purine receptors: GPCR structure and agonist design. Molecular Interventions. 4: 337-47. PMID 15616163 DOI: 10.1124/Mi.4.6.7 |
0.828 |
|
| 2004 |
Costanzi S, Mamedova L, Gao ZG, Jacobson KA. Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. Journal of Medicinal Chemistry. 47: 5393-404. PMID 15481977 DOI: 10.1021/Jm049914C |
0.862 |
|
| 2004 |
Hoffmann C, Soltysiak K, West PL, Jacobson KA. Shift in purine/pyrimidine base recognition upon exchanging extracellular domains in P2Y 1/6 chimeric receptors. Biochemical Pharmacology. 68: 2075-86. PMID 15476678 DOI: 10.1016/J.Bcp.2004.07.014 |
0.776 |
|
| 2004 |
Cattaneo M, Lecchi A, Ohno M, Joshi BV, Besada P, Tchilibon S, Lombardi R, Bischofberger N, Harden TK, Jacobson KA. Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor. Biochemical Pharmacology. 68: 1995-2002. PMID 15476670 DOI: 10.1016/J.Bcp.2004.06.026 |
0.831 |
|
| 2004 |
Gao ZG, Mamedova LK, Chen P, Jacobson KA. 2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors. Biochemical Pharmacology. 68: 1985-93. PMID 15476669 DOI: 10.1016/J.Bcp.2004.06.011 |
0.826 |
|
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