Kenneth A. Jacobson - Publications

Affiliations: 
Molecular Recognition NIDDK, NIH, Bethesda, MD, United States 
Area:
GPCRs, adenosine, P2 receptors
Website:
https://www.niddk.nih.gov/about-niddk/staff-directory/biography/jacobson-kenneth

500 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
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 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  0.367
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  0.862
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  0.587
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  0.398
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  0.727
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  0.77
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  0.611
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  0.519
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  0.793
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  0.436
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  0.742
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  0.441
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  0.434
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  0.664
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  0.693
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  0.404
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  0.642
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  0.546
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  0.458
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  0.577
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  0.489
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  0.846
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  0.544
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  0.818
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  0.446
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  0.533
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  0.698
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  0.51
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  0.588
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  0.634
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  0.359
2020 Jain S, Jacobson KA. Purinergic signaling in diabetes and metabolism. Biochemical Pharmacology. 114393. PMID 33359363 DOI: 10.1016/j.bcp.2020.114393  0.398
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  0.813
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  0.719
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  0.751
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  0.69
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  0.772
2020 Tosh DK, Toti KS, Hurst BL, Julander JG, Jacobson KA. Structure activity relationship of novel antiviral nucleosides against Enterovirus A71. Bioorganic & Medicinal Chemistry Letters. 30: 127599. PMID 33031923 DOI: 10.1016/j.bmcl.2020.127599  0.302
2020 Jacobson KA, Salmaso V. Purinergic signaling: Impact of GPCR structures on rational drug design. Chemmedchem. PMID 32803849 DOI: 10.1002/cmdc.202000465  0.492
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  0.446
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  0.831
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  0.594
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  0.549
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  0.784
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  0.456
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  0.575
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  0.753
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  0.578
2020 Jacobson KA, Reitman ML. Adenosine-Related Mechanisms in Non-Adenosine Receptor Drugs. Cells. 9. PMID 32295065 DOI: 10.3390/Cells9040956  0.426
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  0.563
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  0.779
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  0.66
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  0.578
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  0.708
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  0.581
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  0.324
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  0.568
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  0.649
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  0.855
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  0.451
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  0.601
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  0.806
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  0.612
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
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  0.59
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  0.372
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  0.54
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  0.804
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
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  0.543
2019 Ciruela F, Jacobson KA. Editorial: Purinergic Pharmacology. Frontiers in Pharmacology. 10: 21. PMID 30728779 DOI: 10.3389/Fphar.2019.00021  0.587
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  0.751
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
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  0.355
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
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  0.507
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  0.325
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  0.501
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  0.84
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
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  0.548
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  0.868
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  0.78
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
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  0.576
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  0.564
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  0.603
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  0.675
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  0.79
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  0.722
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  0.583
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  0.587
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  0.699
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  0.552
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  0.455
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  0.5
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  0.506
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  0.377
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  0.815
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  0.43
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  0.455
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  0.823
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  0.453
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  0.686
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  0.496
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  0.663
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  0.717
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  0.819
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  0.797
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  0.579
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  0.607
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  0.608
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  0.641
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  0.774
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  0.687
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  0.465
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  0.713
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  0.542
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  0.38
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  0.846
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  0.535
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  0.429
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  0.812
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  0.458
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  0.675
2015 Jacobson KA, Müller CE. Medicinal Chemistry of Adenosine, P2Y and P2X Receptors. Neuropharmacology. PMID 26686393 DOI: 10.1016/J.Neuropharm.2015.12.001  0.74
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  0.685
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  0.86
2015 Jacobson KA. New paradigms in GPCR drug discovery. Biochemical Pharmacology. PMID 26265138 DOI: 10.1016/J.Bcp.2015.08.085  0.419
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  0.823
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  0.337
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  0.816
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  0.845
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  0.615
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  0.607
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  0.661
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  0.547
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  0.531
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  0.657
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  0.638
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  0.332
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  0.64
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  0.752
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  0.576
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  0.565
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  0.683
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  0.623
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  0.611
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  0.328
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  0.825
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  0.566
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  0.785
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  0.624
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  0.761
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  0.566
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  0.838
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  0.624
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  0.715
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  0.392
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  0.731
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  0.69
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  0.712
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  0.612
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  0.682
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  0.648
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  0.63
2014 Jacobson K, Ciruela F. Synthesis of the Adenosine A2A Receptor Fluorescent Agonist MRS5424 Bio-Protocol. 4. DOI: 10.21769/BIOPROTOC.1069  0.664
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  0.61
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  0.61
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  0.563
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  0.425
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  0.495
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  0.811
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  0.669
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  0.544
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  0.708
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  0.574
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  0.73
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  0.662
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  0.625
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  0.756
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  0.723
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  0.502
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  0.642
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  0.581
2012 Costanzi S, Santhosh Kumar T, Balasubramanian R, Kendall Harden T, Jacobson KA. Virtual screening leads to the discovery of novel non-nucleotide P2Y₁ receptor antagonists. Bioorganic & Medicinal Chemistry. 20: 5254-61. PMID 22831801 DOI: 10.1016/J.Bmc.2012.06.044  0.742
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 P2Y₁₂ receptor-mediated platelet aggregation. Thrombosis and Haemostasis. 108: 119-32. PMID 22628078 DOI: 10.1160/Th11-10-0749  0.483
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  0.788
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  0.677
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  0.552
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  0.65
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  0.542
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  0.66
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  0.705
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  0.722
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  0.75
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  0.39
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  0.787
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  0.706
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  0.739
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  0.676
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  0.409
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  0.63
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  0.355
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  0.703
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  0.689
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  0.835
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  0.692
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  0.573
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  0.704
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  0.754
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  0.786
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  0.563
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  0.597
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  0.667
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  0.757
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  0.613
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  0.499
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  0.723
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  0.569
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  0.508
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  0.623
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  0.723
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  0.531
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  0.828
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  0.883
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  0.532
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  0.753
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  0.53
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  0.798
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  0.657
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  0.693
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  0.751
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
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  0.59
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  0.77
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  0.82
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
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  0.851
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  0.531
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  0.443
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  0.486
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  0.379
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  0.464
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
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  0.623
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  0.48
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  0.511
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  0.746
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  0.823
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  0.669
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  0.729
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  0.692
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  0.831
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  0.84
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  0.773
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
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  0.833
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
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  0.766
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  0.572
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  0.767
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  0.696
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  0.84
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  0.502
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  0.445
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
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  0.823
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
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  0.754
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
2009 Jacobson KA, Kirk KL. John W. Daly - An appreciation Heterocycles. 79: 61-71. DOI: 10.3987/Com-08-S(D)Memoire-1  0.436
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  0.681
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  0.852
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  0.7
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  0.6
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  0.672
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
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  0.651
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  0.65
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  0.834
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  0.417
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  0.701
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  0.679
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  0.84
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  0.649
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  0.788
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  0.73
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  0.705
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  0.382
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  0.76
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  0.685
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  0.743
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  0.41
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  0.624
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  0.67
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  0.702
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  0.781
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  0.801
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  0.861
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  0.365
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  0.654
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  0.401
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  0.637
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  0.736
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  0.699
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  0.694
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  0.492
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  0.755
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  0.662
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  0.718
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  0.826
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  0.685
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  0.563
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  0.471
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  0.849
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  0.573
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  0.734
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  0.632
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  0.758
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  0.652
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  0.644
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  0.736
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  0.727
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  0.881
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  0.837
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  0.653
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  0.795
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  0.61
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  0.694
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  0.732
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  0.464
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  0.714
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  0.565
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  0.531
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  0.716
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  0.819
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  0.736
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  0.764
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  0.557
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  0.753
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  0.447
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  0.854
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  0.777
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  0.388
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  0.617
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  0.69
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  0.565
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  0.766
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  0.655
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  0.715
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  0.675
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  0.537
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  0.672
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  0.713
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  0.568
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  0.764
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  0.723
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  0.868
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  0.698
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  0.463
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  0.671
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  0.708
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  0.567
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  0.559
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  0.766
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  0.649
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  0.359
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  0.685
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  0.506
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  0.736
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  0.808
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  0.831
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  0.786
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  0.839
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  0.827
2004 Ohno M, Costanzi S, Kim HS, Kempeneers V, Vastmans K, Herdewijn P, Maddileti S, Gao ZG, Harden TK, Jacobson KA. Nucleotide analogues containing 2-oxa-bicyclo[2.2.1]heptane and l-alpha-threofuranosyl ring systems: interactions with P2Y receptors. Bioorganic & Medicinal Chemistry. 12: 5619-30. PMID 15465340 DOI: 10.1016/J.Bmc.2004.07.067  0.852
2004 Chhatriwala M, Ravi RG, Patel RI, Boyer JL, Jacobson KA, Harden TK. Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog. The Journal of Pharmacology and Experimental Therapeutics. 311: 1038-43. PMID 15345752 DOI: 10.1124/Jpet.104.068650  0.762
2004 Jeong LS, Kim MJ, Kim HO, Gao ZG, Kim SK, Jacobson KA, Chun MW. Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor. Bioorganic & Medicinal Chemistry Letters. 14: 4851-4. PMID 15341938 DOI: 10.1016/J.Bmcl.2004.07.042  0.762
2004 Guerra L, Favia M, Fanelli T, Calamita G, Svetlo M, Bagorda A, Jacobson KA, Reshkin SJ, Casavola V. Stimulation of Xenopus P2Y1 receptor activates CFTR in A6 cells. Pflã¼Gers Archiv : European Journal of Physiology. 449: 66-75. PMID 15235914 DOI: 10.1007/S00424-004-1293-2  0.523
2004 Gao ZG, Mamedova L, Tchilibon S, Gross AS, Jacobson KA. 2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding. Biochemical Pharmacology. 68: 231-7. PMID 15193995 DOI: 10.1016/J.Bcp.2004.02.039  0.851
2004 Ohno M, Gao ZG, Van Rompaey P, Tchilibon S, Kim SK, Harris BA, Gross AS, Duong HT, Van Calenbergh S, Jacobson KA. Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position. Bioorganic & Medicinal Chemistry. 12: 2995-3007. PMID 15142558 DOI: 10.1016/J.Bmc.2004.03.031  0.718
2004 Gao ZG, Jeong LS, Moon HR, Kim HO, Choi WJ, Shin DH, Elhalem E, Comin MJ, Melman N, Mamedova L, Gross AS, Rodriguez JB, Jacobson KA. Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moiety. Biochemical Pharmacology. 67: 893-901. PMID 15104242 DOI: 10.1016/J.Bcp.2003.10.006  0.847
2004 Mamedova LK, Joshi BV, Gao ZG, von Kügelgen I, Jacobson KA. Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochemical Pharmacology. 67: 1763-70. PMID 15081875 DOI: 10.1016/J.Bcp.2004.01.011  0.846
2004 Gao ZG, Gross AS, Jacobson KA. Effects of the allosteric modulator SCH-202676 on adenosine and P2Y receptors. Life Sciences. 74: 3173-80. PMID 15081581 DOI: 10.1016/J.Lfs.2003.11.014  0.646
2004 Tchilibon S, Kim SK, Gao ZG, Harris BA, Blaustein JB, Gross AS, Duong HT, Melman N, Jacobson KA. Exploring distal regions of the A3 adenosine receptor binding site: sterically constrained N6-(2-phenylethyl)adenosine derivatives as potent ligands. Bioorganic & Medicinal Chemistry. 12: 2021-34. PMID 15080906 DOI: 10.1016/J.Bmc.2004.02.037  0.703
2004 Gao ZG, Jacobson KA. Partial agonists for A(3) adenosine receptors. Current Topics in Medicinal Chemistry. 4: 855-62. PMID 15078216 DOI: 10.2174/1568026043450989  0.554
2004 Jacobson KA, Costanzi S, Ohno M, Joshi BV, Besada P, Xu B, Tchilibon S. Molecular recognition at purine and pyrimidine nucleotide (P2) receptors. Current Topics in Medicinal Chemistry. 4: 805-19. PMID 15078212 DOI: 10.2174/1568026043450961  0.876
2004 Jung KY, Kim SK, Gao ZG, Gross AS, Melman N, Jacobson KA, Kim YC. Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists. Bioorganic & Medicinal Chemistry. 12: 613-23. PMID 14738972 DOI: 10.1016/J.Bmc.2003.10.041  0.814
2004 Mozzicato S, Joshi BV, Jacobson KA, Liang BT. Role of direct RhoA-phospholipase D1 interaction in mediating adenosine-induced protection from cardiac ischemia. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 18: 406-8. PMID 14688204 DOI: 10.1096/Fj.03-0592Fje  0.742
2004 Jacobson K. Preface [Hot Topic: Receptors for Extracellular Nucleosides and Nucleotides (Guest Editor: Kenneth A. Jacobson)] Current Topics in Medicinal Chemistry. 4: i-i. DOI: 10.2174/1568026043450970  0.463
2004 Kim HO, Park JG, Moon HR, Gunaga P, Lim MH, Chun MW, Jacobson KA, Kim H, Jeong LS. Design and Synthesis of A3 Adenosine Receptor Ligands, 2′-Fluoro Analogues of Cl-IB-MECA Cheminform. 35. DOI: 10.1002/CHIN.200405189  0.641
2004 Kim HO, Lim MH, Park JG, Moon HR, Jacobson KA, Kim H, Chun MW, Jeong LS. Design and Synthesis of A3 Adenosine Receptor Ligands, 3′-Fluoro Analogues of Cl-IB-MECA Cheminform. 35. DOI: 10.1002/CHIN.200405188  0.641
2003 Moro S, Deflorian F, Spalluto G, Pastorin G, Cacciari B, Kim SK, Jacobson KA. Demystifying the three dimensional structure of G protein-coupled receptors (GPCRs) with the aid of molecular modeling. Chemical Communications (Cambridge, England). 2949-56. PMID 14703805 DOI: 10.1039/B303439A  0.839
2003 Kim HS, Ohno M, Xu B, Kim HO, Choi Y, Ji XD, Maddileti S, Marquez VE, Harden TK, Jacobson KA. 2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists. Journal of Medicinal Chemistry. 46: 4974-87. PMID 14584948 DOI: 10.1021/Jm030127+  0.805
2003 Kim SK, Gao ZG, Van Rompaey P, Gross AS, Chen A, Van Calenbergh S, Jacobson KA. Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists. Journal of Medicinal Chemistry. 46: 4847-59. PMID 14584936 DOI: 10.1021/Jm0300431  0.684
2003 Goldenberg I, Shainberg A, Jacobson KA, Shneyvays V, Grossman E. Adenosine protects against angiotensin II-induced apoptosis in rat cardiocyte cultures. Molecular and Cellular Biochemistry. 252: 133-9. PMID 14577586 DOI: 10.1023/A:1025551229566  0.483
2003 Kim HO, Park JG, Moon HR, Gunaga P, Lim MH, Chun MW, Jacobson KA, Kim HD, Jeong LS. Design and synthesis of A3 adenosine receptor ligands, 2'-fluoro analogues of Cl-IB-MECA. Nucleosides, Nucleotides & Nucleic Acids. 22: 927-30. PMID 14565313 DOI: 10.1081/NCN-120022687  0.674
2003 Kim HO, Lim MH, Park JG, Moon HR, Jacobson KA, Kim HD, Chun MW, Jeong LS. Design and synthesis of A3 adenosine receptor ligands, 3'-fluoro analogues of Cl-IB-MECA. Nucleosides, Nucleotides & Nucleic Acids. 22: 923-5. PMID 14565312 DOI: 10.1081/Ncn-120022701  0.711
2003 Chun MW, Lim MH, Moon HR, Kim HO, Jacobson KA, Jeong LS. Synthesis of 3'-fluoro analogue of Cl-IB-MECA as adenosine A3 receptor ligand. Nucleic Acids Research. Supplement (2001). 19-20. PMID 14510359 DOI: 10.1093/nass/3.1.19  0.669
2003 Jacobson KA. Molecular recognition in P2 nucleotide receptors. Nucleic Acids Research. Supplement (2001). 3-4. PMID 14510351  0.361
2003 Eltzschig HK, Ibla JC, Furuta GT, Leonard MO, Jacobson KA, Enjyoji K, Robson SC, Colgan SP. Coordinated adenine nucleotide phosphohydrolysis and nucleoside signaling in posthypoxic endothelium: role of ectonucleotidases and adenosine A2B receptors. The Journal of Experimental Medicine. 198: 783-96. PMID 12939345 DOI: 10.1084/Jem.20030891  0.364
2003 Jeong LS, Jin DZ, Kim HO, Shin DH, Moon HR, Gunaga P, Chun MW, Kim YC, Melman N, Gao ZG, Jacobson KA. N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor. Journal of Medicinal Chemistry. 46: 3775-7. PMID 12930138 DOI: 10.1021/Jm034098E  0.778
2003 Choi Y, George C, Comin MJ, Barchi JJ, Kim HS, Jacobson KA, Balzarini J, Mitsuya H, Boyer PL, Hughes SH, Marquez VE. A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude. Journal of Medicinal Chemistry. 46: 3292-9. PMID 12852759 DOI: 10.1021/Jm030116G  0.497
2003 Fedorova IM, Jacobson MA, Basile A, Jacobson KA. Behavioral characterization of mice lacking the A3 adenosine receptor: sensitivity to hypoxic neurodegeneration. Cellular and Molecular Neurobiology. 23: 431-47. PMID 12825837 DOI: 10.1023/A:1023601007518  0.301
2003 Kim SG, Gao ZG, Soltysiak KA, Chang TS, Brodie C, Jacobson KA. P2Y6 nucleotide receptor activates PKC to protect 1321N1 astrocytoma cells against tumor necrosis factor-induced apoptosis. Cellular and Molecular Neurobiology. 23: 401-18. PMID 12825835 DOI: 10.1023/A:1023696806609  0.387
2003 Gorman MW, Ogimoto K, Savage MV, Jacobson KA, Feigl EO. Nucleotide coronary vasodilation in guinea pig hearts. American Journal of Physiology. Heart and Circulatory Physiology. 285: H1040-7. PMID 12763753 DOI: 10.1152/Ajpheart.00981.2002  0.523
2003 Gao ZG, Blaustein JB, Gross AS, Melman N, Jacobson KA. N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors. Biochemical Pharmacology. 65: 1675-84. PMID 12754103 DOI: 10.1016/S0006-2952(03)00153-9  0.529
2003 Kim HS, Jacobson KA. Synthesis of a novel conformationally locked carbocyclic nucleoside ring system. Organic Letters. 5: 1665-8. PMID 12735747 DOI: 10.1021/Ol034326Z  0.479
2003 Wihlborg A, Malmsjö M, Eyjolfsson A, Gustafsson R, Jacobson K, Erlinge D. Extracellular nucleotides induce vasodilatation in human arteries via prostaglandins, nitric oxide and endothelium‐derived hyperpolarising factor British Journal of Pharmacology. 138: 1451-1458. PMID 12721100 DOI: 10.1038/Sj.Bjp.0705186  0.495
2003 Gao ZG, Kim SK, Gross AS, Chen A, Blaustein JB, Jacobson KA. Identification of essential residues involved in the allosteric modulation of the human A(3) adenosine receptor. Molecular Pharmacology. 63: 1021-31. PMID 12695530 DOI: 10.1124/Mol.63.5.1021  0.694
2003 Kim SG, Soltysiak KA, Gao ZG, Chang TS, Chung E, Jacobson KA. Tumor necrosis factor alpha-induced apoptosis in astrocytes is prevented by the activation of P2Y6, but not P2Y4 nucleotide receptors. Biochemical Pharmacology. 65: 923-31. PMID 12623123 DOI: 10.1016/S0006-2952(02)01614-3  0.446
2003 Lim MH, Kim HO, Moon HR, Lee SJ, Chun MW, Gao ZG, Melman N, Jacobson KA, Kim JH, Jeong LS. Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands. Bioorganic & Medicinal Chemistry Letters. 13: 817-20. PMID 12617898 DOI: 10.1016/S0960-894X(03)00027-1  0.707
2003 Gao ZG, Melman N, Erdmann A, Kim SG, Müller CE, IJzerman AP, Jacobson KA. Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors. Biochemical Pharmacology. 65: 525-34. PMID 12566079 DOI: 10.1016/S0006-2952(02)01556-3  0.834
2003 Abbracchio MP, Boeynaems JM, Barnard EA, Boyer JL, Kennedy C, Miras-Portugal MT, King BF, Gachet C, Jacobson KA, Weisman GA, Burnstock G. Characterization of the UDP-glucose receptor (re-named here the P2Y14 receptor) adds diversity to the P2Y receptor family. Trends in Pharmacological Sciences. 24: 52-5. PMID 12559763 DOI: 10.1016/S0165-6147(02)00038-X  0.643
2003 Harper JL, Camerini-Otero CS, Li AH, Kim SA, Jacobson KA, Daly JW. Dihydropyridines as inhibitors of capacitative calcium entry in leukemic HL-60 cells. Biochemical Pharmacology. 65: 329-38. PMID 12527326 DOI: 10.1016/S0006-2952(02)01488-0  0.439
2003 Ozola V, Thorand M, Diekmann M, Qurishi R, Schumacher B, Jacobson KA, Müller CE. 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors. Bioorganic & Medicinal Chemistry. 11: 347-56. PMID 12517430 DOI: 10.1016/S0968-0896(02)00456-X  0.754
2003 Webb TR, Lvovskiy D, Kim SA, Ji Xd, Melman N, Linden J, Jacobson KA. Quinazolines as adenosine receptor antagonists: SAR and selectivity for A2B receptors. Bioorganic & Medicinal Chemistry. 11: 77-85. PMID 12467710 DOI: 10.1016/S0968-0896(02)00323-1  0.615
2003 Gao ZG, Jacobson KA. 2-Chloro-N(6)-cyclopentyladenosine, adenosine A(1) receptor agonist, antagonizes the adenosine A(3) receptor. European Journal of Pharmacology. 443: 39-42. PMID 12044789 DOI: 10.1016/S0014-2999(02)01552-2  0.592
2003 Lim MH, Kim HO, Moon HR, Lee SJ, Chun MW, Gao Z, Melman N, Jacobson KA, Kim JH, Jeong LS. Corrigendum to ‘Design, Synthesis and Binding Affinity of 3′-Fluoro Analogues of C1-IB-MECA as Adenosine A3 Receptor Ligands’[Bioorg. Med. Chem. Lett. 13 (2003) 817]† Bioorganic & Medicinal Chemistry Letters. 13: 2087. DOI: 10.1016/S0960-894X(03)00332-9  0.69
2003 Jacobson KA, Kim HS, Ravi G, Kim S, Lee K, Chen A, Chen W, Kim SG, Barak D, Liang BT, Gao Z. Engineering of A3 adenosine and P2Y nucleotide receptors and their ligands Drug Development Research. 58: 330-339. DOI: 10.1002/Ddr.10168  0.885
2002 Guo D, von Kügelgen I, Moro S, Kim YC, Jacobson KA. Evidence for the Recognition of Non-Nucleotide Antagonists Within the Transmembrane Domains of the Human P2Y(1) Receptor. Drug Development Research. 57: 173-181. PMID 23105165 DOI: 10.1002/Ddr.10145  0.781
2002 Xu B, Stephens A, Kirschenheuter G, Greslin AF, Cheng X, Sennelo J, Cattaneo M, Zighetti ML, Chen A, Kim SA, Kim HS, Bischofberger N, Cook G, Jacobson KA. Acyclic analogues of adenosine bisphosphates as P2Y receptor antagonists: phosphate substitution leads to multiple pathways of inhibition of platelet aggregation. Journal of Medicinal Chemistry. 45: 5694-709. PMID 12477353 DOI: 10.1021/Jm020173U  0.705
2002 Trincavelli ML, Tuscano D, Marroni M, Falleni A, Gremigni V, Ceruti S, Abbracchio MP, Jacobson KA, Cattabeni F, Martini C. A3 adenosine receptors in human astrocytoma cells: agonist-mediated desensitization, internalization, and down-regulation. Molecular Pharmacology. 62: 1373-84. PMID 12435805 DOI: 10.1124/Mol.62.6.1373  0.614
2002 Waldo GL, Corbitt J, Boyer JL, Ravi G, Kim HS, Ji XD, Lacy J, Jacobson KA, Harden TK. Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist. Molecular Pharmacology. 62: 1249-57. PMID 12391289 DOI: 10.1124/Mol.62.5.1249  0.722
2002 Moro S, Jacobson KA. Molecular modeling as a tool to investigate molecular recognition in P2Y receptors. Current Pharmaceutical Design. 8: 2401-13. PMID 12369952 DOI: 10.2174/1381612023392892  0.709
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