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Kenneth A. Jacobson - Publications

Affiliations: 
Molecular Recognition NIDDK, NIH, Bethesda, MD, United States 
Area:
adenosine, P2 receptors
Website:
http://www2.niddk.nih.gov/NIDDKLabs/IntramuralFaculty/JacobsonKenneth.htm

476 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
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2019 Ciruela F, Jacobson KA. Editorial: Purinergic Pharmacology. Frontiers in Pharmacology. 10: 21. PMID 30728779 DOI: 10.3389/fphar.2019.00021  1
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  1
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  1
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  1
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  1
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  1
2018 Navratna V, Tosh DK, Jacobson KA, Gouaux E. Thermostabilization and purification of the human dopamine transporter (hDAT) in an inhibitor and allosteric ligand bound conformation. Plos One. 13: e0200085. PMID 29965988 DOI: 10.1371/journal.pone.0200085  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2016 Lloyd JR, Jayasekara PS, Jacobson KA. Characterization of Polyamidoamino (PAMAM) Dendrimers Using In-Line Reversed Phase LC Electrospray Ionization Mass Spectrometry. Analytical Methods : Advancing Methods and Applications. 8: 263-269. PMID 26997980 DOI: 10.1039/C5AY01995H  1
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  1
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  1
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  1
2016 Lloyd JR, Suresh Jayasekara P, Jacobson KA. Characterization of polyamidoamino (PAMAM) dendrimers using in-line reversed phase LC electrospray ionization mass spectrometry Analytical Methods. 8: 263-269. DOI: 10.1039/c5ay01995h  1
2015 Jacobson KA, Müller CE. Medicinal Chemistry of Adenosine, P2Y and P2X Receptors. Neuropharmacology. PMID 26686393 DOI: 10.1016/j.neuropharm.2015.12.001  1
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  1
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  1
2015 Jacobson KA. New paradigms in GPCR drug discovery. Biochemical Pharmacology. PMID 26265138 DOI: 10.1016/j.bcp.2015.08.085  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2015 Palmer C. A Key Opinion Leader interview: insight into the research and career of Dr KA Jacobson. Expert Opinion On Therapeutic Patents. 25: 125-9. PMID 25495234 DOI: 10.1517/13543776.2015.993539  0.01
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  1
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  1
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  1
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  1
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  1
2015 Jacobson KA. Meet the editorial board Current Topics in Medicinal Chemistry. 15: 279.  1
2014 Kirk KL, Jacobson KA. History of Chemistry in the National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK). Bulletin For the History of Chemistry / Division of the History of Chemistry of the American Chemical Society. 39: 150-165. PMID 26412957  1
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  1
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  1
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  1
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  1
2014 Jayasekara PS, Jacobson KA. Rapid synthesis of alkoxyamine hydrochloride derivatives from alkyl bromide and N,N'-di-tert-butoxycarbonylhydroxylamine ((Boc)2NOH). Synthetic Communications. 44: 2344-2347. PMID 25368434 DOI: 10.1080/00397911.2014.895014  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  0.01
2013 Alexander SP, Benson HE, Faccenda E, Pawson AJ, Sharman JL, McGrath JC, Catterall WA, Spedding M, Peters JA, Harmar AJ, Abul-Hasn N, Anderson CM, Anderson CM, Araiksinen MS, ... ... Jacobson KA, et al. The Concise Guide to PHARMACOLOGY 2013/14: overview. British Journal of Pharmacology. 170: 1449-58. PMID 24528237 DOI: 10.1111/bph.12444  0.04
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  1
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  1
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  1
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  1
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  1
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  1
2013 Abbracchio MP, Boeynaems JM, Cattaneo M, Di Virgilio F, Illes P, Inoue K, Jacobson KA, Teresa Miras-Portugal M, Ralevic V, Robson SC, Verkhratsky A, Zimmermann H. Reply to: 'the discovery of a new class of synaptic transmitters in smooth muscle fifty years ago and amelioration of coronary artery thrombosis'. Acta Physiologica (Oxford, England). 208: 139-40. PMID 23551801 DOI: 10.1111/apha.12101  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2010 Gorman MW, Rooke GA, Savage MV, Jayasekara MP, Jacobson KA, Feigl EO. Adenine nucleotide control of coronary blood flow during exercise. American Journal of Physiology. Heart and Circulatory Physiology. 299: H1981-9. PMID 20852039 DOI: 10.1152/ajpheart.00611.2010  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2010 Avni I, Garzozi HJ, Barequet IS, Segev F, Varssano D, Sartani G, Chetrit N, Bakshi E, Zadok D, Tomkins O, Litvin G, Jacobson KA, Fishman S, Harpaz Z, Farbstein M, et al. Treatment of dry eye syndrome with orally administered CF101: data from a phase 2 clinical trial. Ophthalmology. 117: 1287-93. PMID 20304499 DOI: 10.1016/j.ophtha.2009.11.029  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2009 Shainberg A, Yitzhaki S, Golan O, Jacobson KA, Hochhauser E. Involvement of UTP in protection of cardiomyocytes from hypoxic stress. Canadian Journal of Physiology and Pharmacology. 87: 287-99. PMID 19370082 DOI: 10.1139/Y09-010  1
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  1
2009 Diaz JC, Simakova O, Jacobson KA, Arispe N, Pollard HB. Small molecule blockers of the Alzheimer Abeta calcium channel potently protect neurons from Abeta cytotoxicity. Proceedings of the National Academy of Sciences of the United States of America. 106: 3348-53. PMID 19204293 DOI: 10.1073/pnas.0813355106  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2009 Jacobson KA, Kirk KL. John W. Daly - An appreciation Heterocycles. 79: 61-71. DOI: 10.3987/COM-08-S(D)Memoire-1  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2008 Matot I, Einav S, Weiniger CF, Pearl RG, Abramovitch R, Joshi BV, Jacobson KA. Lung injury after in vivo reperfusion: outcome at 27 hours after reperfusion. Anesthesiology. 109: 269-78. PMID 18648236 DOI: 10.1097/ALN.0b013e31817f5b90  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  0.01
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2006 Yitzhaki S, Shainberg A, Cheporko Y, Vidne BA, Sagie A, Jacobson KA, Hochhauser E. Uridine-5'-triphosphate (UTP) reduces infarct size and improves rat heart function after myocardial infarct. Biochemical Pharmacology. 72: 949-55. PMID 16939682 DOI: 10.1016/j.bcp.2006.07.019  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2006 Jacobson KA, Gao ZG. Adenosine receptors as therapeutic targets. Nature Reviews. Drug Discovery. 5: 247-64. PMID 16518376 DOI: 10.1038/nrd1983  0.16
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2005 Joshi BV, Jacobson KA. Purine derivatives as ligands for A3 adenosine receptors. Current Topics in Medicinal Chemistry. 5: 1275-95. PMID 16305531  1
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  1
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  1
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  1
2005 Berk B, Akgün H, Erol K, Sirmagül B, Gao ZG, Jacobson KA. New 8-substituted xanthiene derivatives as potent bronchodilators. Farmaco (Società Chimica Italiana : 1989). 60: 974-80. PMID 16243321 DOI: 10.1016/j.farmac.2005.08.011  1
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  1
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  1
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  1
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  1
2005 Tchilibon S, Zhang J, Yang Q, Eidelman O, Kim H, Caohuy H, Jacobson KA, Pollard BS, Pollard HB. Amphiphilic pyridinium salts block TNF alpha/NF kappa B signaling and constitutive hypersecretion of interleukin-8 (IL-8) from cystic fibrosis lung epithelial cells. Biochemical Pharmacology. 70: 381-93. PMID 15963954 DOI: 10.1016/j.bcp.2005.05.002  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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. PflüGers Archiv : European Journal of Physiology. 449: 66-75. PMID 15235914 DOI: 10.1007/s00424-004-1293-2  1
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  1
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  1
2004 Srivastava M, Eidelman O, Zhang J, Paweletz C, Caohuy H, Yang Q, Jacobson KA, Heldman E, Huang W, Jozwik C, Pollard BS, Pollard HB. Digitoxin mimics gene therapy with CFTR and suppresses hypersecretion of IL-8 from cystic fibrosis lung epithelial cells. Proceedings of the National Academy of Sciences of the United States of America. 101: 7693-8. PMID 15136726 DOI: 10.1073/pnas.0402030101  1
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  1
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  1
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  1
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  1
2004 Gao ZG, Jacobson KA. Partial agonists for A(3) adenosine receptors. Current Topics in Medicinal Chemistry. 4: 855-62. PMID 15078216  1
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  1
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  1
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  1
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  1
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+  1
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  1
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  1
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  1
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  1
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  1
2003 Jacobson KA. Molecular recognition in P2 nucleotide receptors. Nucleic Acids Research. Supplement (2001). 3-4. PMID 14510351  0.01
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
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  1
2002 Maconi A, Pastorin G, Da Ros T, Spalluto G, Gao ZG, Jacobson KA, Baraldi PG, Cacciari B, Varani K, Moro S, Borea PA. Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist. Journal of Medicinal Chemistry. 45: 3579-82. PMID 12166930  1
2002 Müller CE, Thorand M, Qurishi R, Diekmann M, Jacobson KA, Padgett WL, Daly JW. Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists. Journal of Medicinal Chemistry. 45: 3440-50. PMID 12139454 DOI: 10.1021/jm011093d  1
2002 Jacobson KA, Moro S, Manthey JA, West PL, Ji XD. Interactions of flavones and other phytochemicals with adenosine receptors. Advances in Experimental Medicine and Biology. 505: 163-71. PMID 12083460  1
2002 Kim SA, Marshall MA, Melman N, Kim HS, Müller CE, Linden J, Jacobson KA. Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. Journal of Medicinal Chemistry. 45: 2131-8. PMID 12014951 DOI: 10.1021/jm0104318  1
2002 Ravi RG, Kim HS, Servos J, Zimmermann H, Lee K, Maddileti S, Boyer JL, Harden TK, Jacobson KA. Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists. Journal of Medicinal Chemistry. 45: 2090-100. PMID 11985476 DOI: 10.1021/jm010538v  1
2002 Boyer JL, Adams M, Ghana Ravi R, Jacobson KA, Harden TK. 2-chloro N 6-methyl-(N)-methanocarba-2′-deoxyadenosine-3′, 5′-bisphosphate is a selective high affinity P2Y 1 receptor antagonist British Journal of Pharmacology. 135: 2004-2010. PMID 11959804  1
2002 Kim SG, Ravi G, Hoffmann C, Jung YJ, Kim M, Chen A, Jacobson KA. p53-Independent induction of Fas and apoptosis in leukemic cells by an adenosine derivative, Cl-IB-MECA. Biochemical Pharmacology. 63: 871-80. PMID 11911839  1
2002 Kim HS, Ravi RG, Marquez VE, Maddileti S, Wihlborg AK, Erlinge D, Malmsjö M, Boyer JL, Harden TK, Jacobson KA. Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors. Journal of Medicinal Chemistry. 45: 208-18. PMID 11754592 DOI: 10.1021/jm010369e  1
2001 Brown SG, Kim YC, Kim SA, Jacobson KA, Burnstock G, King BF. Actions of a Series of PPADS Analogs at P2X1 and P2X3 Receptors. Drug Development Research. 53: 281-291. PMID 27134334 DOI: 10.1002/ddr.1197  1
2001 Pollard HB, Eidelman O, Jacobson KA, Srivastava M. Pharmacogenomics of cystic fibrosis. Molecular Interventions. 1: 54-63. PMID 14993338  1
2001 Jacobson KA, Ravi RG, Nandanan E, Kim HS, Moro S, Kim YC, Lee K, Barak D, Marquez VE, Ji XD. Ribose modified nucleosides and nucleotides as ligands for purine receptors. Nucleosides, Nucleotides & Nucleic Acids. 20: 333-41. PMID 11563046 DOI: 10.1081/NCN-100002305  1
2001 Kim HS, Barak D, Harden TK, Boyer JL, Jacobson KA. Acyclic and cyclopropyl analogues of adenosine bisphosphate antagonists of the P2Y1 receptor: structure-activity relationships and receptor docking. Journal of Medicinal Chemistry. 44: 3092-108. PMID 11543678 DOI: 10.1021/jm010082h  1
2001 Ravi G, Lee K, Ji X, Kim HS, Soltysiak KA, Marquez VE, Jacobson KA. Synthesis and purine receptor affinity of 6-oxopurine nucleosides and nucleotides containing (N)-methanocarba-pseudoribose rings. Bioorganic & Medicinal Chemistry Letters. 11: 2295-300. PMID 11527718  1
2001 Baraldi PG, Cacciari B, Moro S, Romagnoli R, Ji Xd, Jacobson KA, Gessi S, Borea PA, Spalluto G. Fluorosulfonyl- and bis-(beta-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies. Journal of Medicinal Chemistry. 44: 2735-42. PMID 11495585  1
2001 Kim YC, Brown SG, Harden TK, Boyer JL, Dubyak G, King BF, Burnstock G, Jacobson KA. Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors. Journal of Medicinal Chemistry. 44: 340-9. PMID 11462975 DOI: 10.1021/jm9904203  1
2001 Jacobson KA, Moro S, Hoffmann C, Kim YC, Kim HS, Ravi RG, Harden TK, Boyer JL. Structurally related nucleotides as selective agonists and antagonists at P2Y1 receptors. Farmaco (Società Chimica Italiana : 1989). 56: 71-5. PMID 11347970 DOI: 10.1016/S0014-827X(01)01023-0  1
2001 Ji X, Kim YC, Ahern DG, Linden J, Jacobson KA. [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochemical Pharmacology. 61: 657-63. PMID 11266650  1
2000 Hoffmann C, Heine P, Pradel G, Kim YC, Jacobson KA, Zimmermann H. Inhibition of Ecto-Apyrase and Ecto-ATPase by Pyridoxal Phosphate-Related Compounds. Drug Development Research. 51: 151-158. PMID 27134333 DOI: 10.1002/1098-2299(200011)51:3<153::AID-DDR3>3.0.CO;2-X  1
2000 Brown SG, King BF, Kim YC, Jang SY, Burnstock G, Jacobson KA. Activity of Novel Adenine Nucleotide Derivatives as Agonists and Antagonists at Recombinant Rat P2X Receptors. Drug Development Research. 49: 253-259. PMID 22791931 DOI: 10.1002/1098-2299(200004)49:4<253::AID-DDR4>3.0.CO;2-1  1
2000 Jacobson KA, Kim YC, King BF. In search of selective P2 receptor ligands: interaction of dihydropyridine derivatives at recombinant rat P2X(2) receptors. Journal of the Autonomic Nervous System. 81: 152-7. PMID 10869714 DOI: 10.1016/S0165-1838(00)00128-4  1
2000 Jiang X, Lim LY, Daly JW, Li AH, Jacobson KA, Roberge M. Structure-activity relationships for G2 checkpoint inhibition by caffeine analogs. International Journal of Oncology. 16: 971-8. PMID 10762633  1
2000 Kim YC, Ji X, Melman N, Linden J, Jacobson KA. Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. Journal of Medicinal Chemistry. 43: 1165-72. PMID 10737749  1
2000 Brambilla R, Cattabeni F, Ceruti S, Barbieri D, Franceschi C, Kim YC, Jacobson KA, Klotz KN, Lohse MJ, Abbracchio MP. Activation of the A3 adenosine receptor affects cell cycle progression and cell growth. Naunyn-Schmiedeberg's Archives of Pharmacology. 361: 225-34. PMID 10731034 DOI: 10.1007/s002109900186  1
2000 Nandanan E, Jang SY, Moro S, Kim HO, Siddiqui MA, Russ P, Marquez VE, Busson R, Herdewijn P, Harden TK, Boyer JL, Jacobson KA. Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands. Journal of Medicinal Chemistry. 43: 829-42. PMID 10715151 DOI: 10.1021/jm990249v  1
2000 Kim YC, Gallo-Rodriguez C, Jang SY, Nandanan E, Adams M, Harden TK, Boyer JL, Jacobson KA. Acyclic analogues of deoxyadenosine 3',5'-bisphosphates as P2Y(1) receptor antagonists. Journal of Medicinal Chemistry. 43: 746-55. PMID 10691699 DOI: 10.1021/jm9905211  1
1999 Li AH, Ji XD, Kim HS, Melman N, Jacobson KA. Pyran Template Approach to the Design of Novel A3 Adenosine Receptor Antagonists. Drug Development Research. 48: 171-177. PMID 27182099 DOI: 10.1002/(SICI)1098-2299(199912)48:4<171::AID-DDR4>3.0.CO;2-5  1
1999 Jacobson KA, Hoffmann C, Cattabeni F, Abbracchio MP. Adenosine-induced cell death: evidence for receptor-mediated signalling. Apoptosis : An International Journal On Programmed Cell Death. 4: 197-211. PMID 14634282  1
1999 Jacobson KA, Hoffmann C, Kim YC, Camaioni E, Nandanan E, Jang SY, Guo DP, Ji XD, von Kügelgen I, Moro S, Ziganshin AU, Rychkov A, King BF, Brown SG, Wildman SS, et al. Molecular recognition in P2 receptors: ligand development aided by molecular modeling and mutagenesis. Progress in Brain Research. 120: 119-32. PMID 10550992  1
1999 Jiang J, Li AH, Jang SY, Chang L, Melman N, Moro S, Ji X, Lobkovsky EB, Clardy JC, Jacobson KA. Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists. Journal of Medicinal Chemistry. 42: 3055-65. PMID 10447949 DOI: 10.1021/jm980688e  1
1999 Fischer B, Yefidoff R, Major DT, Rutman-Halili I, Shneyvays V, Zinman T, Jacobson KA, Shainberg A. Characterization of "mini-nucleotides" as P2X receptor agonists in rat cardiomyocyte cultures. An integrated synthetic, biochemical, and theoretical study. Journal of Medicinal Chemistry. 42: 2685-96. PMID 10411489 DOI: 10.1021/jm990085i  1
1999 Hoffmann C, Moro S, Nicholas RA, Harden TK, Jacobson KA. The role of amino acids in extracellular loops of the human P2Y1 receptor in surface expression and activation processes. The Journal of Biological Chemistry. 274: 14639-47. PMID 10329657 DOI: 10.1074/jbc.274.21.14639  1
1999 Nandanan E, Camaioni E, Jang SY, Kim YC, Cristalli G, Herdewijn P, Secrist JA, Tiwari KN, Mohanram A, Harden TK, Boyer JL, Jacobson KA. Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists. Journal of Medicinal Chemistry. 42: 1625-38. PMID 10229631 DOI: 10.1021/jm980657j  1
1999 Moro S, Hoffmann C, Jacobson KA. Role of the extracellular loops of G protein-coupled receptors in ligand recognition: a molecular modeling study of the human P2Y1 receptor. Biochemistry. 38: 3498-507. PMID 10090736 DOI: 10.1021/bi982369v  1
1999 Li AH, Moro S, Forsyth N, Melman N, Ji XD, Jacobson KA. Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists. Journal of Medicinal Chemistry. 42: 706-21. PMID 10052977 DOI: 10.1021/jm980550w  1
1998 Park KS, Hoffmann C, Kim HO, Padgett WL, Daly JW, Brambilla R, Motta C, Abbracchio MP, Jacobson KA. Activation and Desensitization of Rat A3-Adenosine Receptors by Selective Adenosine Derivatives and Xanthine-7-Ribosides. Drug Development Research. 44: 97-105. PMID 23487508 DOI: 10.1002/(SICI)1098-2299(199806/07)44:2/3<97::AID-DDR7>3.0.CO;2-5  1
1998 Kim YC, Camaioni E, Ziganshin AU, Ji XD, King BF, Wildman SS, Rychkov A, Yoburn J, Kim H, Mohanram A, Harden TK, Boyer JL, Burnstock G, Jacobson KA. Synthesis and Structure-Activity Relationships of Pyridoxal-6-arylazo-5'-phosphate and Phosphonate Derivatives as P2 Receptor Antagonists. Drug Development Research. 45: 52-66. PMID 22922976 DOI: 10.1002/(SICI)1098-2299(199810)45:2<52::AID-DDR2>3.0.CO;2-V  1
1998 Moro S, Li AH, Jacobson KA. Molecular modeling studies of human A3 adenosine antagonists: structural homology and receptor docking. Journal of Chemical Information and Computer Sciences. 38: 1239-48. PMID 9845970  1
1998 Li AH, Moro S, Melman N, Ji XD, Jacobson KA. Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists. Journal of Medicinal Chemistry. 41: 3186-201. PMID 9703464 DOI: 10.1021/jm980093j  1
1998 Kim YC, de Zwart M, Chang L, Moro S, von Frijtag Drabbe Künzel JK, Melman N, IJzerman AP, Jacobson KA. Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. Journal of Medicinal Chemistry. 41: 2835-45. PMID 9667972 DOI: 10.1021/jm980094b  1
1998 Jacobson KA, Kim YC, Wildman SS, Mohanram A, Harden TK, Boyer JL, King BF, Burnstock G. A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors. Journal of Medicinal Chemistry. 41: 2201-6. PMID 9632352 DOI: 10.1021/jm980183o  1
1998 Boyer JL, Mohanram A, Camaioni E, Jacobson KA, Harden TK. Competitive and selective antagonism of P2Y1 receptors by N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate. British Journal of Pharmacology. 124: 1-3. PMID 9630335 DOI: 10.1038/sj.bjp.0701837  1
1998 Moro S, Guo D, Camaioni E, Boyer JL, Harden TK, Jacobson KA. Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. Journal of Medicinal Chemistry. 41: 1456-66. PMID 9554879 DOI: 10.1021/jm970684u  1
1998 Camaioni E, Boyer JL, Mohanram A, Harden TK, Jacobson KA. Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors. Journal of Medicinal Chemistry. 41: 183-90. PMID 9457242 DOI: 10.1021/jm970433l  1
1998 Moro S, van Rhee AM, Sanders LH, Jacobson KA. Flavonoid derivatives as adenosine receptor antagonists: a comparison of the hypothetical receptor binding site based on a comparative molecular field analysis model. Journal of Medicinal Chemistry. 41: 46-52. PMID 9438021 DOI: 10.1021/jm970446z  1
1997 Daly JW, Shi D, Padgett WL, Ji XD, Jacobson KA. Riboflavin: Inhibitory Effects on Receptors, G-Proteins, and Adenylate Cyclase. Drug Development Research. 42: 98-108. PMID 22772360 DOI: 10.1002/(SICI)1098-2299(199710)42:2<98::AID-DDR6>3.0.CO;2-K  1
1997 Jacobson KA, Park KS, Jiang JL, Kim YC, Olah ME, Stiles GL, Ji XD. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 36: 1157-65. PMID 9364471  1
1997 Jiang Q, Guo D, Lee BX, Van Rhee AM, Kim YC, Nicholas RA, Schachter JB, Harden TK, Jacobson KA. A mutational analysis of residues essential for ligand recognition at the human P2Y1 receptor. Molecular Pharmacology. 52: 499-507. PMID 9281613  1
1997 Jiang J, van Rhee AM, Chang L, Patchornik A, Ji XD, Evans P, Melman N, Jacobson KA. Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists. Journal of Medicinal Chemistry. 40: 2596-608. PMID 9258367 DOI: 10.1021/jm970091j  1
1997 Cohen BE, Lee G, Jacobson KA, Kim YC, Huang Z, Sorscher EJ, Pollard HB. 8-cyclopentyl-1,3-dipropylxanthine and other xanthines differentially bind to the wild-type and delta F508 first nucleotide binding fold (NBF-1) domains of the cystic fibrosis transmembrane conductance regulator. Biochemistry. 36: 6455-61. PMID 9174362 DOI: 10.1021/bi970150v  1
1997 Fredholm BB, Abbracchio MP, Burnstock G, Dubyak GR, Harden TK, Jacobson KA, Schwabe U, Williams M. Towards a revised nomenclature for P1 and P2 receptors. Trends in Pharmacological Sciences. 18: 79-82. PMID 9133776 DOI: 10.1016/S0165-6147(96)01038-3  1
1997 Yao Y, Sei Y, Abbracchio MP, Jiang JL, Kim YC, Jacobson KA. Adenosine A3 receptor agonists protect HL-60 and U-937 cells from apoptosis induced by A3 antagonists. Biochemical and Biophysical Research Communications. 232: 317-22. PMID 9125172 DOI: 10.1006/bbrc.1997.6290  1
1996 Siddiqi SM, Ji XD, Melman N, Olah ME, Jain R, Evans P, Glashofer M, Padgett WL, Cohen LA, Daly JW, Stiles GL, Jacobson KA. A SURVEY OF NONXANTHINE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS. Nucleosides & Nucleotides. 15: 693-717. PMID 27043138 DOI: 10.1080/07328319608002416  1
1996 Shin Y, Daly JW, Jacobson KA. Activation of Phosphoinositide Breakdown and Elevation of Intracellular Calcium in a Rat RBL-2H3 Mast Cell Line by Adenosine Analogs: Involvement of A(3)-Adenosine Receptors? Drug Development Research. 39: 36-46. PMID 23087534  1
1996 Jacobson KA, von Lubitz DK, Daly JW, Fredholm BB. Adenosine receptor ligands: differences with acute versus chronic treatment. Trends in Pharmacological Sciences. 17: 108-13. PMID 8936347 DOI: 10.1016/0165-6147(96)10002-X  1
1996 Boyer JL, Siddiqi S, Fischer B, Romero-Avila T, Jacobson KA, Harden TK. Identification of potent P2Y-purinoceptor agonists that are derivatives of adenosine 5'-monophosphate. British Journal of Pharmacology. 118: 1959-64. PMID 8864529  1
1996 Kim YC, Ji XD, Jacobson KA. Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. Journal of Medicinal Chemistry. 39: 4142-8. PMID 8863790 DOI: 10.1021/jm960482i  1
1996 van Rhee AM, Siddiqi SM, Melman N, Shi D, Padgett WL, Daly JW, Jacobson KA. Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists. Journal of Medicinal Chemistry. 39: 398-406. PMID 8558508 DOI: 10.1021/jm9504823  1
1995 Jacobson KA, Fischer B, van Rhee AM. Molecular probes for muscarinic receptors: functionalized congeners of selective muscarinic antagonists. Life Sciences. 56: 823-30. PMID 10188781  1
1995 Van Rhee AM, Fischer B, Van Galen PJ, Jacobson KA. Modelling the P2Y purinoceptor using rhodopsin as template. Drug Design and Discovery. 13: 133-54. PMID 8872457  1
1995 Boyer JL, O'Tuel JW, Fischer B, Jacobson KA, Harden TK. Potent agonist action of 2-thioether derivatives of adenine nucleotides at adenylyl cyclase-linked P2Y-purinoceptors. British Journal of Pharmacology. 116: 2611-6. PMID 8590978  1
1995 Jacobson KA, Fischer B, Ji XD. "Cleavable trifunctional" approach to receptor affinity labeling: chemical regeneration of binding to A1-adenosine receptors. Bioconjugate Chemistry. 6: 255-63. PMID 7632796  1
1995 Von Lubitz DK, Kim J, Beenhakker M, Carter MF, Lin RC, Meshulam Y, Daly JW, Shi D, Zhou LM, Jacobson KA. Chronic NMDA receptor stimulation: therapeutic implications of its effect on adenosine A1 receptors. European Journal of Pharmacology. 283: 185-92. PMID 7498308 DOI: 10.1016/0014-2999(95)00338-L  1
1994 Daly JW, Shi D, Nikodijevic O, Jacobson KA. The role of adenosine receptors in the central action of caffeine. Pharmacopsychoecologia. 7: 201-213. PMID 25821357  1
1994 Burnstock G, Fischer B, Hoyle CH, Maillard M, Ziganshin AU, Brizzolara AL, von Isakovics A, Boyer JL, Harden TK, Jacobson KA. Structure Activity Relationships for Derivatives of Adenosine-5'-Triphosphate as Agonists at P(2) Purinoceptors: Heterogeneity Within P(2X) and P(2Y) Subtypes. Drug Development Research. 31: 206-219. PMID 22962511 DOI: 10.1002/ddr.430310308  1
1994 Bo X, Fischer B, Maillard M, Jacobson KA, Burnstock G. Comparative studies on the affinities of ATP derivatives for P2x-purinoceptors in rat urinary bladder. British Journal of Pharmacology. 112: 1151-9. PMID 7952876  1
1994 Fredholm BB, Abbracchio MP, Burnstock G, Daly JW, Harden TK, Jacobson KA, Leff P, Williams M. Nomenclature and classification of purinoceptors. Pharmacological Reviews. 46: 143-56. PMID 7938164  1
1994 Boyer JL, Zohn IE, Jacobson KA, Harden TK. Differential effects of P2-purinoceptor antagonists on phospholipase C- and adenylyl cyclase-coupled P2Y-purinoceptors. British Journal of Pharmacology. 113: 614-20. PMID 7834215  1
1994 Shi D, Nikodijević O, Jacobson KA, Daly JW. Effects of chronic caffeine on adenosine, dopamine and acetylcholine systems in mice. Archives Internationales De Pharmacodynamie Et De ThéRapie. 328: 261-87. PMID 7625882  1
1993 Jacobson KA, Gallo-Rodriguez C, Melman N, Fischer B, Maillard M, van Bergen A, van Galen PJ, Karton Y. Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists. Journal of Medicinal Chemistry. 36: 1333-42. PMID 8496902  1
1993 Jacobson KA, Nikodijević O, Padgett WL, Gallo-Rodriguez C, Maillard M, Daly JW. 8-(3-Chlorostyryl)caffeine (CSC) is a selective A2-adenosine antagonist in vitro and in vivo. Febs Letters. 323: 141-4. PMID 8495727 DOI: 10.1016/0014-5793(93)81466-D  1
1993 Jacobson KA, Shi D, Gallo-Rodriguez C, Manning M, Müller C, Daly JW, Neumeyer JL, Kiriasis L, Pfleiderer W. Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors. Journal of Medicinal Chemistry. 36: 2639-44. PMID 8410976  1
1993 Jacobson KA, Nikodijević O, Shi D, Gallo-Rodriguez C, Olah ME, Stiles GL, Daly JW. A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. Febs Letters. 336: 57-60. PMID 8262217 DOI: 10.1016/0014-5793(93)81608-3  1
1993 Fischer B, Boyer JL, Hoyle CH, Ziganshin AU, Brizzolara AL, Knight GE, Zimmet J, Burnstock G, Harden TK, Jacobson KA. Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate. Journal of Medicinal Chemistry. 36: 3937-46. PMID 8254622  1
1993 Shi D, Nikodijević O, Jacobson KA, Daly JW. Chronic caffeine alters the density of adenosine, adrenergic, cholinergic, GABA, and serotonin receptors and calcium channels in mouse brain. Cellular and Molecular Neurobiology. 13: 247-61. PMID 8242688 DOI: 10.1007/BF00733753  1
1993 Nikodijević O, Jacobson KA, Daly JW. Locomotor activity in mice during chronic treatment with caffeine and withdrawal. Pharmacology, Biochemistry, and Behavior. 44: 199-216. PMID 7679219 DOI: 10.1016/0091-3057(93)90299-9  1
1992 Hide I, Padgett WL, Jacobson KA, Daly JW. A2A adenosine receptors from rat striatum and rat pheochromocytoma PC12 cells: characterization with radioligand binding and by activation of adenylate cyclase. Molecular Pharmacology. 41: 352-9. PMID 1311411  1
1991 Nikodijević O, Sarges R, Daly JW, Jacobson KA. Behavioral effects of A1- and A2-selective adenosine agonists and antagonists: evidence for synergism and antagonism. The Journal of Pharmacology and Experimental Therapeutics. 259: 286-94. PMID 1920121  1
1990 Nikodijević O, Daly JW, Jacobson KA. Characterization of the locomotor depression produced by an A2-selective adenosine agonist. Febs Letters. 261: 67-70. PMID 2307237  1
1989 Morgan PF, Deckert J, Jacobson KA, Marangos PJ, Daly JW. Potent convulsant actions of the adenosine receptor antagonist, xanthine amine congener (XAC). Life Sciences. 45: 719-28. PMID 2779359 DOI: 10.1016/0024-3205(89)90091-X  1
1989 Jacobson KA, Kiriasis L, Barone S, Bradbury BJ, Kammula U, Campagne JM, Secunda S, Daly JW, Neumeyer JL, Pfleiderer W. Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors. Journal of Medicinal Chemistry. 32: 1873-9. PMID 2754711  1
1988 Deckert J, Morgan PF, Bisserbe JC, Jacobson KA, Kirk KL, Daly JW, Marangos PJ. Autoradiographic localization of mouse brain adenosine receptors with an antagonist ([3H]xanthine amine congener) ligand probe. Neuroscience Letters. 86: 121-6. PMID 3368115 DOI: 10.1016/0304-3940(88)90557-5  1
1988 Jacobson KA, de la Cruz R, Schulick R, Kiriasis L, Padgett W, Pfleiderer W, Kirk KL, Neumeyer JL, Daly JW. 8-Substituted xanthines as antagonists at A1- and A2-adenosine receptors. Biochemical Pharmacology. 37: 3653-61. PMID 3178879 DOI: 10.1016/0006-2952(88)90398-X  1
1988 Daly JW, Hong O, Padgett WL, Shamim MT, Jacobson KA, Ukena D. Non-xanthine heterocycles: activity as antagonists of A1- and A2-adenosine receptors. Biochemical Pharmacology. 37: 655-64. PMID 2829919 DOI: 10.1016/0006-2952(88)90139-6  1
1987 Jacobson KA, Zimmet J, Schulick R, Barone S, Daly JW, Kirk KL. Adenosine analogs with covalently attached lipids have enhanced potency at A1-adenosine receptors. Febs Letters. 225: 97-102. PMID 3691809  1
1987 Evoniuk G, Jacobson KA, Shamim MT, Daly JW, Wurtman RJ. A1- and A2-selective adenosine antagonists: in vivo characterization of cardiovascular effects. The Journal of Pharmacology and Experimental Therapeutics. 242: 882-7. PMID 3656117  1
1987 Jacobson KA, Ukena D, Padgett W, Kirk KL, Daly JW. Molecular probes for extracellular adenosine receptors. Biochemical Pharmacology. 36: 1697-707. PMID 3036153  1
1987 Jacobson KA, Lipkowski AW, Moody TW, Padgett W, Pijl E, Kirk KL, Daly JW. Binary drugs: conjugates of purines and a peptide that bind to both adenosine and substance P receptors. Journal of Medicinal Chemistry. 30: 1529-32. PMID 2441057  1
1987 Fredholm BB, Jacobson KA, Jonzon B, Kirk KL, Li YO, Daly JW. Evidence that a novel 8-phenyl-substituted xanthine derivative is a cardioselective adenosine receptor antagonist in vivo. Journal of Cardiovascular Pharmacology. 9: 396-400. PMID 2438501  1
1983 Jacobson KA, Patchornik A. Visual methods for the nanomolar detection of electrophilic reagents. Journal of Biochemical and Biophysical Methods. 8: 213-22. PMID 6655200 DOI: 10.1016/0165-022X(83)90069-6  1
1983 Jacobson KA, Verlander MS, Rosenkranz RP, Melmon KL, Goodman M. Conjugates of catecholamines. III. Synthesis and characterization of monodisperse oligopeptides conjugates related to isoproterenol. International Journal of Peptide and Protein Research. 22: 284-304. PMID 6629645  1
1983 Verlander MS, Jacobson KA, Rosenkranz RP, Melmon KL, Goodman M. Some novel approaches to the design and synthesis of peptide-catecholamine conjugates. Biopolymers. 22: 531-45. PMID 6324920 DOI: 10.1002/bip.360220166  1
1983 Jacobson KA, Marr-Leisy D, Rosenkranz RP, Verlander MS, Melmon KL, Goodman M. Conjugates of catecholamines. 1. N-alkyl-functionalized carboxylic acid congeners and amides related to isoproterenol. Journal of Medicinal Chemistry. 26: 492-9. PMID 6300399  1
1983 Rosenkranz RP, Hoffman BB, Jacobson KA, Verlander MS, Klevans L, O'Donnell M, Goodman M, Melmon KL. Conjugates of catecholamines. II. In vitro and in vivo pharmacological activity of N-alkyl-functionalized carboxylic acid congeners and amides related to isoproterenol. Molecular Pharmacology. 24: 429-35. PMID 6138706  1
1983 Rosenkranz RP, Jacobson KA, Verlander MS, Klevans L, O'Donnell M, Goodman M, Melmon KL. Conjugates of catecholamines. IV. In vitro and in vivo pharmacological activity of monodisperse oligopeptide conjugates. The Journal of Pharmacology and Experimental Therapeutics. 227: 267-73. PMID 6138424  1
1983 Rosenkranz RP, Jacobson KA, Verlander MS, Goodman M, Melmon KL. Betamimetic activity of peptide catecholamine conjugates. Proceedings of the Western Pharmacology Society. 26: 381-5. PMID 6136983  1
1982 Rosenkranz RP, Jacobson KA, Goodman M, Verlander M, Melmon KL. In vitro and in vivo betamimetic activity of congeners of isoproterenol. Proceedings of the Western Pharmacology Society. 25: 19-23. PMID 6126881  1
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