Zhan-Guo Gao, M.D., Ph.D.


A selection of recent and significant publications can be viewed below.

Adenosine A2A receptor antagonists: from caffeine to selective non-xanthines.
Jacobson KA, Gao ZG, Matricon P, Eddy MT, Carlsson J.
Br J Pharmacol (2020 May 18) Abstract/Full Text
Allosteric Antagonism of the A2A Adenosine Receptor by a Series of Bitopic Ligands.
Gao ZG, Toti KS, Campbell R, Suresh RR, Yang H, Jacobson KA.
Cells (2020 May 12) 9. Abstract/Full Text
A2B Adenosine Receptor and Cancer.
Gao ZG, Jacobson KA.
Int J Mol Sci (2019 Oct 17) 20. Abstract/Full Text
Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development.
Jacobson KA, Tosh DK, Jain S, Gao ZG.
Front Cell Neurosci (2019) 13:124. Abstract/Full Text
Preclinical Evaluation of the First Adenosine A1 Receptor Partial Agonist Radioligand for Positron Emission Tomography Imaging.
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.
J Med Chem (2018 Nov 21) 61:9966-9975. Abstract/Full Text
Extrinsic Tryptophans as NMR Probes of Allosteric Coupling in Membrane Proteins: Application to the A2A Adenosine Receptor.
Eddy MT, Gao ZG, Mannes P, Patel N, Jacobson KA, Katritch V, Stevens RC, Wüthrich K.
J Am Chem Soc (2018 Jul 5) 140:8228-8235. Abstract/Full Text
A3 Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy.
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.
Med Res Rev (2018 Jul) 38:1031-1072. Abstract/Full Text
Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors.
Liu X, Gao ZG, Wu Y, Stevens RC, Jacobson KA, Zhao S.
Sci Rep (2018 May 24) 8:8084. Abstract/Full Text
On the G protein-coupling selectivity of the native A2B adenosine receptor.
Gao ZG, Inoue A, Jacobson KA.
Biochem Pharmacol (2018 May) 151:201-213. Abstract/Full Text
Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling.
White KL, Eddy MT, Gao ZG, Han GW, Lian T, Deary A, Patel N, Jacobson KA, Katritch V, Stevens RC.
Structure (2018 Feb 6) 26:259-269.e5. Abstract/Full Text
Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor.
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.
Cell (2018 Jan 11) 172:68-80.e12. Abstract/Full Text
Purinergic Signaling in Mast Cell Degranulation and Asthma.
Gao ZG, Jacobson KA.
Front Pharmacol (2017) 8:947. Abstract/Full Text
Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor.
Gao ZG, Jacobson KA.
Mol Pharmacol (2017 Nov) 92:613-626. Abstract/Full Text
On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin.
Gao ZG, Jacobson KA.
Biochem Pharmacol (2016 May 1) 107:59-66. Abstract/Full Text
Two disparate ligand-binding sites in the human P2Y1 receptor.
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, Stevens RC, Jacobson KA, Zhao Q, Wu B.
Nature (2015 Apr 16) 520:317-21. Abstract/Full Text
Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.
Gao ZG, Balasubramanian R, Kiselev E, Wei Q, Jacobson KA.
Biochem Pharmacol (2014 Aug 1) 90:297-306. Abstract/Full Text
Structure of the human P2Y12 receptor in complex with an antithrombotic drug.
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, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q.
Nature (2014 May 1) 509:115-8. Abstract/Full Text
Agonist-bound structure of the human P2Y12 receptor.
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, Stevens RC, Wu B, Zhao Q.
Nature (2014 May 1) 509:119-22. Abstract/Full Text
Allosteric modulation and functional selectivity of G protein-coupled receptors.
Gao ZG, Jacobson KA.
Drug Discov Today Technol (2013 Summer) 10:e237-43. Abstract/Full Text
A2B adenosine receptor blockade inhibits growth of prostate cancer cells.
Wei Q, Costanzi S, Balasubramanian R, Gao ZG, Jacobson KA.
Purinergic Signal (2013 Jun) 9:271-80. Abstract/Full Text
AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells.
Balasubramanian R, Maruoka H, Jayasekara PS, Gao ZG, Jacobson KA.
Biochem Pharmacol (2013 Apr 1) 85:991-8. Abstract/Full Text
The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells.
Gao ZG, Wei Q, Jayasekara MP, Jacobson KA.
Purinergic Signal (2013 Mar) 9:31-40. Abstract/Full Text
G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions.
Jacobson KA, Balasubramanian R, Deflorian F, Gao ZG.
Purinergic Signal (2012 Sep) 8:419-36. Abstract/Full Text
Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers.
Gao ZG, Verzijl D, Zweemer A, Ye K, Göblyös A, Ijzerman AP, Jacobson KA.
Biochem Pharmacol (2011 Sep 15) 82:658-68. Abstract/Full Text
Structure of an agonist-bound human A2A adenosine receptor.
Xu F, Wu H, Katritch V, Han GW, Jacobson KA, Gao ZG, Cherezov V, Stevens RC.
Science (2011 Apr 15) 332:322-7. Abstract/Full Text
Allosteric modulation of purine and pyrimidine receptors.
Jacobson KA, Gao ZG, Göblyös A, Ijzerman AP.
Adv Pharmacol (2011) 61:187-220. Abstract/Full Text
Dexamethasone enhances ATP-induced inflammatory responses in endothelial cells.
Ding Y, Gao ZG, Jacobson KA, Suffredini AF.
J Pharmacol Exp Ther (2010 Dec) 335:693-702. Abstract/Full Text
Structure-based discovery of A2A adenosine receptor ligands.
Carlsson J, Yoo L, Gao ZG, Irwin JJ, Shoichet BK, Jacobson KA.
J Med Chem (2010 May 13) 53:3748-55. Abstract/Full Text
UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation.
Gao ZG, Ding Y, Jacobson KA.
Biochem Pharmacol (2010 Mar 15) 79:873-9. Abstract/Full Text
Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000.
Gao ZG, Ye K, Göblyös A, Ijzerman AP, Jacobson KA.
BMC Pharmacol (2008 Dec 12) 8:20. Abstract/Full Text
Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways.
Gao ZG, Jacobson KA.
Pharmacol Res (2008 Apr) 57:303-11. Abstract/Full Text
Emerging adenosine receptor agonists.
Gao ZG, Jacobson KA.
Expert Opin Emerg Drugs (2007 Sep) 12:479-92. Abstract/Full Text
Neoceptors: reengineering GPCRs to recognize tailored ligands.
Jacobson KA, Gao ZG, Liang BT.
Trends Pharmacol Sci (2007 Mar) 28:111-6. Abstract/Full Text
Regulation of death and survival in astrocytes by ADP activating P2Y1 and P2Y12 receptors.
Mamedova LK, Gao ZG, Jacobson KA.
Biochem Pharmacol (2006 Oct 16) 72:1031-41. Abstract/Full Text
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
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.
J Med Chem (2006 May 4) 49:2689-702. Abstract/Full Text
Progress in the pursuit of therapeutic adenosine receptor antagonists.
Moro S, Gao ZG, Jacobson KA, Spalluto G.
Med Res Rev (2006 Mar) 26:131-59. Abstract/Full Text
Adenosine receptors as therapeutic targets.
Jacobson KA, Gao ZG.
Nat Rev Drug Discov (2006 Mar) 5:247-64. Abstract/Full Text
Keynote review: allosterism in membrane receptors.
Gao ZG, Jacobson KA.
Drug Discov Today (2006 Mar) 11:191-202. Abstract/Full Text
Activation of Th1 and Tc1 cell adenosine A2A receptors directly inhibits IL-2 secretion in vitro and IL-2-driven expansion in vivo.
Erdmann AA, Gao ZG, Jung U, Foley J, Borenstein T, Jacobson KA, Fowler DH.
Blood (2005 Jun 15) 105:4707-14. Abstract/Full Text
Allosteric modulation of the adenosine family of receptors.
Gao ZG, Kim SK, Ijzerman AP, Jacobson KA.
Mini Rev Med Chem (2005 Jun) 5:545-53. Abstract/Full Text
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.
Jacobson KA, Ohno M, Duong HT, Kim SK, Tchilibon S, Cesnek M, Holý A, Gao ZG.
Chem Biol (2005 Feb) 12:237-47. Abstract/Full Text
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
Costanzi S, Mamedova L, Gao ZG, Jacobson KA.
J Med Chem (2004 Oct 21) 47:5393-404. Abstract/Full Text
2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding.
Gao ZG, Mamedova L, Tchilibon S, Gross AS, Jacobson KA.
Biochem Pharmacol (2004 Jul 15) 68:231-7. Abstract/Full Text
Partial agonists for A(3) adenosine receptors.
Gao ZG, Jacobson KA.
Curr Top Med Chem (2004) 4:855-62. Abstract/Full Text
N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors.
Gao ZG, Blaustein JB, Gross AS, Melman N, Jacobson KA.
Biochem Pharmacol (2003 May 15) 65:1675-84. Abstract/Full Text
Identification of essential residues involved in the allosteric modulation of the human A(3) adenosine receptor.
Gao ZG, Kim SK, Gross AS, Chen A, Blaustein JB, Jacobson KA.
Mol Pharmacol (2003 May) 63:1021-31. Abstract/Full Text
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.
Gao ZG, Kim SK, Biadatti T, Chen W, Lee K, Barak D, Kim SG, Johnson CR, Jacobson KA.
J Med Chem (2002 Sep 26) 45:4471-84. Abstract/Full Text
Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives.
Gao ZG, Kim SG, Soltysiak KA, Melman N, IJzerman AP, Jacobson KA.
Mol Pharmacol (2002 Jul) 62:81-9. Abstract/Full Text
Identification by site-directed mutagenesis of residues involved in ligand recognition and activation of the human A3 adenosine receptor.
Gao ZG, Chen A, Barak D, Kim SK, Müller CE, Jacobson KA.
J Biol Chem (2002 May 24) 277:19056-63. Abstract/Full Text
Allosteric modulation of A(3) adenosine receptors by a series of 3-(2-pyridinyl)isoquinoline derivatives.
Gao ZG, Van Muijlwijk-Koezen JE, Chen A, Müller CE, Ijzerman AP, Jacobson KA.
Mol Pharmacol (2001 Nov) 60:1057-63. Abstract/Full Text