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Zhan-Guo Gao

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Qiang Wei; Ramachandran Balasubramanian; Stefano Costanzi; Zhan-Guo Gao; Kenneth A Jacobson
A2B adenosine receptor blockade inhibits growth of prostate cancer cells.
P Suresh Jayasekara; T Santhosh Kumar; Steven M Moss; Khai Phan; Dilip K Tosh; Guofeng Zhang; Joseph J Barchi; Zhan-Guo Gao; Kenneth A Jacobson
Modulation of G protein-coupled adenosine receptors by strategically functionalized agonists and antagonists immobilized on gold nanoparticles.
Ramachandran Balasubramanian; Zhan-Guo Gao; P Suresh Jayasekara; Hiroshi Maruoka; Kenneth A Jacobson
AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells.

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2013: Qiang Wei; Ramachandran Balasubramanian; Stefano Costanzi; Zhan-Guo Gao; Kenneth A Jacobson
A2B adenosine receptor blockade inhibits growth of prostate cancer cells.
Purinergic signalling 2013;9(2):271-80.
2013: P Suresh Jayasekara; T Santhosh Kumar; Steven M Moss; Khai Phan; Dilip K Tosh; Guofeng Zhang; Joseph J Barchi; Zhan-Guo Gao; Kenneth A Jacobson
Modulation of G protein-coupled adenosine receptors by strategically functionalized agonists and antagonists immobilized on gold nanoparticles.
Purinergic signalling 2013;9(2):183-98.
2013: Ramachandran Balasubramanian; Zhan-Guo Gao; P Suresh Jayasekara; Hiroshi Maruoka; Kenneth A Jacobson
AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells.
Biochemical pharmacology 2013;85(7):991-8.
2013: Zhan-Guo Gao; M P Suresh Jayasekara; Qiang Wei; Kenneth A Jacobson
The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells.
Purinergic signalling 2013;9(1):31-40.
2012: Dilip K Tosh; Francesca Deflorian; Zhan-Guo Gao; Xiaohui Jiang; Steven M Moss; Silvia Paoletta; Khai Phan; Kenneth Alan Jacobson
Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.
Journal of medicinal chemistry 2012;55(18):8075-90.
2012: Kenneth Alan Jacobson; Ramachandran Balasubramanian; Francesca Deflorian; Zhan-Guo Gao
G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions.
Purinergic signalling 2012;8(3):419-36.
2012: Eszter Kozma; T Santhosh Kumar; Stefano Moro; Silvia Paoletta; Khai Phan; Giampiero Spalluto; Ramachandran Balasubramanian; Stephanie Federico; Zhan-Guo Gao; Kenneth Alan Jacobson
Novel fluorescent antagonist as a molecular probe in A(3) adenosine receptor binding assays using flow cytometry.
Biochemical pharmacology 2012;83(11):1552-61.
2012: Dilip K Tosh; Tina C Wan; Khai Phan; John A Auchampach; Francesca Deflorian; Zhan-Guo Gao; Elizabeth Gizewski; Kenneth Alan Jacobson
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 2012;55(10):4847-60.
2012: Dilip K Tosh; Fei Xu; Khai Phan; Raymond C Stevens; Ruben Abagyan; Francesca Deflorian; Andrei A Gakh; Zhan-Guo Gao; Kenneth Alan Jacobson; Vsevolod Katritch
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.
Journal of medicinal chemistry 2012;55(9):4297-308.
2012: Dilip K Tosh; Qiang Wei; Lena S Yoo; Francesca Deflorian; Zhan-Guo Gao; Khai Phan; Kenneth Alan Jacobson
Click modification in the N6 region of A3 adenosine receptor-selective carbocyclic nucleosides for dendrimeric tethering that preserves pharmacophore recognition.
Bioconjugate chemistry 2012;23(2):232-47.
2011: Zhan-Guo Gao; Anikó Göblyös; Adriaan P IJzerman; Dennis Verzijl; Kai Ye; Annelien Zweemer; Kenneth Alan Jacobson
Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers.
Biochemical pharmacology 2011;82(6):658-68.
2011: Qiang Wei; Qiu-Zhen Liu; Stefano Costanzi; Zhan-Guo Gao; Kenneth Alan Jacobson
Activation of the P2Y1 receptor induces apoptosis and inhibits proliferation of prostate cancer cells.
Biochemical pharmacology 2011;82(4):418-25.
2011: Angela Kecskés; Dilip K Tosh; Qiang Wei; Zhan-Guo Gao; Kenneth Alan Jacobson
GPCR ligand dendrimer (GLiDe) conjugates: adenosine receptor interactions of a series of multivalent xanthine antagonists.
Bioconjugate chemistry 2011;22(6):1115-27.
2011: T Santhosh Kumar; Shilpi Mishra; Francesca Deflorian; Lena S Yoo; Khai Phan; Miklos Kecskés; Angela Szabo; Bidhan Shinkre; Zhan-Guo Gao; William Trenkle; Kenneth Alan Jacobson
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 2011;21(9):2740-5.
2011: Kenneth Alan Jacobson; Zhan-Guo Gao; Anikó Göblyös; Adriaan P IJzerman
Allosteric modulation of purine and pyrimidine receptors.
Advances in pharmacology (San Diego, Calif.) 2011;61():187-220.
2010: Zhan-Guo Gao; Yi Ding; Kenneth Alan Jacobson
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 2010;62(6):500-5.
2010: Bidhan A Shinkre; T Santhosh Kumar; Zhan-Guo Gao; Francesca Deflorian; Kenneth Alan Jacobson; William C Trenkle
Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.
Bioorganic & medicinal chemistry letters 2010;20(19):5690-4.
2010: Miklós Kecskés; T Santhosh Kumar; Lena Yoo; Zhan-Guo Gao; Kenneth Alan Jacobson
Novel Alexa Fluor-488 labeled antagonist of the A(2A) adenosine receptor: Application to a fluorescence polarization-based receptor binding assay.
Biochemical pharmacology 2010;80(4):506-11.
2010: Zhan-Guo Gao; Yi Ding; Kenneth Alan Jacobson
UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation.
Biochemical pharmacology 2010;79(6):873-9.
2010: Dilip K Tosh; Lena S Yoo; Moshe Chinn; Kunlun Hong; S Michael Kilbey; Matthew O Barrett; Ingrid P Fricks; T Kendall Harden; Zhan-Guo Gao; Kenneth Alan Jacobson
Polyamidoamine (PAMAM) dendrimer conjugates of "clickable" agonists of the A3 adenosine receptor and coactivation of the P2Y14 receptor by a tethered nucleotide.
Bioconjugate chemistry 2010;21(2):372-84.
2010: Dilip K Tosh; Moshe Chinn; Lena S Yoo; Dong Wook Kang; Hans Luecke; Zhan-Guo Gao; Kenneth Alan Jacobson
2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists.
Bioorganic & medicinal chemistry 2010;18(2):508-17.
2010: Arijit Das; Gangadhar J Sanjayan; Miklós Kecskés; Lena Yoo; Zhan-Guo Gao; Kenneth Alan Jacobson
Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2A adenosine receptor agonists.
Journal of nanobiotechnology 2010;8():11.
2009: Dilip K Tosh; Moshe Chinn; Andrei A Ivanov; Athena M Klutz; Zhan-Guo Gao; Kenneth Alan Jacobson
Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.
Journal of medicinal chemistry 2009;52(23):7580-92.
2009: Won Jun Choi; Hyuk Woo Lee; Hea Ok Kim; Moshe Chinn; Zhan-Guo Gao; Amit Patel; Kenneth Alan Jacobson; Hyung Ryong Moon; Young Hoon Jung; Lak Shin Jeong
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.
Bioorganic & medicinal chemistry 2009;17(23):8003-11.
2009: Yoonkyung Kim; Béatrice Hechler; Zhan-Guo Gao; Christian Gachet; Kenneth Alan Jacobson
PEGylated dendritic unimolecular micelles as versatile carriers for ligands of G protein-coupled receptors.
Bioconjugate chemistry 2009;20(10):1888-98.
2009: Shantanu Pal; Won Jun Choi; Seung Ah Choe; Cara L Heller; Zhan-Guo Gao; Moshe Chinn; Kenneth Alan Jacobson; Xiyan Hou; Sang Kook Lee; Hea Ok Kim; Lak Shin Jeong
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.
Bioorganic & medicinal chemistry 2009;17(10):3733-8.
2009: Yoonkyung Kim; Sonia De Castro; Zhan-Guo Gao; Adriaan P IJzerman; Kenneth Alan Jacobson
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 2009;52(7):2098-108.
2009: Yoonkyung Kim; Athena M Klutz; Béatrice Hechler; Zhan-Guo Gao; Christian Gachet; Kenneth Alan Jacobson
Application of the functionalized congener approach to dendrimer-based signaling agents acting through A(2A) adenosine receptors.
Purinergic signalling 2009;5(1):39-50.
2009: Zhan-Guo Gao; Bao Teng; Haitao Wu; Bhalchandra V Joshi; Gary L Griffiths; Kenneth Alan Jacobson
Synthesis and pharmacological characterization of [(125)I]MRS1898, a high-affinity, selective radioligand for the rat A(3) adenosine receptor.
Purinergic signalling 2009;5(1):31-7.
2009: Dale O Kiesewetter; Lixin Lang; Ying Ma; Abesh Kumar Bhattacharjee; Zhan-Guo Gao; Bhalchandra V Joshi; Artem Melman; Sonia De Castro; Kenneth Alan Jacobson
Synthesis and characterization of [76Br]-labeled high-affinity A3 adenosine receptor ligands for positron emission tomography.
Nuclear medicine and biology 2009;36(1):3-10.
2008: Lak Shin Jeong; Shantanu Pal; Seung Ah Choe; Won Jun Choi; Kenneth Alan Jacobson; Zhan-Guo Gao; Athena M Klutz; Xiyan Hou; Hea Ok Kim; Hyuk Woo Lee; Sang Kook Lee; Dilip K Tosh; Hyung Ryong Moon
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.
Journal of medicinal chemistry 2008;51(20):6609-13.
2008: Artem Melman; Ben Wang; Bhalchandra V Joshi; Zhan-Guo Gao; Sonia de Castro; Cara L Heller; Soo-Kyung Kim; Lak Shin Jeong; Kenneth Alan Jacobson
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.
Bioorganic & medicinal chemistry 2008;16(18):8546-56.
2008: Artem Melman; Zhan-Guo Gao; Deepmala Kumar; Tina C Wan; Elizabeth Gizewski; John A Auchampach; Kenneth Alan Jacobson
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
Bioorganic & medicinal chemistry letters 2008;18(9):2813-9.
2008: Andrei A Ivanov; Ben Wang; Athena M Klutz; Vincent L Chen; Zhan-Guo Gao; Kenneth Alan Jacobson
Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists.
Journal of medicinal chemistry 2008;51(7):2088-99.
2008: Zhan-Guo Gao; Kenneth Alan Jacobson
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 2008;57(4):303-11.
2008: Moon Woo Chun; Sung Wook Choi; Tae Kyung Kang; Won Jun Choi; Hea Ok Kim; Zhan-Guo Gao; Kenneth Alan Jacobson; Lak Shin Jeong
Synthesis of 3'-acetamidoadenosine derivatives as potential A3 adenosine receptor agonists.
Nucleosides, nucleotides & nucleic acids 2008;27(4):408-20.
2008: Zhan-Guo Gao; Béatrice Hechler; Pedro Besada; Christian Gachet; Kenneth Alan Jacobson
Caged agonist of P2Y1 and P2Y12 receptors for light-directed facilitation of platelet aggregation.
Biochemical pharmacology 2008;75(6):1341-7.
2008: Lak Shin Jeong; Hyuk Woo Lee; Hea Ok Kim; Dilip K Tosh; Shantanu Pal; Won Jun Choi; Zhan-Guo Gao; Amit R Patel; Wanda Williams; Kenneth Alan Jacobson; Hee-Doo Kim
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.
Bioorganic & medicinal chemistry letters 2008;18(5):1612-6.
2008: Zhan-Guo Gao; Kai Ye; Anikó Göblyös; Adriaan P IJzerman; Kenneth Alan Jacobson
Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000.
BMC pharmacology 2008;8():20.
2008: Athena M Klutz; Zhan-Guo Gao; John Lloyd; Asher Shainberg; Kenneth Alan Jacobson
Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates.
Journal of nanobiotechnology 2008;6():12.
2007: Zhan-Guo Gao; Kenneth Alan Jacobson
Emerging adenosine receptor agonists.
Expert opinion on emerging drugs 2007;12(3):479-92.
2007: Lak Shin Jeong; Seung Ah Choe; Prashantha Gunaga; Hea Ok Kim; Hyuk Woo Lee; Sang Kook Lee; Dilip K Tosh; Amit Patel; Krishnan K Palaniappan; Zhan-Guo Gao; Kenneth Alan Jacobson; Hyung Ryong Moon
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 2007;50(14):3159-62.
2007: Krishnan K Palaniappan; Zhan-Guo Gao; Andrei A Ivanov; Rebecca Greaves; Hayamitsu Adachi; Pedro Besada; Hea Ok Kim; Ae Yil Kim; Seung Ah Choe; Lak Shin Jeong; Kenneth Alan Jacobson
Probing the binding site of the A1 adenosine receptor reengineered for orthogonal recognition by tailored nucleosides.
Biochemistry 2007;46(25):7437-48.
2007: Hayamitsu Adachi; Krishnan K Palaniappan; Andrei A Ivanov; Nathaniel Bergman; Zhan-Guo Gao; Kenneth Alan Jacobson
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.
Journal of medicinal chemistry 2007;50(8):1810-27.
2007: Kenneth Alan Jacobson; Zhan-Guo Gao; Bruce T Liang
Neoceptors: reengineering GPCRs to recognize tailored ligands.
Trends in pharmacological sciences 2007;28(3):111-6.
2007: Lak Shin Jeong; Seung Ah Choe; Ae Yil Kim; Hea Ok Kim; Zhan-Guo Gao; Kenneth Alan Jacobson; Moon Woo Chun; Hyung Ryong Moon
Synthesis of N6-substituted 3'-ureidoadenosine derivatives as highly potent agonists at the mutant A3 adenosine receptor.
Nucleosides, nucleotides & nucleic acids 2007;26(6-7):717-9.
2007: Lak Shin Jeong; Hyuk Woo Lee; Hea Ok Kim; Ji Young Jung; Prashantha Gunaga; Sang Kook Lee; Eun-Jin Lee; Moon Woo Chun; Zhan-Guo Gao; Kenneth Alan Jacobson; Hyung Ryong Moon
Design, synthesis, and anti-tumor activity of 4'-thionucleosides as potent and selective agonists at the human A3 adenosine receptor.
Nucleosides, nucleotides & nucleic acids 2007;26(10-12):1565-8.
2007: Lak Shin Jeong; Prashantha Gunaga; Hea Ok Kim; Dilip K Tosh; Hyuk Woo Lee; Seung Ah Choe; Hyung Ryong Moon; Zhan-Guo Gao; Kenneth Alan Jacobson; Moon Woo Chun
Stereoselective synthesis of 1'-functionalized-4'-thionucleosides.
Nucleosides, nucleotides & nucleic acids 2007;26(8-9):1011-4.
2006: Liesbet Cosyn; Krishnan K Palaniappan; Soo-Kyung Kim; Heng T Duong; Zhan-Guo Gao; Kenneth Alan Jacobson; Serge Van Calenbergh
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.
Journal of medicinal chemistry 2006;49(25):7373-83.
2006: Soo-Kyung Kim; Zhan-Guo Gao; Lak Shin Jeong; Kenneth Alan Jacobson
Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor.
Journal of molecular graphics & modelling 2006;25(4):562-77.
2006: Liaman Mamedova; Zhan-Guo Gao; Kenneth Alan Jacobson
Regulation of death and survival in astrocytes by ADP activating P2Y1 and P2Y12 receptors.
Biochemical pharmacology 2006;72(8):1031-41.
2006: Lak Shin Jeong; Hyuk Woo Lee; Hea Ok Kim; Ji Young Jung; Zhan-Guo Gao; Heng T Duong; Srikar Rao; Kenneth Alan Jacobson; Dae Hong Shin; Jeong A Lee; Prashantha Gunaga; Sang Kook Lee; Dong Zhe Jin; Moon Woo Chun; Hyung Ryong Moon
Design, synthesis, and biological activity of N6-substituted-4'-thioadenosines at the human A3 adenosine receptor.
Bioorganic & medicinal chemistry 2006;14(14):4718-30.
2006: Zhan-Guo Gao; Heng T Duong; Lak Shin Jeong; Ae Yil Kim; Hea Ok Kim; Myong Jung Kim; Soo-Kyung Kim; Bruce T Liang; Liaman Mamedova; Tatiana Sonina; Serge Van Calenbergh; Philippe Van Rompaey; Kenneth Alan Jacobson
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
Journal of medicinal chemistry 2006;49(9):2689-702.
2006: Zhan-Guo Gao; Kenneth Alan Jacobson
Keynote review: allosterism in membrane receptors.
Drug discovery today 2006;11(5-6):191-202.
2006: Kenneth Alan Jacobson; Zhan-Guo Gao
Adenosine receptors as therapeutic targets.
Nature reviews. Drug discovery 2006;5(3):247-64.
2006: Liesbet Cosyn; Zhan-Guo Gao; Philippe Van Rompaey; Changrui Lu; Kenneth Alan Jacobson; Serge Van Calenbergh
Synthesis of hypermodified adenosine derivatives as selective adenosine A3 receptor ligands.
Bioorganic & medicinal chemistry 2006;14(5):1403-12.
2006: Kenneth Alan Jacobson; Stefano Costanzi; Andrei A Ivanov; Susanna Tchilibon; Pedro Besada; Zhan-Guo Gao; Savitri Maddileti; T Kendall Harden
Structure activity and molecular modeling analyses of ribose- and base-modified uridine 5'-triphosphate analogues at the human P2Y2 and P2Y4 receptors.
Biochemical pharmacology 2006;71(4):540-9.
2006: Zhan-Guo Gao; Bhalchandra V Joshi; Athena M Klutz; Soo-Kyung Kim; Hyuk Woo Lee; Hea Ok Kim; Lak Shin Jeong; Kenneth Alan Jacobson
Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety.
Bioorganic & medicinal chemistry letters 2006;16(3):596-601.
2006: Lak Shin Jeong; Hyuk Woo Lee; Kenneth Alan Jacobson; Hea Ok Kim; Dae Hong Shin; Jeong A Lee; Zhan-Guo Gao; Changrui Lu; Heng T Duong; Prashantha Gunaga; Sang Kook Lee; Dong Zhe Jin; Moon Woo Chun; Hyung Ryong Moon
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 2006;49(1):273-81.
2006: Kenneth Alan Jacobson; Stefano Costanzi; Soo-Kyung Kim; Eunjoo Roh; Bhalchandra V Joshi; Susanna Tchilibon; Heng T Duong; Zhan-Guo Gao
Action of nucleosides and nucleotides at 7 transmembrane-spanning receptors.
Nucleosides, nucleotides & nucleic acids 2006;25(12):1425-36.
2005: Kenneth Alan Jacobson; Zhan-Guo Gao; Susanna Tchilibon; Heng T Duong; Bhalchandra V Joshi; Dmitry Sonin; Bruce T Liang
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 2005;48(26):8103-7.
2005: Liaman Mamedova; Valérie Capra; Maria Rosa Accomazzo; Zhan-Guo Gao; Silvia Ferrario; Marta Fumagalli; Maria P Abbracchio; G Enrico Rovati; Kenneth Alan Jacobson
CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors.
Biochemical pharmacology 2005;71(1-2):115-25.
2005: Melissa Perreira; Asher Shainberg; Craig J Thomas; Zhan-Guo Gao; Jian-Kang Jiang; Athena M Klutz; Changrui Lu; Kenneth Alan Jacobson
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
Journal of medicinal chemistry 2005;48(15):4910-8.
2005: Andreas A Erdmann; Zhan-Guo Gao; Unsu Jung; Jason Foley; Todd Borenstein; Kenneth Alan Jacobson; Daniel H Fowler
Activation of Th1 and Tc1 cell adenosine A2A receptors directly inhibits IL-2 secretion in vitro and IL-2-driven expansion in vivo.
Blood 2005;105(12):4707-14.
2005: Zhan-Guo Gao; Soo-Kyung Kim; Adriaan P IJzerman; Kenneth Alan Jacobson
Allosteric modulation of the adenosine family of receptors.
Mini reviews in medicinal chemistry 2005;5(6):545-53.
2005: Susanna Tchilibon; Bhalchandra V Joshi; Soo-Kyung Kim; Heng T Duong; Zhan-Guo Gao; Kenneth Alan Jacobson
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
Journal of medicinal chemistry 2005;48(6):1745-58.
2005: Philippe Van Rompaey; Kenneth Alan Jacobson; Ariel S Gross; Zhan-Guo Gao; Serge Van Calenbergh
Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety.
Bioorganic & medicinal chemistry 2005;13(4):973-83.
2005: Kenneth Alan Jacobson; Michihiro Ohno; Heng T Duong; Soo-Kyung Kim; Susanna Tchilibon; Michal Cesnek; Antonín Holý; Zhan-Guo Gao
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.
Chemistry & biology 2005;12(2):237-47.
2005: Heng T Duong; Zhan-Guo Gao; Kenneth Alan Jacobson
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 2005;24(10-12):1507-17.
2005: Hyouk Woo Lee; Dae Hong Shin; Ji Young Jeong; Hea Ok Kim; Moon Woo Chun; Neli Melman; Zhan-Guo Gao; Kenneth Alan Jacobson; Lak Shin Jeong
D-4'-thioadenosine derivatives as highly potent and selective agonists at the human A3 adenosine receptor.
Nucleosides, nucleotides & nucleic acids 2005;24(5-7):607-9.
2004: Kenneth Alan Jacobson; Soo-Kyung Kim; Stefano Costanzi; Zhan-Guo Gao
Purine receptors: GPCR structure and agonist design.
Molecular interventions 2004;4(6):337-47.
2004: Zhan-Guo Gao; Liaman Mamedova; Peiran Chen; Kenneth Alan Jacobson
2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors.
Biochemical pharmacology 2004;68(10):1985-93.
2004: Michihiro Ohno; Stefano Costanzi; Hak-Sung Kim; Veerle Kempeneers; Karen Vastmans; Piet Herdewijn; Savitri Maddileti; Zhan-Guo Gao; T Kendall Harden; Kenneth Alan Jacobson
Nucleotide analogues containing 2-oxa-bicyclo[2.2.1]heptane and l-alpha-threofuranosyl ring systems: interactions with P2Y receptors.
Bioorganic & medicinal chemistry 2004;12(21):5619-30.
2004: Stefano Costanzi; Liaman Mamedova; Zhan-Guo Gao; Kenneth Alan Jacobson
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
Journal of medicinal chemistry 2004;47(22):5393-404.
2004: Lak Shin Jeong; Myong Jung Kim; Hea Ok Kim; Zhan-Guo Gao; Soo-Kyung Kim; Kenneth Alan Jacobson; Moon Woo Chun
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 2004;14(19):4851-4.
2004: Zhan-Guo Gao; Liaman Mamedova; Susanna Tchilibon; Ariel S Gross; Kenneth Alan Jacobson
2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding.
Biochemical pharmacology 2004;68(2):231-7.
2004: Michihiro Ohno; Zhan-Guo Gao; Philippe Van Rompaey; Susanna Tchilibon; Soo-Kyung Kim; Brian A Harris; Ariel S Gross; Heng T Duong; Serge Van Calenbergh; Kenneth Alan Jacobson
Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position.
Bioorganic & medicinal chemistry 2004;12(11):2995-3007.
2004: Zhan-Guo Gao; Ariel S Gross; Kenneth Alan Jacobson
Effects of the allosteric modulator SCH-202676 on adenosine and P2Y receptors.
Life sciences 2004;74(25):3173-80.
2004: Liaman Mamedova; Bhalchandra V Joshi; Zhan-Guo Gao; Ivar von Kügelgen; Kenneth Alan Jacobson
Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors.
Biochemical pharmacology 2004;67(9):1763-70.
2004: Susanna Tchilibon; Soo-Kyung Kim; Zhan-Guo Gao; Brian A Harris; Joshua B Blaustein; Ariel S Gross; Heng T Duong; Neli Melman; Kenneth Alan Jacobson
Exploring distal regions of the A3 adenosine receptor binding site: sterically constrained N6-(2-phenylethyl)adenosine derivatives as potent ligands.
Bioorganic & medicinal chemistry 2004;12(9):2021-34.
2004: Zhan-Guo Gao; Lak Shin Jeong; Hyung Ryong Moon; Hea Ok Kim; Won Jun Choi; Dae Hong Shin; Eleonora Elhalem; Maria J Comin; Neli Melman; Liaman Mamedova; Ariel S Gross; Juan B Rodriguez; Kenneth Alan Jacobson
Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moiety.
Biochemical pharmacology 2004;67(5):893-901.
2004: Kwan-Young Jung; Soo-Kyung Kim; Zhan-Guo Gao; Ariel S Gross; Neli Melman; Kenneth Alan Jacobson; Yong-Chul Kim
Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists.
Bioorganic & medicinal chemistry 2004;12(3):613-23.
2004: Zhan-Guo Gao; Kenneth Alan Jacobson
Partial agonists for A(3) adenosine receptors.
Current topics in medicinal chemistry 2004;4(8):855-62.
2003: Soo-Kyung Kim; Zhan-Guo Gao; Philippe Van Rompaey; Ariel S Gross; Aishe Chen; Serge Van Calenbergh; Kenneth Alan Jacobson
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.
Journal of medicinal chemistry 2003;46(23):4847-59.
2003: Lak Shin Jeong; Dong Zhe Jin; Hea Ok Kim; Dae Hong Shin; Hyung Ryong Moon; Prashantha Gunaga; Moon Woo Chun; Yong-Chul Kim; Neli Melman; Zhan-Guo Gao; Kenneth Alan Jacobson
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.
Journal of medicinal chemistry 2003;46(18):3775-7.
2003: Seong G Kim; Zhan-Guo Gao; Kelly A Soltysiak; Tong-Shin Chang; Chaya Brodie; Kenneth Alan Jacobson
P2Y6 nucleotide receptor activates PKC to protect 1321N1 astrocytoma cells against tumor necrosis factor-induced apoptosis.
Cellular and molecular neurobiology 2003;23(3):401-18.
2003: Zhan-Guo Gao; Joshua B Blaustein; Ariel S Gross; Neli Melman; Kenneth Alan Jacobson
N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors.
Biochemical pharmacology 2003;65(10):1675-84.
2003: Zhan-Guo Gao; Soo-Kyung Kim; Ariel S Gross; Aishe Chen; Joshua B Blaustein; Kenneth Alan Jacobson
Identification of essential residues involved in the allosteric modulation of the human A(3) adenosine receptor.
Molecular pharmacology 2003;63(5):1021-31.
2003: Seong G Kim; Kelly A Soltysiak; Zhan-Guo Gao; Tong-Shin Chang; Eunju Chung; Kenneth Alan Jacobson
Tumor necrosis factor alpha-induced apoptosis in astrocytes is prevented by the activation of P2Y6, but not P2Y4 nucleotide receptors.
Biochemical pharmacology 2003;65(6):923-31.
2003: Moo Hong Lim; Hea Ok Kim; Hyung Ryong Moon; Seung Jin Lee; Moon Woo Chun; Zhan-Guo Gao; Neli Melman; Kenneth Alan Jacobson; Joong Hyup Kim; Lak Shin Jeong
Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands.
Bioorganic & medicinal chemistry letters 2003;13(5):817-20.
2003: Zhan-Guo Gao; Neli Melman; Andreas A Erdmann; Seong-Gon Kim; Christa E Müller; Adriaan P IJzerman; Kenneth Alan Jacobson
Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors.
Biochemical pharmacology 2003;65(4):525-34.
2002: Zhan-Guo Gao; Soo-Kyung Kim; Thibaud Biadatti; Wangzhong Chen; Kyeong Lee; Dov Barak; Seong-Gon Kim; Carl R Johnson; Kenneth Alan Jacobson
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.
Journal of medicinal chemistry 2002;45(20):4471-84.
2002: Zhan-Guo Gao; Seong-Gon Kim; Kelly A Soltysiak; Neli Melman; Adriaan P IJzerman; Kenneth Alan Jacobson
Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives.
Molecular pharmacology 2002;62(1):81-9.
2002: Zhan-Guo Gao; Aishe Chen; Dov Barak; Soo-Kyung Kim; Christa E Müller; Kenneth Alan Jacobson
Identification by site-directed mutagenesis of residues involved in ligand recognition and activation of the human A3 adenosine receptor.
The Journal of biological chemistry 2002;277(21):19056-63.
2002: Zhan-Guo Gao; Kenneth Alan Jacobson
2-Chloro-N(6)-cyclopentyladenosine, adenosine A(1) receptor agonist, antagonizes the adenosine A(3) receptor.
European journal of pharmacology 2002;443(1-3):39-42.
2001: Kenneth Alan Jacobson; Zhan-Guo Gao; Aishe Chen; Dov Barak; Soon-Ai Kim; Kyeong Lee; Andreas Link; P V Rompaey; Serge Van Calenbergh; Bruce T Liang
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.
Journal of medicinal chemistry 2001;44(24):4125-36.
2001: Zhan-Guo Gao; J E Van Muijlwijk-Koezen; Aishe Chen; Christa E Müller; Adriaan P IJzerman; Kenneth Alan Jacobson
Allosteric modulation of A(3) adenosine receptors by a series of 3-(2-pyridinyl)isoquinoline derivatives.
Molecular pharmacology 2001;60(5):1057-63.
2001: Aishe Chen; Zhan-Guo Gao; Dov Barak; Bruce T Liang; Kenneth Alan Jacobson
Constitutive activation of A(3) adenosine receptors by site-directed mutagenesis.
Biochemical and biophysical research communications 2001;284(3):596-601.