Zhang-Guo Gao

发表

Structure of an Agonist-Bound Human A2A Adenosine Receptor

R. Stevens, K. Jacobson, Fei Xu, 2011, Science.

Allosteric modulation and functional selectivity of G protein-coupled receptors.

K. Jacobson, Zhang-Guo Gao, 2013, Drug discovery today. Technologies.

Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.

K. Jacobson, Zhang-Guo Gao, S. Costanzi, 2004, Journal of medicinal chemistry.

Structure activity and molecular modeling analyses of ribose- and base-modified uridine 5'-triphosphate analogues at the human P2Y2 and P2Y4 receptors.

K. Jacobson, Zhang-Guo Gao, T. K. Harden, 2006, Biochemical pharmacology.

Agonist-bound structure of the human P2Y12 receptor

Hualiang Jiang, R. Stevens, K. Jacobson, 2014, Nature.

Structure of the human P2Y12 receptor in complex with an antithrombotic drug

Steven M. Moss, Hualiang Jiang, R. Stevens, 2014, Nature.

Two disparate ligand-binding sites in the human P2Y1 receptor

Hualiang Jiang, R. Stevens, K. Jacobson, 2015, Nature.

Constitutive Activation of A3 Adenosine Receptors by Site-Directed Mutagenesis

K. Jacobson, Zhang-Guo Gao, D. Barak, 2001 .

Adenosine receptors as therapeutic targets

K. Jacobson, Zhang-Guo Gao, 2006, Nature Reviews Drug Discovery.

Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.

Johannes Brussee, Kenneth A Jacobson, Kai Ye, 2006, Journal of medicinal chemistry.

Identification by Site-directed Mutagenesis of Residues Involved in Ligand Recognition and Activation of the Human A3 Adenosine Receptor*

K. Jacobson, C. Müller, Zhang-Guo Gao, 2002, The Journal of Biological Chemistry.

Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives.

Adriaan P IJzerman, Kenneth A Jacobson, K. Jacobson, 2002, Molecular pharmacology.

Medicinal Chemistry of the A 3 Adenosine Receptor

K. Jacobson, Zhang-Guo Gao, P. Baraldi, 2018 .

Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound A₂A adenosine receptor.

Fei Xu, Francesca Deflorian, Vsevolod Katritch, 2012, Journal of medicinal chemistry.

Synthesis of N 6-Substituted 3′-Ureidoadenosine Derivatives as Highly Potent Agonists at the Mutant A3 Adenosine Receptor

K. Jacobson, Zhang-Guo Gao, H. Moon, 2007, Nucleosides, nucleotides & nucleic acids.

Progress in the pursuit of therapeutic adenosine receptor antagonists

Giampiero Spalluto, Kenneth A Jacobson, S. Moro, 2006, Medicinal research reviews.

Purine receptors: GPCR structure and agonist design.

K. Jacobson, Zhang-Guo Gao, S. Costanzi, 2004, Molecular interventions.

Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moiety.

K. Jacobson, Zhang-Guo Gao, H. Moon, 2004, Biochemical pharmacology.

Identification of essential residues involved in the allosteric modulation of the human A(3) adenosine receptor.

Kenneth A Jacobson, K. Jacobson, Zhang-Guo Gao, 2003, Molecular pharmacology.

Engineering of A3 adenosine and P2Y nucleotide receptors and their ligands

K. Jacobson, Zhang-Guo Gao, D. Barak, 2003, Drug development research.

2-Chloro-N6-cyclopentyladenosine, adenosine A1 receptor agonist, antagonizes the adenosine A3 receptor

K. Jacobson, Zhang-Guo Gao, 2002 .

Fragment optimization for GPCRs by molecular dynamics free energy calculations: Probing druggable subpockets of the A2A adenosine receptor binding site

K. Jacobson, P. Matricon, G. Marucci, 2017, Scientific Reports.

Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A₂A and A₃ adenosine receptor ligands.

K. Jacobson, Sun Choi, Zhang-Guo Gao, 2012, Journal of medicinal chemistry.

Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.

K. Jacobson, Zhang-Guo Gao, L. Jeong, 2008, Bioorganic & medicinal chemistry.

Modulation of G protein-coupled adenosine receptors by strategically functionalized agonists and antagonists immobilized on gold nanoparticles

Steven M. Moss, K. Jacobson, Zhang-Guo Gao, 2013, Purinergic Signalling.

Probing the binding site of the A1 adenosine receptor reengineered for orthogonal recognition by tailored nucleosides.

K. Jacobson, Zhang-Guo Gao, K. Palaniappan, 2007, Biochemistry.

Nucleotide analogues containing 2-oxa-bicyclo[2.2.1]heptane and l-alpha-threofuranosyl ring systems: interactions with P2Y receptors.

T Kendall Harden, Stefano Costanzi, Piet Herdewijn, 2004, Bioorganic & medicinal chemistry.

Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors

R. Stevens, K. Jacobson, Zhang-Guo Gao, 2018, Scientific Reports.

Ligand design by targeting a binding site water

K. Jacobson, P. Matricon, Zhang-Guo Gao, 2020, Chemical science.

Synthesis and Anti-Renal Fibrosis Activity of Conformationally Locked Truncated 2-Hexynyl-N6-Substituted-(N)-Methanocarba-nucleosides as A3 Adenosine Receptor Antagonists and Partial Agonists

Steven M. Moss, K. Jacobson, M. Cui, 2014, Journal of medicinal chemistry.

Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates

K. Jacobson, Zhang-Guo Gao, A. Shainberg, 2008, Journal of nanobiotechnology.

Application of the functionalized congener approach to dendrimer-based signaling agents acting through A2A adenosine receptors

K. Jacobson, Zhang-Guo Gao, C. Gachet, 2008, Purinergic Signalling.

Machine Learning for Discovery of New ADORA Modulators

S. Ekins, K. Jacobson, Zhang-Guo Gao, 2022, Frontiers in Pharmacology.

IL-2 secretion in vitro and IL-2-driven expansion in vivo receptors directly inhibits 2A Activation of Th1 and Tc1 cell adenosine A

Zhang-Guo Gao, D. Fowler, J. Foley, 2013 .

Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.

K. Jacobson, A. IJzerman, Zhang-Guo Gao, 2009, Journal of medicinal chemistry.

Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.

K. Jacobson, Zhang-Guo Gao, W. J. Choi, 2008, Bioorganic & medicinal chemistry letters.

Synthesis and pharmacological characterization of [125I]MRS1898, a high-affinity, selective radioligand for the rat A3 adenosine receptor

K. Jacobson, Zhang-Guo Gao, G. Griffiths, 2008, Purinergic Signalling.

Synthesis of 3′-Acetamidoadenosine Derivatives as Potential A3 Adenosine Receptor Agonists

K. Jacobson, Zhang-Guo Gao, M. Chun, 2008, Nucleosides, nucleotides & nucleic acids.

Design, synthesis, and biological activity of N6-substituted-4'-thioadenosines at the human A3 adenosine receptor.

K. Jacobson, Zhang-Guo Gao, H. Moon, 2006, Bioorganic & medicinal chemistry.

"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.

K. Jacobson, Zhang-Guo Gao, Craig J. Thomas, 2005, Journal of medicinal chemistry.

Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety.

K. Jacobson, Philippe van Rompaey, S. van Calenbergh, 2005, Bioorganic & medicinal chemistry.

New 8-substituted xanthiene derivatives as potent bronchodilators.

K. Jacobson, Zhang-Guo Gao, K. Erol, 2005, Farmaco.

Effects of the allosteric modulator SCH-202676 on adenosine and P2Y receptors.

K. Jacobson, Zhang-Guo Gao, A. Gross, 2004, Life sciences.

Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.

K. Jacobson, Zhang-Guo Gao, M. Chun, 2004, Bioorganic & medicinal chemistry letters.

Chapter 13. A3 Adenosine Receptors.

K. Jacobson, Zhang-Guo Gao, B. Joshi, 2003, Annual reports in medicinal chemistry.

A2B adenosine receptor blockade inhibits growth of prostate cancer cells

K. Jacobson, Zhang-Guo Gao, S. Costanzi, 2013, Purinergic Signalling.

AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells.

K. Jacobson, Zhang-Guo Gao, H. Maruoka, 2013, Biochemical pharmacology.

Exploration of Alternative Scaffolds for P2Y14 Receptor Antagonists Containing a Biaryl Core.

K. Jacobson, T. Karcz, Zhang-Guo Gao, 2020, Journal of medicinal chemistry.

Novel fluorescent antagonist as a molecular probe in A(3) adenosine receptor binding assays using flow cytometry.

S. Moro, S. Federico, G. Spalluto, 2012, Biochemical pharmacology.

Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.

K. Jacobson, Zhang-Guo Gao, E. Kiselev, 2014, Biochemical pharmacology.

PEGylated dendritic unimolecular micelles as versatile carriers for ligands of G protein-coupled receptors.

K. Jacobson, Zhang-Guo Gao, C. Gachet, 2009, Bioconjugate chemistry.

Polyamidoamine (PAMAM) dendrimer conjugates of "clickable" agonists of the A3 adenosine receptor and coactivation of the P2Y14 receptor by a tethered nucleotide.

Jacobson, K. Jacobson, Zhang-Guo Gao, 2010, Bioconjugate chemistry.

Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor

K. Jacobson, Zhang-Guo Gao, 2017, Molecular Pharmacology.

Adenosine A2A receptor antagonists: from caffeine to selective non‐xanthines

K. Jacobson, P. Matricon, Zhang-Guo Gao, 2020, British journal of pharmacology.

Nucleotide P2Y1 receptor agonists are in vitro and in vivo prodrugs of A1/A3 adenosine receptor agonists: implications for roles of P2Y1 and A1/A3 receptors in physiology and pathology

K. Jacobson, C. Müller, Zhang-Guo Gao, 2020, Purinergic Signalling.

P2Y6 Nucleotide Receptor Activates PKC to Protect 1321N1 Astrocytoma Cells Against Tumor Necrosis Factor-Induced Apoptosis

K. Jacobson, Zhang-Guo Gao, C. Brodie, 2003, Cellular and Molecular Neurobiology.

Phosphatidylinositol 5-phosphate 4-kinase

F. Tamanoi, K. Jacobson, Mark A Sussman, 2012 .

Purinergic Signaling in Mast Cell Degranulation and Asthma

K. Jacobson, Zhang-Guo Gao, 2017, Front. Pharmacol..

GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2A Adenosine Receptor

R. Stevens, K. Jacobson, Sun Choi, 2022, Journal of medicinal chemistry.

CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors.

K. Jacobson, Zhang-Guo Gao, L. Mamedova, 2005, Biochemical pharmacology.

Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists.

K. Jacobson, Zhang-Guo Gao, A. Ivanov, 2008, Journal of medicinal chemistry.

Protection from Myocardial Ischemia/Reperfusion Injury by a Positive Allosteric Modulator of the A3 Adenosine Receptor

K. Jacobson, A. IJzerman, J. V. van Veldhoven, 2012, Journal of Pharmacology and Experimental Therapeutics.

The role of P2Y14 and other P2Y receptors in degranulation of human LAD2 mast cells

K. Jacobson, Zhang-Guo Gao, M. P. S. Jayasekara, 2013, Purinergic Signalling.

Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors.

K. Jacobson, Zhang-Guo Gao, L. Mamedova, 2004, Biochemical pharmacology.

Tumor necrosis factor alpha-induced apoptosis in astrocytes is prevented by the activation of P2Y6, but not P2Y4 nucleotide receptors.

K. Jacobson, Zhang-Guo Gao, T. Chang, 2003, Biochemical pharmacology.

Fluorescent A2A and A3 adenosine receptor antagonists as flow cytometry probes

K. Jacobson, Zhang-Guo Gao, V. Salmaso, 2022, Purinergic Signalling.

Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling.

R. Stevens, K. Jacobson, V. Katritch, 2018, Structure.

2-Chloro-N(6)-cyclopentyladenosine, adenosine A(1) receptor agonist, antagonizes the adenosine A(3) receptor.

K. Jacobson, Zhang-Guo Gao, 2002, European journal of pharmacology.

Allosteric Coupling of Drug Binding and Intracellular Signaling in the A 2 A Adenosine Receptor Graphical Abstract Highlights

K. Wüthrich, R. Stevens, K. Jacobson, 2017 .

Assessment of biased agonism at the A3 adenosine receptor using β-arrestin and miniGαi recruitment assays.

K. Jacobson, Zhang-Guo Gao, C. Stove, 2020, Biochemical pharmacology.

Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition.

K. Jacobson, Zhang-Guo Gao, Z. Şahin, 2020, European journal of medicinal chemistry.

Preclinical Evaluation of the First Adenosine A1 Receptor Partial Agonist Radioligand for Positron Emission Tomography Imaging.

N. Volkow, Gene-Jack Wang, K. Jacobson, 2018, Journal of medicinal chemistry.

Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists

K. Jacobson, Zhang-Guo Gao, J. Auchampach, 2016, Journal of medicinal chemistry.

Synthesis and characterization of [76Br]-labeled high-affinity A3 adenosine receptor ligands for positron emission tomography.

K. Jacobson, Zhang-Guo Gao, Ying Ma, 2009, Nuclear medicine and biology.

2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding.

K. Jacobson, Zhang-Guo Gao, L. Mamedova, 2004, Biochemical pharmacology.

Exploring distal regions of the A3 adenosine receptor binding site: sterically constrained N6-(2-phenylethyl)adenosine derivatives as potent ligands.

Kenneth A Jacobson, K. Jacobson, Zhang-Guo Gao, 2004, Bioorganic & medicinal chemistry.

Biological Evaluation of 5'-(N-Ethylcarboxamido)adenosine Analogues as Grp94-Selective Inhibitors.

K. Jacobson, Zhang-Guo Gao, B. Blagg, 2021, ACS medicinal chemistry letters.

NUCLEOSIDE PRODRUGS OF A3 ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS.

K. Jacobson, Zhang-Guo Gao, K. Palaniappan, 2006, Collection of Czechoslovak chemical communications.

Keynote review: allosterism in membrane receptors.

K. Jacobson, Zhang-Guo Gao, 2006, Drug discovery today.

Discovery of Highly Potent Adenosine A1 Receptor Agonists: Targeting Positron Emission Tomography Probes.

N. Volkow, K. Jacobson, J. Fowler, 2021, ACS chemical neuroscience.

Activation of the P2Y1 receptor induces apoptosis and inhibits proliferation of prostate cancer cells.

K. Jacobson, Zhang-Guo Gao, S. Costanzi, 2011, Biochemical pharmacology.

A2B Adenosine Receptor and Cancer

K. Jacobson, Zhang-Guo Gao, 2019, International journal of molecular sciences.

UDP‐glucose acting at P2Y14 receptors is a mediator of mast cell degranulation

K. Jacobson, Zhang-Guo Gao, Yi-Jiun Ding, 2010, Biochemical pharmacology.

P2Y(13) receptor is responsible for ADP-mediated degranulation in RBL-2H3 rat mast cells.

K. Jacobson, Zhang-Guo Gao, Yi-Jiun Ding, 2010, Pharmacological research.

Neoceptors: reengineering GPCRs to recognize tailored ligands.

K. Jacobson, Zhang-Guo Gao, B. Liang, 2007, Trends in pharmacological sciences.

Regulation of death and survival in astrocytes by ADP activating P2Y1 and P2Y12 receptors.

K. Jacobson, Zhang-Guo Gao, L. Mamedova, 2006, Biochemical pharmacology.

Structure-Activity Studies of 1H-Imidazo[4,5-c]quinolin-4-amine Derivatives as A3 Adenosine Receptor Positive Allosteric Modulators.

K. Jacobson, Zhang-Guo Gao, J. Auchampach, 2022, Journal of medicinal chemistry.

Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.

K. Jacobson, Zhang-Guo Gao, J. Auchampach, 2008, Bioorganic & medicinal chemistry letters.

On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin.

K. Jacobson, Zhang-Guo Gao, 2016, Biochemical pharmacology.

Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways.

K. Jacobson, Zhang-Guo Gao, 2008, Pharmacological research.

Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor

K. Wüthrich, R. Stevens, K. Jacobson, 2018, Cell.

Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.

Ruben Abagyan, Fei Xu, Francesca Deflorian, 2012, Journal of medicinal chemistry.

Novel alendronate-CGS21680 conjugate reduces bone resorption and induces new bone formation in post-menopausal osteoporosis and inflammatory osteolysis mouse models

K. Jacobson, Zhang-Guo Gao, B. Cronstein, 2022, Arthritis research & therapy.

Convergent synthesis of 2-thioether-substituted (N)-methanocarba-adenosines as purine receptor agonists

K. Jacobson, R. B. Poe, Zhang-Guo Gao, 2021, RSC advances.

G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions

K. Jacobson, F. Deflorian, Zhang-Guo Gao, 2012, Purinergic Signalling.

Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development

K. Jacobson, Zhang-Guo Gao, D. Tosh, 2019, Front. Cell. Neurosci..

A3 Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy

K. Jacobson, Zhang-Guo Gao, K. Varani, 2018, Medicinal research reviews.

Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position.

K. Jacobson, Philippe van Rompaey, S. van Calenbergh, 2004, Bioorganic & medicinal chemistry.

Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.

K. Jacobson, Philippe van Rompaey, S. van Calenbergh, 2006, Journal of medicinal chemistry.

Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists.

K. Jacobson, Zhang-Guo Gao, Yong‐Chul Kim, 2004, Bioorganic & medicinal chemistry.

2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.

K. Jacobson, S. van Calenbergh, Zhang-Guo Gao, 2006, Journal of medicinal chemistry.

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.

K. Jacobson, Zhang-Guo Gao, H. Moon, 2007, Journal of medicinal chemistry.

N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.

K. Jacobson, Zhang-Guo Gao, H. Moon, 2003, Journal of medicinal chemistry.

Species dependence of A3 adenosine receptor pharmacology and function

K. Jacobson, Zhang-Guo Gao, J. Auchampach, 2022, Purinergic Signalling.

Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.

K. Jacobson, Zhang-Guo Gao, A. Ivanov, 2007, Journal of medicinal chemistry.

N6-Substituted 5'-N-Methylcarbamoyl-4'-selenoadenosines as Potent and Selective A3 Adenosine Receptor Agonists with Unusual Sugar Puckering and Nucleobase Orientation.

Steven M. Moss, K. Jacobson, M. Cui, 2017, Journal of medicinal chemistry.

Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.

K. Jacobson, Zhang-Guo Gao, B. Joshi, 2005, Journal of medicinal chemistry.

Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.

K. Jacobson, Zhang-Guo Gao, H. Moon, 2006, Journal of medicinal chemistry.

(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.

K. Jacobson, Zhang-Guo Gao, B. Joshi, 2005, Journal of medicinal chemistry.

Partial Agonists for A3 Adenosine Receptors

K. Jacobson, Zhang-Guo Gao, 2004 .

N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors.

K. Jacobson, Zhang-Guo Gao, N. Melman, 2003, Biochemical pharmacology.

Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.

K. Jacobson, Zhang-Guo Gao, A. Ivanov, 2009, Journal of medicinal chemistry.

Structural Determinants of A3 Adenosine Receptor Activation: Nucleoside Ligands at the Agonist/Antagonist Boundary

Kenneth A. Jacobson, Carl R. Johnson, Dov Barak, 2002 .

2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors.

K. Jacobson, Zhang-Guo Gao, L. Mamedova, 2004, Biochemical pharmacology.

Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands.

K. Jacobson, Zhang-Guo Gao, H. Moon, 2003, Bioorganic & medicinal chemistry letters.

Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.

Carl R. Johnson, Dov Barak, Kenneth A Jacobson, 2002, Journal of medicinal chemistry.

SYNTHESIS OF 3′-UREIDOADENOSINE ANALOGUES AND THEIR BINDING AFFINITY TO THE A3 ADENOSINE RECEPTOR

K. Jacobson, Zhang-Guo Gao, M. Chun, 2005, Nucleosides, nucleotides & nucleic acids.

Design and in Vivo Characterization of A1 Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series.

K. Jacobson, M. Reitman, Zhang-Guo Gao, 2019, Journal of medicinal chemistry.

Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors.

K. Jacobson, A. IJzerman, C. Müller, 2003, Biochemical Pharmacology.

Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A3 Adenosine Receptor Homology Models and Structural Network Analysis Can Predict This Boundary.

K. Jacobson, Sun Choi, Zhang-Guo Gao, 2021, Journal of Medicinal Chemistry.

In Vivo Phenotypic Screening for Treating Chronic Neuropathic Pain: Modification of C2-Arylethynyl Group of Conformationally Constrained A3 Adenosine Receptor Agonists

Steven M. Moss, K. Jacobson, Zhang-Guo Gao, 2014, Journal of medicinal chemistry.

Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.

Francesca Deflorian, Kenneth A Jacobson, K. Jacobson, 2012, Journal of medicinal chemistry.

A3 Adenosine Receptor Agonists: History and Future Perspectives

K. Jacobson, Zhang-Guo Gao, G. Sanjayan, 2010 .

Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.

K. Jacobson, Zhang-Guo Gao, H. Moon, 2009, Bioorganic & medicinal chemistry.

Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.

Sang Kook Lee, Kenneth A Jacobson, K. Jacobson, 2009, Bioorganic & medicinal chemistry.

Stereoselective Synthesis of 1′-Functionalized-4′-Thionucleosides

K. Jacobson, Zhang-Guo Gao, H. Moon, 2007, Nucleosides, nucleotides & nucleic acids.

Design, Synthesis, and Anti-Tumor Activity of 4′-Thionucleosides as Potent and Selective Agonists at the Human A3 Adenosine Receptor

K. Jacobson, Zhang-Guo Gao, H. Moon, 2007, Nucleosides, nucleotides & nucleic acids.

2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists.

K. Jacobson, Zhang-Guo Gao, D. Kang, 2010, Bioorganic & medicinal chemistry.

Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors

R. Stevens, K. Jacobson, Zhang-Guo Gao, 2018, Scientific Reports.

PCAF Lysine Acetyltransferase

F. Tamanoi, K. Jacobson, Mark A Sussman, 2008 .

Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.

K. Jacobson, A. Janowsky, Zhang-Guo Gao, 2017, Journal of medicinal chemistry.

Interaction of A3 adenosine receptor ligands with the human multidrug transporter ABCG2.

K. Jacobson, Zhang-Guo Gao, S. Ambudkar, 2022, European journal of medicinal chemistry.

Activation of Th1 and Tc1 cell adenosine A2A receptors directly inhibits IL-2 secretion in vitro and IL-2-driven expansion in vivo.

K. Jacobson, Zhang-Guo Gao, D. Fowler, 2005, Blood.

Molecular Docking Screening Using Agonist-Bound GPCR Structures: Probing the A2A Adenosine Receptor

David Rodríguez, Jens Carlsson, Kenneth A. Jacobson, 2015, J. Chem. Inf. Model..

Accelerating the Throughput of Affinity Mass Spectrometry-Based Ligand Screening toward a G Protein-Coupled Receptor.

R. Stevens, K. Jacobson, Zhang-Guo Gao, 2019, Analytical chemistry.

Extrinsic Tryptophans as NMR Probes of Allosteric Coupling in Membrane Proteins: Application to the A2A Adenosine Receptor.

K. Wüthrich, R. Stevens, K. Jacobson, 2018, Journal of the American Chemical Society.

Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.

K. Jacobson, F. Deflorian, Zhang-Guo Gao, 2010, Bioorganic & medicinal chemistry letters.

A 1 Adenosine Receptor Agonists, Antagonists, and Allosteric Modulators

K. Jacobson, Zhang-Guo Gao, D. Tosh, 2018 .

Limits of Ligand Selectivity from Docking to Models: In Silico Screening for A1 Adenosine Receptor Antagonists

Peter Kolb, Andrej Sali, Kenneth A. Jacobson, 2012, PloS one.

Dexamethasone Enhances ATP-Induced Inflammatory Responses in Endothelial Cells

K. Jacobson, Zhang-Guo Gao, A. Suffredini, 2010, Journal of Pharmacology and Experimental Therapeutics.

Anti-ischemic effects of multivalent dendrimeric A₃ adenosine receptor agonists in cultured cardiomyocytes and in the isolated rat heart.

K. Jacobson, Zhang-Guo Gao, D. Tosh, 2012, Pharmacological research.

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

F. Ciruela, K. Jacobson, Zhang-Guo Gao, 2017, MedChemComm.

Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.

Silvia Paoletta, Steven M. Moss, Kenneth A Jacobson, 2013, Journal of medicinal chemistry.

Selective A3 Adenosine Receptor Antagonist Radioligand for Human and Rodent Species.

K. Jacobson, R. B. Poe, Zhang-Guo Gao, 2022, ACS medicinal chemistry letters.

A3 adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity.

K. Jacobson, Zhang-Guo Gao, O. Gavrilova, 2021, European journal of medicinal chemistry.

Effects of Purinergic Receptor Deletion or Pharmacologic Modulation on Pulmonary Inflammation in Mice

K. Jacobson, T. Karcz, Zhang-Guo Gao, 2022, ACS pharmacology & translational science.

Characterization of Dual-Acting A3 Adenosine Receptor Positive Allosteric Modulators That Preferentially Enhance Adenosine-Induced Gαi3 and GαoA Isoprotein Activation.

Brian C. Smith, K. Jacobson, Zhang-Guo Gao, 2022, ACS pharmacology & translational science.

Pharmacological characterization of DPTN and other selective A3 adenosine receptor antagonists

K. Jacobson, Zhang-Guo Gao, R. Suresh, 2021, Purinergic Signalling.

Allosteric Antagonism of the A2A Adenosine Receptor by a Series of Bitopic Ligands

K. Jacobson, Zhang-Guo Gao, Kiran S Toti, 2020, Cells.

Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A3 Adenosine Receptors: Affinity Enhancement by N6-(2-Phenylethyl) Substitution.

K. Jacobson, M. Reitman, Zhang-Guo Gao, 2020, Journal of medicinal chemistry.

Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A3 Receptor Agonists.

K. Jacobson, Zhang-Guo Gao, J. Auchampach, 2020, ACS medicinal chemistry letters.

On the G protein‐coupling selectivity of the native A2B adenosine receptor

K. Jacobson, Zhang-Guo Gao, A. Inoue, 2017, Biochemical pharmacology.

Fragment optimization for GPCRs by molecular dynamics free energy calculations: Probing druggable subpockets of the A2A adenosine receptor binding site

K. Jacobson, P. Matricon, G. Marucci, 2017, Scientific Reports.

Emerging adenosine receptor agonists

K. Jacobson, Zhang-Guo Gao, 2007, Expert opinion on emerging drugs.

1 A 2 B adenosine receptor and cancer 2

K. Jacobson, Zhang-Guo Gao, 2019 .

Why do anti-inflammatory therapies fail to improve insulin sensitivity?

Jian-ping Ye, Zhang-Guo Gao, Zhan-guo Gao, 2011, Acta Pharmacologica Sinica.

Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.

K. Jacobson, Zhang-Guo Gao, J. Auchampach, 2015, ACS medicinal chemistry letters.

Emerging adenosine receptor agonists – an update

K. Jacobson, Zhang-Guo Gao, 2011, Expert opinion on emerging drugs.

Rapamycin weekly maintenance dosing and the potential efficacy of combination sorafenib plus rapamycin but not atorvastatin or doxycycline in tuberous sclerosis preclinical models

Adriaan P IJzerman, Kenneth A Jacobson, Kai Ye, 2009, BMC pharmacology.

Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.

Steven M. Moss, K. Jacobson, F. Deflorian, 2012, Journal of medicinal chemistry.

A2B adenosine receptor blockade inhibits growth of prostate cancer cells

K. Jacobson, Zhang-Guo Gao, S. Costanzi, 2013, Purinergic Signalling.

GPCR ligand dendrimer (GLiDe) conjugates: adenosine receptor interactions of a series of multivalent xanthine antagonists.

K. Jacobson, Zhang-Guo Gao, A. Kecskés, 2011, Bioconjugate chemistry.

Signaling of the human P2Y1 receptor measured by a yeast growth assay with comparisons to assays of phospholipase C and calcium mobilization in 1321N1 human astrocytoma cells

J. Wess, K. Jacobson, Zhang-Guo Gao, 2005, Purinergic Signalling.

Repurposing of a Nucleoside Scaffold from Adenosine Receptor Agonists to Opioid Receptor Antagonists

K. Jacobson, A. Janowsky, Zhang-Guo Gao, 2018, ACS omega.

Terpenes from Cannabis sativa Induce Antinociception in Mouse Chronic Neuropathic Pain via Activation of Spinal Cord Adenosine A2A Receptors

K. Jacobson, Zhang-Guo Gao, J. Streicher, 2023, bioRxiv.

The role of P2Y14 and other P2Y receptors in degranulation of human LAD2 mast cells

K. Jacobson, Zhang-Guo Gao, M. P. S. Jayasekara, 2013, Purinergic Signalling.

Nucleotides Acting at P2Y Receptors: Connecting Structure and Function

R. Stevens, K. Jacobson, V. Katritch, 2015, Molecular Pharmacology.

Structure-Based Discovery of A2A Adenosine Receptor Ligands

Brian K. Shoichet, John J. Irwin, Jens Carlsson, 2010, Journal of medicinal chemistry.

Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A3 adenosine receptor antagonists.

K. Jacobson, Zhang-Guo Gao, J. Auchampach, 2018, MedChemComm.

Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists.

David Rodríguez, Jens Carlsson, Saibal Chakraborty, 2016, ACS chemical biology.

Probing structure‐activity relationship in &bgr;‐arrestin2 recruitment of diversely substituted adenosine derivatives

K. Jacobson, Zhang-Guo Gao, C. Stove, 2018, Biochemical pharmacology.

Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2A adenosine receptor agonists

Gangadhar J Sanjayan, Kenneth A Jacobson, K. Jacobson, 2010, Journal of nanobiotechnology.

ResearchNucleoside conjugates of quantum dots for characterization of G protein-coupled receptors : strategies for immobilizing A 2 A adenosine receptor agonists

K. Jacobson, Zhang-Guo Gao, Arijit Das, 2015 .

characterization of G protein-coupled receptors: strategies for immobilizing A 2A adenosine receptor agonists

K. Jacobson, Zhang-Guo Gao, Arijit Das, 2010 .

Exchange of a nuclear corepressor between NF-kappaB and CREB mediates inhibition of phosphoenolpyruvate carboxykinase transcription by NF-kappaB.

Zhang-Guo Gao, J. Yan, J. Weng, 2010, Chinese medical journal.

Structure Activity Relationship of 3-Nitro-2-(trifluoromethyl)-2H-chromene Derivatives as P2Y6 Receptor Antagonists.

K. Jacobson, Zhang-Guo Gao, Ngan B. Phung, 2021, Bioorganic & medicinal chemistry letters.

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

K. Jacobson, Zhang-Guo Gao, H. Duong, 2005, Nucleosides, nucleotides & nucleic acids.

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.

S. Moro, K. Klotz, S. Federico, 2010, Bioorganic & medicinal chemistry.

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.

S. Moro, K. Klotz, S. Federico, 2011, Journal of medicinal chemistry.

Anionic Phospholipids Control Mechanisms of GPCR-G Protein Recognition

K. Jacobson, Zhang-Guo Gao, M. Eddy, 2023, bioRxiv.

The role of activated adenosine receptors in degranulation of human LAD2 mast cells

K. Jacobson, Zhang-Guo Gao, Ang Li, 2014, Purinergic Signalling.

Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor.

Kenneth A Jacobson, K. Jacobson, Zhang-Guo Gao, 2006, Journal of molecular graphics & modelling.

Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety.

K. Jacobson, Zhang-Guo Gao, L. Jeong, 2006, Bioorganic & medicinal chemistry letters.

Nucleoside-derived antagonists to A3 adenosine receptors lower mouse intraocular pressure and act across species.

K. Jacobson, R. Stone, Zhang-Guo Gao, 2010, Experimental eye research.

Novel Alexa Fluor-488 labeled antagonist of the A(2A) adenosine receptor: Application to a fluorescence polarization-based receptor binding assay.

K. Jacobson, Zhang-Guo Gao, Miklós Kecskés, 2010, Biochemical pharmacology.

Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.

Jacobson, K. Jacobson, Zhang-Guo Gao, 2008, Journal of medicinal chemistry.

Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.

Kenneth A Jacobson, K. Jacobson, Philippe van Rompaey, 2003, Journal of medicinal chemistry.

Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist.

S. Moro, G. Spalluto, G. Pastorin, 2002, Journal of medicinal chemistry.

Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators.

Steven M. Moss, K. Jacobson, S. van Calenbergh, 2014, Bioorganic & medicinal chemistry.

Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers.

Kenneth A Jacobson, Kai Ye, K. Jacobson, 2011, Biochemical pharmacology.

Site-directed mutagenesis studies of human A2A adenosine receptors

K. Jacobson, A. IJzerman, Zhang-Guo Gao, 2000 .

Action of Nucleosides and Nucleotides at 7 Transmembrane-Spanning Receptors

K. Jacobson, Zhang-Guo Gao, S. Costanzi, 2006, Nucleosides, nucleotides & nucleic acids.

Allosteric modulation of the adenosine family of receptors.

Kenneth A Jacobson, K. Jacobson, A. IJzerman, 2005, Mini reviews in medicinal chemistry.

Conjugable A3 adenosine receptor antagonists for the development of functionalized ligands and their use in fluorescent probes.

S. Moro, S. Federico, G. Spalluto, 2019, European journal of medicinal chemistry.

Species differences and mechanism of action of A3 adenosine receptor allosteric modulators

K. Jacobson, A. IJzerman, Zhang-Guo Gao, 2018, Purinergic Signalling.

Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT2B/5HT2C Serotonin Receptor Antagonists.

K. Jacobson, Zhang-Guo Gao, S. Crane, 2016, Journal of medicinal chemistry.

Caged agonist of P2Y1 and P2Y12 receptors for light-directed facilitation of platelet aggregation.

K. Jacobson, Zhang-Guo Gao, C. Gachet, 2008, Biochemical pharmacology.

Fei Xu Adenosine Receptor 2 AStructure of an Agonist-Bound Human A

R. Stevens, K. Jacobson, V. Katritch, 2012 .

John Daly Lecture: Structure-guided Drug Design for Adenosine and P2Y Receptors☆

K. Jacobson, Zhang-Guo Gao, E. Kiselev, 2014, Computational and structural biotechnology journal.

Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.

Steven M. Moss, K. Jacobson, Zhang-Guo Gao, 2014, ACS medicinal chemistry letters.

Nucleotides Acting at P 2 Y Receptors : Connecting Structure and Function

R. Stevens, K. Jacobson, V. Katritch, 2015 .

Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.

K. Jacobson, F. Deflorian, Zhang-Guo Gao, 2011, ACS medicinal chemistry letters.

Synthesis of hypermodified adenosine derivatives as selective adenosine A3 receptor ligands.

K. Jacobson, Philippe van Rompaey, S. van Calenbergh, 2006, Bioorganic & medicinal chemistry.

A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.

K. Jacobson, Zhang-Guo Gao, S. Tchilibon, 2005, Chemistry & biology.

Modulation of G protein-coupled adenosine receptors by strategically functionalized agonists and antagonists immobilized on gold nanoparticles

Steven M. Moss, K. Jacobson, Zhang-Guo Gao, 2013, Purinergic Signalling.

Structure-Based Design, Synthesis by Click Chemistry and in Vivo Activity of Highly Selective A3 Adenosine Receptor Agonists.

Silvia Paoletta, Kenneth A Jacobson, K. Jacobson, 2015, MedChemComm.

Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions.

K. Jacobson, Zhang-Guo Gao, S. Paoletta, 2012, ACS medicinal chemistry letters.

Allosteric modulation of purine and pyrimidine receptors.

K. Jacobson, A. IJzerman, A. Göblyös, 2011, Advances in pharmacology.

Adenosine Receptor Agonists Using Structure-Based Ligand Design

R. Abagyan, R. Stevens, K. Jacobson, 2012 .

Partial agonists for A(3) adenosine receptors.

K. Jacobson, Zhang-Guo Gao, 2004, Current topics in medicinal chemistry.

Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists.

Jens Carlsson, Kenneth A Jacobson, K. Jacobson, 2012, ACS medicinal chemistry letters.

Discovery of New Human A(2A) Adenosine Receptor Agonists: Design, Synthesis, and Binding Mode of Truncated 2-Hexynyl-4'-thioadenosine.

K. Jacobson, Sun Choi, Zhang-Guo Gao, 2010, ACS medicinal chemistry letters.

Click modification in the N6 region of A3 adenosine receptor-selective carbocyclic nucleosides for dendrimeric tethering that preserves pharmacophore recognition.

K. Jacobson, F. Deflorian, Zhang-Guo Gao, 2012, Bioconjugate chemistry.

Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2Y14 Receptor Antagonists.

K. Jacobson, Zhang-Guo Gao, Sylvie Breton, 2023, Journal of medicinal chemistry.

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.

K. Jacobson, F. Deflorian, Zhang-Guo Gao, 2011, Bioorganic & medicinal chemistry letters.

PTPe (RPTPe and Cyt-PTPe)

F. Tamanoi, K. Jacobson, Mark A Sussman, 2012 .

Synthesis and evaluation of adenosine derivatives as A1, A2A, A2B and A3 adenosine receptor ligands containing boron clusters as phenyl isosteres and selective A3 agonists.

K. Jacobson, Zhang-Guo Gao, Harsha Rao, 2021, European journal of medicinal chemistry.

Structure activity relationships of 5-HT2B and 5-HT2C serotonin receptor antagonists: N6, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.

K. Jacobson, Zhang-Guo Gao, J. McCorvy, 2023, European journal of medicinal chemistry.

A2B adenosine receptor activation and modulation by protein kinase C

K. Jacobson, Zhang-Guo Gao, A. Inoue, 2023, iScience.

Synthesis and Anti-Renal Fibrosis Activity of Conformationally Locked Truncated 2-Hexynyl-N6-Substituted-(N)-Methanocarba-nucleosides as A3 Adenosine Receptor Antagonists and Partial Agonists

Steven M. Moss, M. Cui, Sun Choi, 2014, Journal of Medicinal Chemistry.

The role of activated adenosine receptors in degranulation of human LAD2 mast cells

K. Jacobson, Zhang-Guo Gao, Ang Li, 2014, Purinergic Signalling.

Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000

Zhang-Guo Gao, Kenneth A. Jacobson, Anikó Göblyös, 2008, BMC pharmacology.

Site-directed mutagenesis studies of human A(2A) adenosine receptors: involvement of glu(13) and his(278) in ligand binding and sodium modulation.

K. Jacobson, A. IJzerman, Zhang-Guo Gao, 2000, Biochemical pharmacology.

Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.

K. Jacobson, S. van Calenbergh, Zhang-Guo Gao, 2001, Journal of medicinal chemistry.

First Potent Macrocyclic A3 Adenosine Receptor Agonists Reveal G-Protein and β-Arrestin2 Signaling Preferences.

K. Jacobson, Zhang-Guo Gao, J. Auchampach, 2023, ACS pharmacology & translational science.

Membrane Mimetic-Dependence of GPCR Energy Landscapes

Zhang-Guo Gao, M. Eddy, A. Ray, 2023, bioRxiv.

G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions

K. Jacobson, F. Deflorian, Zhang-Guo Gao, 2012, Purinergic Signalling.

Novel fluorescent antagonist as a molecular probe in A(3) adenosine receptor binding assays using flow cytometry.

S. Moro, S. Federico, G. Spalluto, 2012, Biochemical pharmacology.

Allosteric modulation and functional selectivity of G protein-coupled receptors.

K. Jacobson, Zhang-Guo Gao, 2013, Drug discovery today. Technologies.

Preclinical evaluation of the first adenosine A 1 receptor partial agonist radioligand for positron emission tomography (PET) imaging

Gene-Jack Wang, Zhang-Guo Gao, C. Wiers, 2021 .

A2B adenosine receptor signaling and regulation.

Zhang-Guo Gao, Mansour Haddad, Kenneth A. Jacobson, 2024, Purinergic signalling.

Programmable Nanoscaffolds That Control Ligand Display to a G-Protein-Coupled Receptor in Membranes To Allow Dissection of Multivalent Effects

Steven M. Moss, S. Durell, K. Jacobson, 2014, Journal of the American Chemical Society.

Protection from Myocardial Ischemia/Reperfusion Injury by a Positive Allosteric Modulator of the A3 Adenosine Receptor

K. Jacobson, A. IJzerman, J. V. van Veldhoven, 2012, Journal of Pharmacology and Experimental Therapeutics.

Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.

K. Jacobson, F. Deflorian, Zhang-Guo Gao, 2012, Journal of medicinal chemistry.

Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A2A/A3 Adenosine Receptor Antagonists and Their Cancer Immunotherapeutic Activity.

K. Jacobson, Zhang-Guo Gao, L. Jeong, 2023, Journal of medicinal chemistry.

N6-Substituted 5'-N-Methylcarbamoyl-4'-selenoadenosines as Potent and Selective A3 Adenosine Receptor Agonists with Unusual Sugar Puckering and Nucleobase Orientation.

Steven M. Moss, K. Jacobson, Sun Choi, 2017, Journal of medicinal chemistry.

Discovery of A New Human A2A Adenosine Receptor Agonist, Truncated 2-Hexynyl-4′-thioadenosine

K. Jacobson, Sun Choi, Zhang-Guo Gao, 2010 .

Nucleoside-derived antagonists to A3 adenosine receptors lower mouse intraocular pressure and act across species.

K. Jacobson, R. Stone, Zhang-Guo Gao, 2010, Experimental eye research.

Genetic and functional modulation by agonist MRS5698 and allosteric enhancer LUF6000 at the native A3 adenosine receptor in HL-60 cells

Zhang-Guo Gao, D. Tosh, Kenneth A. Jacobson, 2024, Purinergic Signalling Purinergic Signalling.

Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A2A Adenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors.

Zhang-Guo Gao, L. Jeong, Jinha Yu, 2024, Journal of medicinal chemistry.

Lipid Trolling to Optimize A3 Adenosine Receptor-Positive Allosteric Modulators (PAMs).

Zhang-Guo Gao, J. Auchampach, V. Salmaso, 2024, Journal of medicinal chemistry.

Chimeras Derived from a P2Y14 Receptor Antagonist and UDP-Sugar Agonists for Potential Treatment of Inflammation.

Zhang-Guo Gao, Zhoumou Chen, Young-Hwan Jung, 2024, ACS pharmacology & translational science.

Allosteric modulation of A(3) adenosine receptors by a series of 3-(2-pyridinyl)isoquinoline derivatives.

K. Jacobson, A. IJzerman, C. Müller, 2001, Molecular pharmacology.

Constitutive activation of A(3) adenosine receptors by site-directed mutagenesis.

K. Jacobson, Zhang-Guo Gao, D. Barak, 2001, Biochemical and biophysical research communications.

Membrane mimetic-dependence of GPCR energy landscapes.

Zhang-Guo Gao, M. Eddy, A. Ray, 2024, Structure.

Protein kinase CK 2 : in search for its regulation

J. Kotera, Zhang-Guo Gao, P. Storz, 2017 .