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Author Details

Kenneth A Jacobson
National Institutes of Health
1982
789
89
Andrej Sali (CM4AI)
PMIDPaper TitleJournal TitlePublished Year
36918461Covalently Binding Adenosine A<sub>3</sub> Receptor Agonist ICBM Irreversibly Reduces Voltage-Gated Ca<sup>2+</sup> Currents in Dorsal Root Ganglion Neurons.Purinergic Signal2024
36711594Anionic Phospholipids Control Mechanisms of GPCR-G Protein Recognition.bioRxiv2023
37562117Structure activity relationships of 5-HT<sub>2B</sub> and 5-HT<sub>2C</sub> serotonin receptor antagonists: N<sup>6</sup>, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.Eur J Med Chem2023
37705595First Potent Macrocyclic A<sub>3</sub> Adenosine Receptor Agonists Reveal G-Protein and β-Arrestin2 Signaling Preferences.ACS Pharmacol Transl Sci2023
37705594Assay-Dependent Inverse Agonism at the A<sub>3</sub> Adenosine Receptor: When Neutral Is Not Neutral.ACS Pharmacol Transl Sci2023
37741687A<sub>2A</sub> adenosine receptor agonists, antagonists, inverse agonists and partial agonists.Int Rev Neurobiol2023
37541364Anti-inflammatory potency of novel ecto-5'-nucleotidase/CD73 inhibitors in astrocyte culture model of neuroinflammation.Eur J Pharmacol2023
37605951Cannabidiol negatively modulates adenosine A<sub>2A</sub> receptor functioning in living cells.Acta Neuropsychiatr2023
37603740Specific inhibition of an anticancer target, polo-like kinase 1, by allosterically dismantling its mechanism of substrate recognition.Proc Natl Acad Sci U S A2023
37603705Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A<sub>2A</sub>/A<sub>3</sub> Adenosine Receptor Antagonists and Their Cancer Immunotherapeutic Activity.J Med Chem2023
37676356Editorial: Small molecules and biologics for future purinergic therapeutics.Purinergic Signal2023
35687212Fluorescent A<sub>2A</sub> and A<sub>3</sub> adenosine receptor antagonists as flow cytometry probes.Purinergic Signal2023
37382926Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2Y<sub>14</sub> Receptor Antagonists.J Med Chem2023
37404375A<sub>2B</sub> adenosine receptor activation and modulation by protein kinase C.iScience2023
37034662Terpenes from <i>Cannabis sativa</i> Induce Antinociception in Mouse Chronic Neuropathic Pain via Activation of Spinal Cord Adenosine A<sub>2A</sub> Receptors.bioRxiv2023
37261289Editorial: Purinergic pharmacology, Volume II.Front Pharmacol2023
36926457Structural Optimization and Anticancer Activity of Polo-like Kinase 1 (Plk1) Polo-Box Domain (PBD) Inhibitors and Their Prodrugs.ACS Pharmacol Transl Sci2023
36781870Anionic phospholipids control mechanisms of GPCR-G protein recognition.Nat Commun2023
36781825In vivo phenotypic validation of adenosine receptor-dependent activity of non-adenosine drugs.Purinergic Signal2023
36538251Species dependence of A<sub>3</sub> adenosine receptor pharmacology and function.Purinergic Signal2023
32424811Adenosine A<sub>2A</sub> receptor antagonists: from caffeine to selective non-xanthines.Br J Pharmacol2022
35408685Development of Bicyclo[3.1.0]hexane-Based A<sub>3</sub> Receptor Ligands: Closing the Gaps in the Structure-Affinity Relationships.Molecules2022
35572558Optical Control of Adenosine A<sub>3</sub> Receptor Signaling: Towards a Multimodal Phototherapy in Psoriasis?Front Immunol2022
35395239Kinetic profiling and functional characterization of 8-phenylxanthine derivatives as A<sub>2B</sub> adenosine receptor antagonists.Biochem Pharmacol2022
35566035Pathophysiological Role and Medicinal Chemistry of A<sub>2A</sub> Adenosine Receptor Antagonists in Alzheimer's Disease.Molecules2022
35454173Synthesis and Effect of Conformationally Locked Carbocyclic Guanine Nucleotides on Dynamin.Biomolecules2022
35450351Selective A<sub>3</sub> Adenosine Receptor Antagonist Radioligand for Human and Rodent Species.ACS Med Chem Lett2022
35814244Machine Learning for Discovery of New ADORA Modulators.Front Pharmacol2022
36494860Novel alendronate-CGS21680 conjugate reduces bone resorption and induces new bone formation in post-menopausal osteoporosis and inflammatory osteolysis mouse models.Arthritis Res Ther2022
36150180Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2<i>H</i>-naphtho[1,2-<i>b</i>][1,4]diazepine-2,4(3<i>H</i>)-diones as P2X4 Receptor Antagonists.J Med Chem2022
36367749Structure-Activity Studies of 1<i>H</i>-Imidazo[4,5-<i>c</i>]quinolin-4-amine Derivatives as A<sub>3</sub> Adenosine Receptor Positive Allosteric Modulators.J Med Chem2022
36362112Adenosine A<sub>3</sub> Receptor (A<sub>3</sub>AR) Agonist for the Treatment of Bleomycin-Induced Lung Fibrosis in Mice.Int J Mol Sci2022
36268115Effects of Purinergic Receptor Deletion or Pharmacologic Modulation on Pulmonary Inflammation in Mice.ACS Pharmacol Transl Sci2022
35983277Characterization of Dual-Acting A<sub>3</sub> Adenosine Receptor Positive Allosteric Modulators That Preferentially Enhance Adenosine-Induced Gα<sub>i3</sub> and Gα<sub>oA</sub> Isoprotein Activation.ACS Pharmacol Transl Sci2022
36089113Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y<sub>6</sub> receptor antagonists.Bioorg Med Chem Lett2022
35977382GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A<sub>2A</sub> Adenosine Receptor.J Med Chem2022
36003949Stereospecific antiseizure activity in mouse and rat epilepsy models by a pyridinium inhibitor of TNFα/NFκB signaling.Eur J Med Chem Rep2022
35152062Interaction of A<sub>3</sub> adenosine receptor ligands with the human multidrug transporter ABCG2.Eur J Med Chem2022
35093182Targeting the A<sub>3</sub> adenosine receptor to prevent and reverse chemotherapy-induced neurotoxicities in mice.Acta Neuropathol Commun2022
35302044International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update.Pharmacol Rev2022
35113556Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y<sub>14</sub>R Antagonist.J Med Chem2022
35231671Adipocyte purinergic receptors activated by uracil nucleotides as obesity and type 2 diabetes targets.Curr Opin Pharmacol2022
35080883Structure-Activity Relationship of 3-Methylcytidine-5'-α,β-methylenediphosphates as CD73 Inhibitors.J Med Chem2022
35335209Dihydropyridines Potentiate ATP-Induced Currents Mediated by the Full-Length Human P2X5 Receptor.Molecules2022
34844790A<sub>3</sub> adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity.Eur J Med Chem2022
34844537A<sub>2A</sub> Adenosine Receptor Antagonists in Neurodegenerative Diseases.Curr Med Chem2022
34075613Spinal A<sub>3</sub> adenosine receptor activation acutely restores morphine antinociception in opioid tolerant male rats.J Neurosci Res2022
32794053Tribute to Prof. Geoffrey Burnstock: transition of purinergicsignaling to drug discovery.Purinergic Signal2021
35480676Convergent synthesis of 2-thioether-substituted (<i>N</i>)-methanocarba-adenosines as purine receptor agonists.RSC Adv2021
33792561UDP-glucose and P2Y14 receptor amplify allergen-induced airway eosinophilia.J Clin Invest2021
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Collaborators

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Co-authored papers 207
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iHuman Institute, ShanghaiTech University
Co-authored papers 18
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University of California San Francisco
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Uppsala University
Co-authored papers 8
Bridge Institute, University of Southern California
Co-authored papers 7
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Albert Einstein College of Medicine
Co-authored papers 4
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Co-authored papers 4
Co-authored papers 3
Henan Normal University
Co-authored papers 3
Co-authored papers 3
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Co-authored papers 3
Oregon Research Institute
Co-authored papers 2
University of Colorado School of Medicine
Co-authored papers 2
University of California San Diego.
Co-authored papers 2
ShanghaiTech University, China iHuman Institute
Co-authored papers 2
National Institutes of Health
Co-authored papers 2
iHuman Institute, ShanghaiTech University
Co-authored papers 2
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Co-authored papers 2
First Hospital of Shanxi Medical University, Shanxi Medical University
Co-authored papers 2
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Lawrence Berkeley National Laboratory
Co-authored papers 2
VA San Diego Healthcare System (VASDHS)
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National Institute of Biomedical Imaging and Bioengineering
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JiangYuan Hospital Affiliated to Jiangsu Institute of Nuclear Medicine
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University of California San Francisco
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