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  1. Dual N6/C7-Substituted 7-Deazapurine and Tricyclic Ribonucleosides with Affinity for G Protein-Coupled Receptors

    Article • ACS Medicinal Chemistry Letters, December 2023, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • European Journal of Medicinal Chemistry, November 2023, Elsevier

    Dr Kenneth A. Jacobson

  3. Synthesis and biological evaluation of carboxamide and quinoline derivatives as P2X7R antagonists

    Article • Bioorganic Chemistry, November 2023, Elsevier

    Dr Kenneth A. Jacobson

  4. Membrane Mimetic-Dependence of GPCR Energy Landscapes

    Article • October 2023, Cold Spring Harbor Laboratory Press

    Dr Kenneth A. Jacobson

  5. Anti-inflammatory potency of novel ecto-5′-nucleotidase/CD73 inhibitors in astrocyte culture model of neuroinflammation

    Article • European Journal of Pharmacology, October 2023, Elsevier

    Dr Kenneth A. Jacobson

  6. Assay-Dependent Inverse Agonism at the A3 Adenosine Receptor: When Neutral Is Not Neutral

    Article • ACS Pharmacology & Translational Science, August 2023, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson, Christophe Stove

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

    Article • ACS Pharmacology & Translational Science, August 2023, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  8. A2B adenosine receptor activation and modulation by protein kinase C

    Article • iScience, July 2023, Elsevier

    Dr Kenneth A. Jacobson

  9. New paradigms in purinergic receptor ligand discovery

    Article • Neuropharmacology, June 2023, Elsevier

    Dr Kenneth A. Jacobson

  10. Adenosine receptors in GtoPdb v.2023.1

    Article • IUPHAR/BPS Guide to Pharmacology CITE, April 2023, Edinburgh University Library

    Dr Kenneth A. Jacobson

  11. Covalently Binding Adenosine A3 Receptor Agonist ICBM Irreversibly Reduces Voltage-Gated Ca2+ Currents in Dorsal Root Ganglion Neurons

    Article • Purinergic Signalling, March 2023, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  12. The Ups and Downs in Drug Design: Adventures in Medicinal Chemistry. By Victor E. Marquez

    Article • ChemMedChem, January 2023, Wiley

    Dr Kenneth A. Jacobson

  13. Stereospecific antiseizure activity in mouse and rat epilepsy models by a pyridinium inhibitor of TNFα/NFκB signaling

    Article • European Journal of Medicinal Chemistry Reports, December 2022, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Journal of Medicinal Chemistry, November 2022, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  15. Adenosine A3 Receptor (A3AR) Agonist for the Treatment of Bleomycin-Induced Lung Fibrosis in Mice

    Article • International Journal of Molecular Sciences, November 2022, MDPI AG

    Dr Kenneth A. Jacobson

  16. Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y6 receptor antagonists

    Article • Bioorganic & Medicinal Chemistry Letters, November 2022, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • ACS Pharmacology & Translational Science, October 2022, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  18. Structure–Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2H-naphtho[1,2-b][1,4]diazepine-2,4(3H)-diones as P2X4 Receptor Antagonists

    Article • Journal of Medicinal Chemistry, September 2022, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • ACS Pharmacology & Translational Science, July 2022, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  20. A2A Adenosine Receptor Antagonists in Neurodegenerative Diseases

    Article • Current Medicinal Chemistry, June 2022, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  21. Fluorescent A2A and A3 adenosine receptor antagonists as flow cytometry probes

    Article • Purinergic Signalling, June 2022, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  22. Optical Control of Adenosine A3 Receptor Signaling: Towards a Multimodal Phototherapy in Psoriasis?

    Article • Frontiers in Immunology, April 2022, Frontiers

    Dr Kenneth A. Jacobson

  23. Pathophysiological Role and Medicinal Chemistry of A2A Adenosine Receptor Antagonists in Alzheimer’s Disease

    Article • Molecules, April 2022, MDPI AG

    Dr Kenneth A. Jacobson

  24. Synthesis and Effect of Conformationally Locked Carbocyclic Guanine Nucleotides on Dynamin

    Article • Biomolecules, April 2022, MDPI AG

    Dr Kenneth A. Jacobson

  25. Adipocyte purinergic receptors activated by uracil nucleotides as obesity and type 2 diabetes targets

    Article • Current Opinion in Pharmacology, April 2022, Elsevier

    Dr Kenneth A. Jacobson

  26. Development of Bicyclo[3.1.0]hexane-Based A3 Receptor Ligands: Closing the Gaps in the Structure–Affinity Relationships

    Article • Molecules, March 2022, MDPI AG

    Dr Kenneth A. Jacobson

  27. Dihydropyridines Potentiate ATP-Induced Currents Mediated by the Full-Length Human P2X5 Receptor

    Article • Molecules, March 2022, MDPI AG

    Dr Kenneth A. Jacobson

  28. Development of Bicyclo[3.1.0]hexane-based A<sub>3</sub> Receptor Ligands – Closing the Gaps in the Structure-affinity Relationships

    Article • March 2022, MDPI AG

    Dr Kenneth A. Jacobson

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

    Article • ACS Medicinal Chemistry Letters, March 2022, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  30. Targeting the A3 adenosine receptor to prevent and reverse chemotherapy-induced neurotoxicities in mice

    Article • Acta Neuropathologica Communications, January 2022, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  31. Structure–Activity Relationship of 3-Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors

    Article • Journal of Medicinal Chemistry, January 2022, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • European Journal of Medicinal Chemistry, January 2022, Elsevier

    Dr Kenneth A. Jacobson

  33. A3 adenosine receptor agonists containing dopamine Moieties for enhanced interspecies affinity

    Article • European Journal of Medicinal Chemistry, November 2021, Elsevier

    Christophe Stove, Dr Kenneth A. Jacobson

  34. 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

    Article • European Journal of Medicinal Chemistry, November 2021, Elsevier

    Dr Kenneth A. Jacobson

  35. Pharmacological characterization of DPTN and other selective A3 adenosine receptor antagonists

    Article • Purinergic Signalling, October 2021, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  36. Adenosine A1 receptor is dispensable for hepatocyte glucose metabolism and insulin sensitivity

    Article • Biochemical Pharmacology, October 2021, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • ACS Chemical Neuroscience, September 2021, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Journal of Medicinal Chemistry, August 2021, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  39. Purinergic Signaling in Liver Pathophysiology

    Article • Frontiers in Endocrinology, August 2021, Frontiers

    Dr Kenneth A. Jacobson

  40. Uncovering the Mechanisms of Adenosine Receptor-Mediated Pain Control: Focus on the A3 Receptor Subtype

    Article • International Journal of Molecular Sciences, July 2021, MDPI AG

    Dr Kenneth A. Jacobson

  41. Adenosine receptors in GtoPdb v.2021.2

    Article • IUPHAR/BPS Guide to Pharmacology CITE, June 2021, Edinburgh University Library

    Dr Kenneth A. Jacobson

  42. Spinal A 3 adenosine receptor activation acutely restores morphine antinociception in opioid tolerant male rats

    Article • Journal of Neuroscience Research, June 2021, Wiley

    Dr Kenneth A. Jacobson

  43. Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y6 receptor antagonists

    Article • Bioorganic & Medicinal Chemistry Letters, June 2021, Elsevier

    Dr Kenneth A. Jacobson

  44. Adipocyte P2Y14 receptors play a key role in regulating whole-body glucose and lipid homeostasis

    Article • JCI Insight, May 2021, American Society for Clinical Investigation

    Dr Kenneth A. Jacobson

  45. Purinergic signaling in diabetes and metabolism

    Article • Biochemical Pharmacology, May 2021, Elsevier

    Dr Kenneth A. Jacobson

  46. Adenosine Metabotropic Receptors in Chronic Pain Management

    Article • Frontiers in Pharmacology, April 2021, Frontiers

    Dr Kenneth A. Jacobson

  47. Design and Synthesis of 2,6-Disubstituted-4′-Selenoadenosine-5′-N,N-Dimethyluronamide Derivatives as Human A3 Adenosine Receptor Antagonists

    Article • Pharmaceuticals, April 2021, MDPI AG

    Dr Kenneth A. Jacobson

  48. UDP-glucose and P2Y14 receptor amplify allergen-induced airway eosinophilia

    Article • Journal of Clinical Investigation, April 2021, American Society for Clinical Investigation

    Dr Kenneth A. Jacobson

  49. Adenosine A3 agonists reverse neuropathic pain via T cell–mediated production of IL-10

    Article • Journal of Clinical Investigation, April 2021, American Society for Clinical Investigation

    Dr Kenneth A. Jacobson

  50. Adenosine A2A Receptors Are Upregulated in Peripheral Blood Mononuclear Cells from Atrial Fibrillation Patients

    Article • International Journal of Molecular Sciences, March 2021, MDPI AG

    Dr Kenneth A. Jacobson

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

    Article • ACS Medicinal Chemistry Letters, March 2021, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  52. Adenosine Kinase Expression Determines DNA Methylation in Cancer Cell Lines

    Article • ACS Pharmacology & Translational Science, February 2021, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • European Journal of Medicinal Chemistry, February 2021, Elsevier

    Dr Kenneth A. Jacobson

  54. Ligand design by targeting a binding site water

    Article • Chemical Science, January 2021, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

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

    Article • RSC Advances, January 2021, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  56. Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets

    Article • RSC Medicinal Chemistry, January 2021, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  57. Fragment-based design of selective GPCR ligands guided by free energy simulations

    Article • Chemical Communications, January 2021, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  58. Adenosine Receptors

    Article • January 2021, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  59. Purinergic GPCR transmembrane residues involved in ligand recognition and dimerization

    Article • January 2021, Elsevier

    Dr Kenneth A. Jacobson

  60. Activation of neuronal adenosine A1 receptors causes hypothermia through central and peripheral mechanisms

    Article • PLoS ONE, December 2020, PLOS

    Dr Kenneth A. Jacobson

  61. Structure activity relationship of novel antiviral nucleosides against Enterovirus A71

    Article • Bioorganic & Medicinal Chemistry Letters, December 2020, Elsevier

    Dr Kenneth A. Jacobson

  62. Lack of adipocyte purinergic P2Y 6 receptor greatly improves whole body glucose homeostasis

    Article • Proceedings of the National Academy of Sciences, November 2020, Proceedings of the National Academy of Sciences

    Dr Kenneth A. Jacobson

  63. Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1

    Article • Journal of Medicinal Chemistry, November 2020, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  64. Update of P2X receptor properties and their pharmacology: IUPHAR Review 30

    Article • British Journal of Pharmacology, October 2020, Wiley

    Dr Kenneth A. Jacobson

  65. Cover Feature: Purinergic Signaling: Impact of GPCR Structures on Rational Drug Design (ChemMedChem 21/2020)

    Article • ChemMedChem, October 2020, Wiley

    Dr Kenneth A. Jacobson

  66. Purinergic Signaling: Impact of GPCR Structures on Rational Drug Design

    Article • ChemMedChem, September 2020, Wiley

    Dr Kenneth A. Jacobson

  67. Tribute to Prof. Geoffrey Burnstock: transition of purinergicsignaling to drug discovery

    Article • Purinergic Signalling, August 2020, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  68. Design and in vivo activity of A3 adenosine receptor agonist prodrugs

    Article • Purinergic Signalling, July 2020, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  69. In Silico Drug Design for Purinergic GPCRs: Overview on Molecular Dynamics Applied to Adenosine and P2Y Receptors

    Article • Biomolecules, May 2020, MDPI AG

    Dr Kenneth A. Jacobson

  70. Chronic morphine-induced changes in signaling at the A3 adenosine receptor contribute to morphine-induced hyperalgesia, tolerance and withdrawal.

    Article • Journal of Pharmacology and Experimental Therapeutics, May 2020, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  71. A 2A adenosine receptor antagonists: From caffeine to selective non‐xanthines

    Article • British Journal of Pharmacology, May 2020, Wiley

    Dr Kenneth A. Jacobson

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

    Article • Cells, May 2020, MDPI AG

    Dr Kenneth A. Jacobson

  73. P2Y14 Receptor Antagonists Reverse Chronic Neuropathic Pain in a Mouse Model

    Article • ACS Medicinal Chemistry Letters, April 2020, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  74. Adenosine-Related Mechanisms in Non-Adenosine Receptor Drugs

    Article • Cells, April 2020, MDPI AG

    Dr Kenneth A. Jacobson

  75. Adenosine-Related Mechanisms in Non-Adenosine Receptor Drugs

    Article • April 2020, MDPI AG

    Dr Kenneth A. Jacobson

  76. Lack of Adipocyte Purinergic P2Y6 Receptor Greatly Improves Whole Body Glucose Homeostasis

    Article • April 2020, Cold Spring Harbor Laboratory Press

    Dr Kenneth A. Jacobson

  77. Peptide-Liganded G Protein-Coupled Receptors as Neurotherapeutics

    Article • ACS Pharmacology & Translational Science, March 2020, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Analytical Chemistry, March 2020, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, March 2020, Elsevier

    Christophe Stove, Dr Kenneth A. Jacobson

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

    Article • ACS Medicinal Chemistry Letters, February 2020, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  81. Update of P2Y Receptor Pharmacology: IUPHAR Review:27

    Article • British Journal of Pharmacology, February 2020, Wiley

    Dr Kenneth A. Jacobson

  82. Adenosine A1-A2A Receptor-Receptor Interaction: Contribution to Guanosine-Mediated Effects

    Article • Cells, December 2019, MDPI AG

    Dr Kenneth A. Jacobson

  83. A3 adenosine receptor activation mechanisms: molecular dynamics analysis of inactive, active, and fully active states

    Article • Journal of Computer-Aided Molecular Design, November 2019, Springer Science + Business Media

    Dr Kenneth A. Jacobson

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

    Article • European Journal of Medicinal Chemistry, November 2019, Elsevier

    Dr Kenneth A. Jacobson

  85. A2B Adenosine Receptor and Cancer

    Article • International Journal of Molecular Sciences, October 2019, MDPI AG

    Dr Kenneth A. Jacobson

  86. A2B Adenosine Receptor and Cancer

    Article • October 2019, MDPI AG

    Dr Kenneth A. Jacobson

  87. Adenosine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

    Article • IUPHAR/BPS Guide to Pharmacology CITE, September 2019, Edinburgh University Library

    Dr Kenneth A. Jacobson

  88. Survey of ribose ring pucker of signaling nucleosides and nucleotides

    Article • Nucleosides Nucleotides & Nucleic Acids, August 2019, Taylor & Francis

    Dr Kenneth A. Jacobson

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

    Article • Analytical Chemistry, June 2019, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  90. Evidence for the Interaction of A3 Adenosine Receptor Agonists at the Drug-Binding Site(s) of Human P-glycoprotein (ABCB1)

    Article • Molecular Pharmacology, May 2019, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  91. Deficiency of adenosine deaminase 2 triggers adenosine-mediated NETosis and TNF production in patients with DADA2

    Article • Blood, April 2019, American Society of Hematology

    Dr Kenneth A. Jacobson

  92. Physiology and effects of nucleosides in mice lacking all four adenosine receptors

    Article • PLoS Biology, March 2019, PLOS

    Dr Kenneth A. Jacobson

  93. Editorial: Purinergic Pharmacology

    Article • Frontiers in Pharmacology, January 2019, Frontiers

    Dr Kenneth A. Jacobson

  94. Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines to develop functionalized ligands to target adenosine receptors: fluorescent ligands as an example

    Article • MedChemComm, January 2019, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  95. Purinergic Pharmacology

    Article • January 2019, Frontiers

    Dr Kenneth A. Jacobson

  96. Probing Structure-Activity Relationship in β-Arrestin2 Recruitment of Diversely Substituted Adenosine Derivatives

    Article • Biochemical Pharmacology, October 2018, Elsevier

    Dr Kenneth A. Jacobson, Christophe Stove

  97. Remote control of movement disorders using a photoactive adenosine A 2A receptor antagonist

    Article • Journal of Controlled Release, August 2018, Elsevier

    Dr Kenneth A. Jacobson

  98. Author Correction: Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors

    Article • Scientific Reports, July 2018, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  99. Activation of basal forebrain purinergic P2 receptors promotes wakefulness in mice

    Article • Scientific Reports, July 2018, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  100. Thermostabilization and purification of the human dopamine transporter (hDAT) in an inhibitor and allosteric ligand bound conformation

    Article • PLoS ONE, July 2018, PLOS

    Dr Kenneth A. Jacobson

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

    Article • Journal of the American Chemical Society, June 2018, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Scientific Reports, May 2018, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  103. Structure-Guided Modification of Heterocyclic Antagonists of the P2Y14 Receptor

    Article • Journal of Medicinal Chemistry, May 2018, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  104. Activation of adenosine A 2A or A 2B receptors causes hypothermia in mice

    Article • Neuropharmacology, March 2018, Elsevier

    Dr Kenneth A. Jacobson

  105. Chemotherapy-induced pain is promoted by enhanced spinal adenosine kinase levels through astrocyte-dependent mechanisms

    Article • Pain, February 2018, Wolters Kluwer Health

    Dr Kenneth A. Jacobson

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

    Article • Structure, February 2018, Elsevier

    Dr Kenneth A. Jacobson

  107. A binding kinetics study of human adenosine A 3 receptor agonists

    Article • Biochemical Pharmacology, January 2018, Elsevier

    Dr Kenneth A. Jacobson

  108. Allosteric Coupling of Drug Binding and Intracellular Signaling in the A 2A Adenosine Receptor

    Article • Cell, January 2018, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • MedChemComm, January 2018, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  110. P2Y14 Receptor

    Article • January 2018, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  111. Purinergic Signaling in Mast Cell Degranulation and Asthma

    Article • Frontiers in Pharmacology, December 2017, Frontiers

    Dr Kenneth A. Jacobson

  112. Polypharmacology of conformationally locked methanocarba nucleosides

    Article • Drug Discovery Today, December 2017, Elsevier

    Dr Kenneth A. Jacobson

  113. Purinergic drug targets for gastrointestinal disorders

    Article • Current Opinion in Pharmacology, December 2017, Elsevier

    Dr Kenneth A. Jacobson

  114. Breakthrough in GPCR Crystallography and Its Impact on Computer-Aided Drug Design

    Article • November 2017, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  115. Demystifying P2Y1 Receptor Ligand Recognition through Docking and Molecular Dynamics Analyses

    Article • Journal of Chemical Information and Computer Sciences, November 2017, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Purinergic Signalling, November 2017, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  117. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor

    Article • Molecular Pharmacology, September 2017, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  118. Polypharmacology of N6-(3-Iodobenzyl)adenosine-5′-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Poten...

    Article • Journal of Medicinal Chemistry, August 2017, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  119. Fragment optimization for GPCRs by molecular dynamics free energy calculations: Probing druggable subpockets of the A 2A adenosine receptor binding site

    Article • Scientific Reports, July 2017, Nature

    Dr Kenneth A. Jacobson

  120. A3Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy

    Article • Medicinal Research Reviews, July 2017, Wiley

    Dr Kenneth A. Jacobson, Dr Mojgan Aghazadeh Tabrizi

  121. Highly selective A3 adenosine receptor agonists relieve chronic neuropathic pain

    Article • Expert Opinion on Therapeutic Patents, June 2017, Taylor & Francis

    Dr Kenneth A. Jacobson

  122. Exploring the Role of N6-Substituents in Potent Dual Acting 5′-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice

    Article • Journal of Medicinal Chemistry, May 2017, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Journal of Medicinal Chemistry, April 2017, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  124. (193) Contribution of IL-10 and T cells in beneficial effects exerted by A 3 adenosine receptor agonists in blocking and reversing neuropathic pain

    Article • Journal of Pain, April 2017, Elsevier

    Dr Kenneth A. Jacobson

  125. (192) Targeting A3 adenosine receptor in HIV-1 gp120-induced neuropathic pain

    Article • Journal of Pain, April 2017, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Journal of Medicinal Chemistry, March 2017, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  127. Structural Probing and Molecular Modeling of the A3 Adenosine Receptor: A Focus on Agonist Binding

    Article • Molecules, March 2017, MDPI AG

    Dr Kenneth A. Jacobson

  128. Hypothermia in mouse is caused by adenosine A1 and A3 receptor agonists and AMP via three distinct mechanisms

    Article • Neuropharmacology, March 2017, Elsevier

    Dr Kenneth A. Jacobson

  129. Pyrimidine nucleotides containing a (S)-methanocarba ring as P2Y6 receptor agonists

    Article • MedChemComm, January 2017, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  130. 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

    Article • MedChemComm, January 2017, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  131. Adenosine ☆

    Article • January 2017, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Journal of Medicinal Chemistry, December 2016, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  133. Ocular Purine Receptors as Drug Targets in the Eye

    Article • Journal of Ocular Pharmacology and Therapeutics, October 2016, Mary Ann Liebert Inc

    Dr Kenneth A. Jacobson

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

    Article • ACS Chemical Biology, August 2016, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  135. South (S)- and North (N)-Methanocarba-7-Deazaadenosine Analogues as Inhibitors of Human Adenosine Kinase

    Article • Journal of Medicinal Chemistry, July 2016, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  136. UDP-glucose promotes neutrophil recruitment in the lung

    Article • Purinergic Signalling, July 2016, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  137. Structure-Based Design of 3-(4-Aryl-1 H -1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y 14 Receptor Antagonists

    Article • Journal of Medicinal Chemistry, July 2016, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  138. Structure-Activity Analysis of Biased Agonism at the Human Adenosine A3 Receptor

    Article • Molecular Pharmacology, May 2016, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, May 2016, Elsevier

    Dr Kenneth A. Jacobson

  140. Purine ( N )-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A 3 Adenosine Receptor Agonists

    Article • Journal of Medicinal Chemistry, April 2016, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  141. Identification of A3adenosine receptor agonists as novel non-narcotic analgesics

    Article • British Journal of Pharmacology, March 2016, Wiley

    Dr Kenneth A. Jacobson

  142. Rigid Adenine Nucleoside Derivatives as Novel Modulators of the Human Sodium Symporters for Dopamine and Norepinephrine

    Article • Journal of Pharmacology and Experimental Therapeutics, January 2016, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  143. Characterization of polyamidoamino (PAMAM) dendrimers using in-line reversed phase LC electrospray ionization mass spectrometry

    Article • Analytical Methods, January 2016, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  144. Inherited dysfunctional platelet P2Y12 receptor mutations associated with bleeding disorders

    Article • Hämostaseologie, January 2016, Schattauer GmbH

    Dr Kenneth A. Jacobson

  145. New paradigms in GPCR drug discovery

    Article • Biochemical Pharmacology, December 2015, Elsevier

    Dr Kenneth A. Jacobson

  146. Medicinal chemistry of adenosine, P2Y and P2X receptors

    Article • Neuropharmacology, December 2015, Elsevier

    Dr Kenneth A. Jacobson

  147. The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors

    Article • British Journal of Pharmacology, December 2015, Wiley

    Dr Christopher Southan, Dr Anthony P Davenport, Dr Kenneth A. Jacobson, Stephen Alexander

  148. Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors

    Article • Journal of Pharmacology and Experimental Therapeutics, November 2015, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  149. Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands

    Article • Neuropharmacology, November 2015, Elsevier

    Dr Kenneth A. Jacobson

  150. Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y14 receptor

    Article • Bioorganic & Medicinal Chemistry Letters, November 2015, Elsevier

    Dr Kenneth A. Jacobson

  151. Metabolic mapping of A3 adenosine receptor agonist MRS5980

    Article • Biochemical Pharmacology, September 2015, Elsevier

    Dr Kenneth A. Jacobson

  152. Increased Signaling via Adenosine A1 Receptors, Sleep Deprivation, Imipramine, and Ketamine Inhibit Depressive-like Behavior via Induction of Homer1a

    Article • Neuron, August 2015, Elsevier

    Dr Kenneth A. Jacobson, Prof Andrea de Bartolomeis

  153. Modeling ligand recognition at the P2Y12 receptor in light of X-ray structural information

    Article • Journal of Computer-Aided Molecular Design, July 2015, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  154. Rigidified A 3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy

    Article • ACS Medicinal Chemistry Letters, July 2015, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  155. Molecular modeling of the human P2Y14 receptor: A template for structure-based design of selective agonist ligands

    Article • Bioorganic & Medicinal Chemistry, July 2015, Elsevier

    Dr Kenneth A. Jacobson

  156. Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain

    Article • Purinergic Signalling, June 2015, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  157. Correction: Ford et al., Engagement of the GABA to KCC2 Signaling Pathway Contributes to the Analgesic Effects of A3AR Agonists in Neuropathic Pain

    Article • Journal of Neuroscience, June 2015, Society for Neuroscience

    Dr Kenneth A. Jacobson

  158. Engagement of the GABA to KCC2 Signaling Pathway Contributes to the Analgesic Effects of A3AR Agonists in Neuropathic Pain

    Article • Journal of Neuroscience, April 2015, Society for Neuroscience

    Dr Kenneth A. Jacobson

  159. Nucleotides Acting at P2Y Receptors: Connecting Structure and Function

    Article • Molecular Pharmacology, April 2015, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  160. The human P2Y1 receptor in complex with BPTU

    Article • April 2015, Protein Data Bank, Rutgers University

    Dr Kenneth A. Jacobson

  161. The human P2Y1 receptor in complex with MRS2500

    Article • April 2015, Protein Data Bank, Rutgers University

    Dr Kenneth A. Jacobson

  162. Two disparate ligand-binding sites in the human P2Y1 receptor

    Article • Nature, March 2015, Nature

    Dr Kenneth A. Jacobson

  163. Renal Intercalated Cells Sense and Mediate Inflammation via the P2Y14 Receptor

    Article • PLoS ONE, March 2015, PLOS

    Dr Kenneth A. Jacobson

  164. Molecular Docking Screening Using Agonist-Bound GPCR Structures: Probing the A 2A Adenosine Receptor

    Article • Journal of Chemical Information and Computer Sciences, March 2015, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  165. Meet the Editorial Board

    Article • Current Topics in Medicinal Chemistry, February 2015, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  166. Spinal neuroimmune activation is independent of T-cell infiltration and attenuated by A3 adenosine receptor agonists in a model of oxaliplatin-induced peripheral neuropathy

    Article • Brain Behavior and Immunity, February 2015, Elsevier

    Dr Kenneth A. Jacobson

  167. Structure-based design, synthesis by click chemistry and in vivo activity of highly selective A3 adenosine receptor agonists

    Article • MedChemComm, January 2015, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

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

    Article • Computational and Structural Biotechnology Journal, January 2015, Elsevier

    Dr Kenneth A. Jacobson

  169. P2X4 receptor–eNOS signaling pathway in cardiac myocytes as a novel protective mechanism in heart failure

    Article • Computational and Structural Biotechnology Journal, January 2015, Elsevier

    Dr Kenneth A. Jacobson

  170. Enhancement of Glucose Uptake in Mouse Skeletal Muscle Cells and Adipocytes by P2Y6 Receptor Agonists

    Article • PLoS ONE, December 2014, PLOS

    Dr Kenneth A. Jacobson

  171. Exploring a 2-Naphthoic Acid Template for the Structure-Based Design of P2Y 14 Receptor Antagonist Molecular Probes

    Article • ACS Chemical Biology, December 2014, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  172. A Key Opinion Leader interview: insight into the research and career of Dr KA Jacobson

    Article • Expert Opinion on Therapeutic Patents, December 2014, Informa Healthcare

    Dr Kenneth A. Jacobson

  173. In Vivo Phenotypic Screening for Treating Chronic Neuropathic Pain: Modification of C 2-Arylethynyl Group of Conformationally Constrained A 3 Adenosine Receptor Agonists

    Article • Journal of Medicinal Chemistry, December 2014, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  174. Computational studies to predict or explain G protein coupled receptor polypharmacology

    Article • Trends in Pharmacological Sciences, December 2014, Elsevier

    Dr Kenneth A. Jacobson

  175. A3 adenosine receptor agonist prevents the development of paclitaxel-induced neuropathic pain by modulating spinal glial-restricted redox-dependent signaling pathways

    Article • Pain, December 2014, Wolters Kluwer Health

    Dr Kenneth A. Jacobson, Salvatore Cuzzocrea

  176. Identification of a new dysfunctional platelet P2Y12 receptor variant associated with bleeding diathesis

    Article • Blood, November 2014, American Society of Hematology

    Dr Kenneth A. Jacobson

  177. Uncovering Caffeine’s Adenosine A 2A Receptor Inverse Agonism in Experimental Parkinsonism

    Article • ACS Chemical Biology, November 2014, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  178. Endogenous adenosine A3 receptor activation selectively alleviates persistent pain states

    Article • Brain, November 2014, Oxford University Press (OUP)

    Dr Kenneth A. Jacobson

  179. Photomodulation of G Protein-Coupled Adenosine Receptors by a Novel Light-Switchable Ligand

    Article • Bioconjugate Chemistry, October 2014, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  180. Portraying G Protein-Coupled Receptors with Fluorescent Ligands

    Article • ACS Chemical Biology, September 2014, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  181. Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A 2A Adenosine Receptor

    Article • ACS Medicinal Chemistry Letters, September 2014, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Journal of the American Chemical Society, September 2014, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry, August 2014, Elsevier

    Dr Kenneth A. Jacobson

  184. Probing biased/partial agonism at the G protein-coupled A2B adenosine receptor

    Article • Biochemical Pharmacology, August 2014, Elsevier

    Dr Kenneth A. Jacobson

  185. Extended N6 substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor

    Article • Bioorganic & Medicinal Chemistry Letters, August 2014, Elsevier

    Dr Kenneth A. Jacobson

  186. Potential for Developing Purinergic Drugs for Gastrointestinal Diseases

    Article • Inflammatory Bowel Diseases, July 2014, Wolters Kluwer Health

    Dr Kenneth A. Jacobson

  187. Rapid Synthesis of Alkoxyamine Hydrochloride Derivatives from Alkyl Bromide andN,N′-Di-tert-butoxycarbonylhydroxylamine [(Boc)2NOH]

    Article • Synthetic Communications, June 2014, Taylor & Francis

    Dr Kenneth A. Jacobson

  188. Structural Probing of Off-Target G Protein-Coupled Receptor Activities within a Series of Adenosine/Adenine Congeners

    Article • PLoS ONE, May 2014, PLOS

    Dr Kenneth A. Jacobson

  189. 4-Alkyloxyimino Derivatives of Uridine-5′-triphosphate: Distal Modification of Potent Agonists as a Strategy for Molecular Probes of P2Y 2 , P2Y 4 , and P2Y 6 Receptors

    Article • Journal of Medicinal Chemistry, May 2014, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  190. Agonist-bound structure of the human P2Y12 receptor

    Article • Nature, April 2014, Springer Science + Business Media

    Dr Kenneth A. Jacobson

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

    Article • March 2014, Protein Data Bank, Rutgers University

    Dr Kenneth A. Jacobson

  192. Structure of P2Y12 Receptor

    Article • Nature, March 2014, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  193. Novel Protective Role of Endogenous Cardiac Myocyte P2X4 Receptors in Heart Failure

    Article • Circulation Heart Failure, March 2014, Wolters Kluwer Health

    Dr Kenneth A. Jacobson

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

    Article • Purinergic Signalling, March 2014, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  195. Synthesis and Anti-Renal Fibrosis Activity of Conformationally Locked Truncated 2-Hexynyl- N 6 -Substituted-( N )-Methanocarba-nucleosides as A 3 Adenosine Receptor Antagonists and Partial Agonists

    Article • Journal of Medicinal Chemistry, February 2014, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  196. A3Adenosine Receptor Allosteric Modulator Induces an Anti-Inflammatory Effect:In VivoStudies and Molecular Mechanism of Action

    Article • Mediators of Inflammation, January 2014, Hindawi Publishing Corporation

    Dr Kenneth A. Jacobson

  197. Rational Design of Sulfonated A 3 Adenosine Receptor-Selective Nucleosides as Pharmacological Tools To Study Chronic Neuropathic Pain

    Article • Journal of Medicinal Chemistry, July 2013, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  198. P2Y2 receptor agonist with enhanced stability protects the heart from ischemic damage in vitro and in vivo

    Article • Purinergic Signalling, July 2013, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  199. Dopamine D2 receptor-mediated modulation of adenosine A2A receptor agonist binding within the A2AR/D2R oligomer framework

    Article • Neurochemistry International, July 2013, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Drug Discovery Today Technologies, June 2013, Elsevier

    Dr Kenneth A. Jacobson

  201. The Therapeutic Effect of 2-Cyclohexylthio-AMP in Heart Failure

    Article • Journal of Cardiovascular Pharmacology, June 2013, Wolters Kluwer Health

    Dr Kenneth A. Jacobson

  202. Structure-Based Approaches to Ligands for G-Protein-Coupled Adenosine and P2Y Receptors, from Small Molecules to Nanoconjugates †

    Article • Journal of Medicinal Chemistry, May 2013, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  203. Reply to: ‘The discovery of a new class of synaptic transmitters in smooth muscle fifty years ago and amelioration of coronary artery thrombosis’

    Article • Acta Physiologica, April 2013, Wiley

    Dr Kenneth A. Jacobson

  204. A Selective High-Affinity Antagonist of the P2Y14 Receptor Inhibits UDP-Glucose–Stimulated Chemotaxis of Human Neutrophils

    Article • Molecular Pharmacology, April 2013, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  205. Characterization by flow cytometry of fluorescent, selective agonist probes of the A3 adenosine receptor

    Article • Biochemical Pharmacology, April 2013, Elsevier

    Dr Kenneth A. Jacobson

  206. AMP-activated protein kinase as regulator of P2Y6 receptor-induced insulin secretion in mouse pancreatic β-cells

    Article • Biochemical Pharmacology, April 2013, Elsevier

    Dr Kenneth A. Jacobson

  207. 5′-Phosphate and 5′-Phosphonate Ester Derivatives of (N)-Methanocarba Adenosine with in Vivo Cardioprotective Activity

    Article • Journal of Medicinal Chemistry, February 2013, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  208. A2B adenosine receptor blockade inhibits growth of prostate cancer cells

    Article • Purinergic Signalling, January 2013, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  209. Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches

    Article • MedChemComm, January 2013, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  210. Additions and corrections and MedChemWatch Issue 19

    Article • MedChemComm, January 2013, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  211. 4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2Y6 receptor

    Article • MedChemComm, January 2013, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  212. Probing GPCR Structure

    Article • January 2013, Elsevier

    Dr Kenneth A. Jacobson

  213. Fluorescent ligands for adenosine receptors

    Article • Bioorganic & Medicinal Chemistry Letters, January 2013, Elsevier

    Dr Kenneth A. Jacobson, Stephanie Federico

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

    Article • PLoS ONE, November 2012, PLOS

    Dr Kenneth A. Jacobson

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

    Article • Purinergic Signalling, November 2012, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  216. Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R

    Article • Journal of Neurochemistry, September 2012, Wiley

    Dr Kenneth A. Jacobson, Dr. Dasiel Oscar Borroto Escuela, Professor Kjell Fuxe

  217. Structural Sweet Spot for A 1 Adenosine Receptor Activation by Truncated (N)-Methanocarba Nucleosides: Receptor Docking and Potent Anticonvulsant Activity

    Article • Journal of Medicinal Chemistry, September 2012, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  218. Structure–Activity Relationships and Molecular Modeling of 1,2,4-Triazoles as Adenosine Receptor Antagonists

    Article • ACS Medicinal Chemistry Letters, September 2012, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  219. Molecular structure of P2Y receptors: mutagenesis, modeling, and chemical probes

    Article • Wiley Interdisciplinary Reviews Membrane Transport and Signalling, September 2012, Wiley

    Dr Kenneth A. Jacobson

  220. Virtual screening leads to the discovery of novel non-nucleotide P2Y1 receptor antagonists

    Article • Bioorganic & Medicinal Chemistry, September 2012, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Purinergic Signalling, July 2012, Springer Science + Business Media

    Dr Kenneth A. Jacobson

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

    Article • ACS Medicinal Chemistry Letters, July 2012, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  223. New Insights for Drug Design from the X-Ray Crystallographic Structures of G-Protein-Coupled Receptors

    Article • Molecular Pharmacology, June 2012, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  224. Novel fluorescent antagonist as a molecular probe in A3 adenosine receptor binding assays using flow cytometry

    Article • Biochemical Pharmacology, June 2012, Elsevier

    Dr Kenneth A. Jacobson

  225. Farnesyl pyrophosphate is an endogenous antagonist to ADP-stimulated P2Y12 receptor-mediated platelet aggregation

    Article • Thrombosis and Haemostasis, May 2012, Schattauer GmbH

    Dr Kenneth A. Jacobson

  226. Structure-Guided Design of A 3 Adenosine Receptor-Selective Nucleosides: Combination of 2-Arylethynyl and Bicyclo[3.1.0]hexane Substitutions

    Article • Journal of Medicinal Chemistry, May 2012, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  227. Optimization of Adenosine 5′-Carboxamide Derivatives as Adenosine Receptor Agonists Using Structure-Based Ligand Design and Fragment Screening

    Article • Journal of Medicinal Chemistry, May 2012, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  228. Synthesis and P2Y2 receptor agonist activities of uridine 5′-phosphonate analogues

    Article • Bioorganic & Medicinal Chemistry, April 2012, Elsevier

    Dr Kenneth A. Jacobson

  229. Pharmacological and therapeutic effects of A3 adenosine receptor agonists

    Article • Drug Discovery Today, April 2012, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Pharmacological Research, March 2012, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Purinergic Signalling, February 2012, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  232. Controlling murine and rat chronic pain through A 3 adenosine receptor activation

    Article • The FASEB Journal, February 2012, Wiley

    Dr Kenneth A. Jacobson

  233. Click Modification in the N 6 Region of A 3 Adenosine Receptor-Selective Carbocyclic Nucleosides for Dendrimeric Tethering that Preserves Pharmacophore Recognition

    Article • Bioconjugate Chemistry, February 2012, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  234. Structure–Activity Relationships of Truncated C2- or C8-Substituted Adenosine Derivatives as Dual Acting A 2A and A 3 Adenosine Receptor Ligands

    Article • Journal of Medicinal Chemistry, January 2012, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  235. Evaluation of Molecular Modeling of Agonist Binding in Light of the Crystallographic Structure of an Agonist-Bound A2A Adenosine Receptor

    Article • Journal of Medicinal Chemistry, December 2011, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  236. Emerging adenosine receptor agonists – an update

    Article • Expert Opinion on Emerging Drugs, December 2011, Informa Healthcare

    Dr Kenneth A. Jacobson

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

    Article • Journal of Pharmacology and Experimental Therapeutics, October 2011, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  238. Small Molecule Positive Allosteric Modulation of TRPV1 Activation by Vanilloids and Acidic pH

    Article • Journal of Pharmacology and Experimental Therapeutics, October 2011, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  239. Functionally biased modulation of A3 adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers

    Article • Biochemical Pharmacology, September 2011, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • ACS Medicinal Chemistry Letters, August 2011, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  241. Striatal adenosine A2A receptor-mediated positron emission tomographic imaging in 6-hydroxydopamine-lesioned rats using [18F]-MRS5425

    Article • Nuclear Medicine and Biology, August 2011, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, August 2011, Elsevier

    Dr Kenneth A. Jacobson

  243. Pyrimidine Nucleotides with 4-Alkyloxyimino and Terminal Tetraphosphate δ-Ester Modifications as Selective Agonists of the P2Y 4 Receptor

    Article • Journal of Medicinal Chemistry, June 2011, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  244. GPCR Ligand Dendrimer (GLiDe) Conjugates: Adenosine Receptor Interactions of a Series of Multivalent Xanthine Antagonists

    Article • Bioconjugate Chemistry, June 2011, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  245. CF102 an A3 adenosine receptor agonist mediates anti-tumor and anti-inflammatory effects in the liver

    Article • Journal of Cellular Physiology, June 2011, Wiley

    Dr Kenneth A. Jacobson

  246. Article • Bulletin of the Korean Chemical Society, May 2011, Korean Chemical Society

    Dr Kenneth A. Jacobson

  247. Recent developments in adenosine receptor ligands and their potential as novel drugs

    Article • Biochimica et Biophysica Acta (BBA) - Biomembranes, May 2011, Elsevier

    Dr Kenneth A. Jacobson

  248. 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

    Article • Bioorganic & Medicinal Chemistry Letters, May 2011, Elsevier

    Dr Kenneth A. Jacobson

  249. Predicted structures of agonist and antagonist bound complexes of adenosine A3 receptor

    Article • Proteins Structure Function and Bioinformatics, April 2011, Wiley

    Dr Kenneth A. Jacobson

  250. Comparison of three GPCR structural templates for modeling of the P2Y12 nucleotide receptor

    Article • Journal of Computer-Aided Molecular Design, April 2011, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  251. Structure of an Agonist-Bound Human A2A Adenosine Receptor

    Article • Science, March 2011, American Association for the Advancement of Science

    Dr Kenneth A. Jacobson

  252. Pharmacochemistry of the platelet purinergic receptors

    Article • Purinergic Signalling, February 2011, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  253. 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

    Article • Journal of Medicinal Chemistry, February 2011, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  254. International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update

    Article • Pharmacological Reviews, February 2011, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  255. Regio- and stereoselective synthesis of truncated 3′-aminocarbanucleosides and their binding affinity at the A3 adenosine receptor

    Article • Organic & Biomolecular Chemistry, January 2011, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  256. Preface

    Article • January 2011, Elsevier

    Dr Kenneth A. Jacobson

  257. Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts

    Article • BMC Pharmacology, January 2011, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  258. Allosteric Modulation of Purine and Pyrimidine Receptors

    Article • January 2011, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • ACS Medicinal Chemistry Letters, December 2010, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  260. P2Y13 receptor is responsible for ADP-mediated degranulation in RBL-2H3 rat mast cells

    Article • Pharmacological Research, December 2010, Elsevier

    Dr Kenneth A. Jacobson

  261. GPCR ligand–dendrimer (GLiDe) conjugates: future smart drugs?

    Article • Trends in Pharmacological Sciences, December 2010, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry Letters, October 2010, Elsevier

    Dr Kenneth A. Jacobson

  263. Quantification of recombinant and platelet P2Y1 receptors utilizing a [125I]-labeled high-affinity antagonist 2-iodo-N6-methyl-(N)-methanocarba-2′-deoxyadenosine-3′,5′-bisphosphate ([125I]MRS2500)

    Article • Pharmacological Research, October 2010, Elsevier

    Dr Kenneth A. Jacobson

  264. Design, synthesis, and binding of homologated truncated 4′-thioadenosine derivatives at the human A3 adenosine receptors

    Article • Bioorganic & Medicinal Chemistry, October 2010, Elsevier

    Dr Kenneth A. Jacobson

  265. Adenine nucleotide control of coronary blood flow during exercise

    Article • AJP Heart and Circulatory Physiology, September 2010, American Physiological Society

    Dr Kenneth A. Jacobson

  266. Dexamethasone Enhances ATP-Induced Inflammatory Responses in Endothelial Cells

    Article • Journal of Pharmacology and Experimental Therapeutics, September 2010, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  267. Stimulation of the P2X7 receptor kills rat retinal ganglion cells in vivo

    Article • Experimental Eye Research, September 2010, Elsevier

    Dr Kenneth A. Jacobson

  268. Xanthines as Adenosine Receptor Antagonists

    Article • August 2010, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  269. Novel Alexa Fluor-488 labeled antagonist of the A2A adenosine receptor: Application to a fluorescence polarization-based receptor binding assay

    Article • Biochemical Pharmacology, August 2010, Elsevier

    Dr Kenneth A. Jacobson

  270. Functionalized Congeners of P2Y 1 Receptor Antagonists: 2-Alkynyl ( N )-Methanocarba 2′-Deoxyadenosine 3′,5′-Bisphosphate Analogues and Conjugation to a Polyamidoamine (PAMAM) Dendrimer Carrier

    Article • Bioconjugate Chemistry, July 2010, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  271. Treatment of Dry Eye Syndrome with Orally Administered CF101

    Article • Ophthalmology, July 2010, Elsevier

    Dr Kenneth A. Jacobson

  272. P2Y nucleotide receptors: promise of therapeutic applications

    Article • Drug Discovery Today, July 2010, Elsevier

    Dr Kenneth A. Jacobson

  273. Multivalent dendrimeric and monomeric adenosine agonists attenuate cell death in HL-1 mouse cardiomyocytes expressing the A3 receptor

    Article • Biochemical Pharmacology, July 2010, Elsevier

    Dr Kenneth A. Jacobson

  274. Pyrimidine Ribonucleotides with Enhanced Selectivity as P2Y 6 Receptor Agonists: Novel 4-Alkyloxyimino, (S)-Methanocarba, and 5′-Triphosphate γ-Ester Modifications †

    Article • Journal of Medicinal Chemistry, June 2010, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  275. Structure-Based Discovery of A 2A Adenosine Receptor Ligands

    Article • Journal of Medicinal Chemistry, May 2010, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  276. Activation of distinct P2Y receptor subtypes stimulates insulin secretion in MIN6 mouse pancreatic β cells

    Article • Biochemical Pharmacology, May 2010, Elsevier

    Dr Kenneth A. Jacobson

  277. 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

    Article • Bioorganic & Medicinal Chemistry, April 2010, Elsevier

    Dr Kenneth A. Jacobson

  278. Synthesis and pharmacological characterization of [125I]MRS5127, a high affinity, selective agonist radioligand for the A3 adenosine receptor

    Article • Biochemical Pharmacology, April 2010, Elsevier

    Dr Kenneth A. Jacobson

  279. Structure−Activity Relationship of (N)-Methanocarba Phosphonate Analogues of 5′-AMP as Cardioprotective Agents Acting Through a Cardiac P2X Receptor

    Article • Journal of Medicinal Chemistry, March 2010, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  280. Treatment of Heart Failure by a Methanocarba Derivative of Adenosine Monophosphate: Implication for a Role of Cardiac Purinergic P2X Receptors

    Article • Journal of Pharmacology and Experimental Therapeutics, March 2010, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  281. UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation

    Article • Biochemical Pharmacology, March 2010, Elsevier

    Dr Kenneth A. Jacobson

  282. Polyamidoamine (PAMAM) Dendrimer Conjugates of “Clickable” Agonists of the A 3 Adenosine Receptor and Coactivation of the P2Y 14 Receptor by a Tethered Nucleotide

    Article • Bioconjugate Chemistry, February 2010, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  283. Human P2Y 14 Receptor Agonists: Truncation of the Hexose Moiety of Uridine-5′-Diphosphoglucose and Its Replacement with Alkyl and Aryl Groups

    Article • Journal of Medicinal Chemistry, January 2010, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  284. The A3 adenosine receptor attenuates the calcium rise triggered by NMDA receptors in retinal ganglion cells

    Article • Neurochemistry International, January 2010, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Experimental Eye Research, January 2010, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Journal of Nanobiotechnology, January 2010, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  287. 2-Dialkynyl derivatives of (N)-methanocarba nucleosides: ‘Clickable’ A3 adenosine receptor-selective agonists

    Article • Bioorganic & Medicinal Chemistry, January 2010, Elsevier

    Dr Kenneth A. Jacobson

  288. Functionalized Congeners of A 3 Adenosine Receptor-Selective Nucleosides Containing a Bicyclo[3.1.0]hexane Ring System †

    Article • Journal of Medicinal Chemistry, December 2009, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  289. Rhodopsin and the Others: A Historical Perspective on Structural Studies of G Protein-Coupled Receptors

    Article • Current Pharmaceutical Design, December 2009, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  290. Design and synthesis of N6-substituted-4′-thioadenosine-5′-uronamides as potent and selective human A3 adenosine receptor agonists

    Article • Bioorganic & Medicinal Chemistry, December 2009, Elsevier

    Dr Kenneth A. Jacobson

  291. Molecular Modeling and Reengineering of A3 Adenosine Receptors

    Article • November 2009, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  292. Adenosine A3 Receptors in Muscle Protection

    Article • November 2009, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  293. A3 Adenosine Receptor Agonists: History and Future Perspectives

    Article • November 2009, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  294. PEGylated Dendritic Unimolecular Micelles as Versatile Carriers for Ligands of G Protein-Coupled Receptors

    Article • Bioconjugate Chemistry, October 2009, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  295. Functionalized Congener Approach to the Design of Ligands for G Protein-Coupled Receptors (GPCRs)

    Article • Bioconjugate Chemistry, October 2009, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  296. Quantification of Gi-Mediated Inhibition of Adenylyl Cyclase Activity Reveals That UDP Is a Potent Agonist of the Human P2Y14 Receptor

    Article • Molecular Pharmacology, September 2009, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  297. Enhanced Potency of Nucleotide−Dendrimer Conjugates as Agonists of the P2Y 14 Receptor: Multivalent Effect in G Protein-Coupled Receptor Recognition

    Article • Bioconjugate Chemistry, August 2009, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  298. Molecular recognition in the P2Y14 receptor: Probing the structurally permissive terminal sugar moiety of uridine-5′-diphosphoglucose

    Article • Bioorganic & Medicinal Chemistry, July 2009, Elsevier

    Dr Kenneth A. Jacobson

  299. Synthesis and P2Y receptor activity of nucleoside 5′-phosphonate derivatives

    Article • Bioorganic & Medicinal Chemistry Letters, June 2009, Elsevier

    Dr Kenneth A. Jacobson

  300. Evaluation of Homology Modeling of G-Protein-Coupled Receptors in Light of the A 2A Adenosine Receptor Crystallographic Structure

    Article • Journal of Medicinal Chemistry, May 2009, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry, May 2009, Elsevier

    Dr Kenneth A. Jacobson

  302. Novel 2- and 4-Substituted 1 H -Imidazo[4,5- c ]quinolin-4-amine Derivatives as Allosteric Modulators of the A 3 Adenosine Receptor

    Article • Journal of Medicinal Chemistry, April 2009, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  303. Involvement of UTP in protection of cardiomyocytes from hypoxic stressThis article is one of a selection of papers from the NATO Advanced Research Workshop on Translational Knowledge for Heart Health (published in part 2 of a 2-part Special Issue).

    Article • Canadian Journal of Physiology and Pharmacology, April 2009, Canadian Science Publishing

    Dr Kenneth A. Jacobson

  304. Small molecule blockers of the Alzheimer Aβ calcium channel potently protect neurons from Aβ cytotoxicity

    Article • Proceedings of the National Academy of Sciences, March 2009, Proceedings of the National Academy of Sciences

    Dr Kenneth A. Jacobson

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

    Article • Nuclear Medicine and Biology, January 2009, Elsevier

    Dr Kenneth A. Jacobson

  306. Nucleoside-based A3 adenosine receptor antagonists as drug candidates

    Article • Drugs of the Future, January 2009, Prous Science

    Dr Kenneth A. Jacobson

  307. Medicinal Chemistry of the A3 Adenosine Receptor: Agonists, Antagonists, and Receptor Engineering

    Article • January 2009, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  308. John W. Daly – An Appreciation

    Article • Heterocycles, January 2009, Japan Institute of Heterocyclic Chemistry

    Dr Kenneth A. Jacobson

  309. Introduction to Adenosine Receptors as Therapeutic Targets

    Article • January 2009, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  310. Corrigendum to “Synthesis and structure–activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor” [Bioorg. Med. Chem. Lett. 18 (2008) 571–575]

    Article • Bioorganic & Medicinal Chemistry Letters, January 2009, Elsevier

    Dr Kenneth A. Jacobson

  311. Adenosine Receptors: The Contributions by John W. Daly

    Article • Heterocycles, January 2009, Japan Institute of Heterocyclic Chemistry

    Dr Kenneth A. Jacobson

  312. Adenosine

    Article • January 2009, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • BMC Pharmacology, December 2008, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  314. Conformational changes involved in G-protein-coupled-receptor activation

    Article • Trends in Pharmacological Sciences, December 2008, Elsevier

    Dr Kenneth A. Jacobson

  315. Structure−Activity Relationships of Truncated d - and l -4′-Thioadenosine Derivatives as Species-Independent A 3 Adenosine Receptor Antagonists(1)

    Article • Journal of Medicinal Chemistry, October 2008, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  316. Synthesis of Enantiomerically Pure ( S )-Methanocarbaribo Uracil Nucleoside Derivatives for Use as Antiviral Agents and P2Y Receptor Ligands

    Article • The Journal of Organic Chemistry, October 2008, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  317. Structure–activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1)

    Article • Bioorganic & Medicinal Chemistry, October 2008, Elsevier

    Dr Kenneth A. Jacobson

  318. Evidence for the possible involvement of the P2Y6 receptor in Ca2+ mobilization and insulin secretion in mouse pancreatic islets

    Article • Purinergic Signalling, September 2008, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  319. Selective A3 adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system

    Article • Bioorganic & Medicinal Chemistry, September 2008, Elsevier

    Dr Kenneth A. Jacobson

  320. Attenuation of apoptosis in vitro and ischemia/reperfusion injury in vivo in mouse skeletal muscle by P2Y6 receptor activation

    Article • Pharmacological Research, September 2008, Elsevier

    Dr Kenneth A. Jacobson

  321. The A3 adenosine receptor agonist CF502 inhibits the PI3K, PKB/Akt and NF-κB signaling pathway in synoviocytes from rheumatoid arthritis patients and in adjuvant-induced arthritis rats

    Article • Biochemical Pharmacology, August 2008, Elsevier

    Dr Kenneth A. Jacobson

  322. Systematic Investigation of Polyamidoamine Dendrimers Surface-Modified with Poly(ethylene glycol) for Drug Delivery Applications: Synthesis, Characterization, and Evaluation of Cytotoxicity

    Article • Bioconjugate Chemistry, August 2008, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  323. Molecular modeling of a PAMAM-CGS21680 dendrimer bound to an A2A adenosine receptor homodimer

    Article • Bioorganic & Medicinal Chemistry Letters, August 2008, Elsevier

    Dr Kenneth A. Jacobson

  324. Lung Injury after In Vivo Reperfusion

    Article • Anesthesiology, August 2008, Wolters Kluwer Health

    Dr Kenneth A. Jacobson

  325. Adenosine A2A receptor dynamics studied with the novel fluorescent agonist Alexa488-APEC

    Article • European Journal of Pharmacology, August 2008, Elsevier

    Dr Kenneth A. Jacobson

  326. Preface: special issue on medicinal chemistry of purines

    Article • Purinergic Signalling, July 2008, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  327. Development of selective agonists and antagonists of P2Y receptors

    Article • Purinergic Signalling, July 2008, Springer Science + Business Media

    Dr Kenneth A. Jacobson

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

    Article • Purinergic Signalling, July 2008, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  329. Development of Selective High Affinity Antagonists, Agonists, and Radioligands for the P2Y1 Receptor

    Article • Combinatorial Chemistry & High Throughput Screening, July 2008, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  330. Role of P2X purinergic receptors in the rescue of ischemic heart failure

    Article • AJP Heart and Circulatory Physiology, June 2008, American Physiological Society

    Dr Kenneth A. Jacobson

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

    Article • Purinergic Signalling, June 2008, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  332. Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists

    Article • Bioorganic & Medicinal Chemistry, June 2008, Elsevier

    Dr Kenneth A. Jacobson

  333. Ligand and structure-based methodologies for the prediction of the activity of G protein-coupled receptor ligands

    Article • Journal of Computer-Aided Molecular Design, May 2008, Springer Science + Business Media

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry Letters, May 2008, Elsevier

    Dr Kenneth A. Jacobson

  335. Synthesis of 3′-Acetamidoadenosine Derivatives as Potential A3Adenosine Receptor Agonists

    Article • Nucleosides Nucleotides & Nucleic Acids, April 2008, Taylor & Francis

    Dr Kenneth A. Jacobson

  336. Translocation of arrestin induced by human A3 adenosine receptor ligands in an engineered cell line: Comparison with G protein-dependent pathways

    Article • Pharmacological Research, April 2008, Elsevier

    Dr Kenneth A. Jacobson

  337. Probing Distal Regions of the A 2B Adenosine Receptor by Quantitative Structure−Activity Relationship Modeling of Known and Novel Agonists

    Article • Journal of Medicinal Chemistry, April 2008, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry Letters, March 2008, Elsevier

    Dr Kenneth A. Jacobson

  339. Ligand-Specific Changes in M 3 Muscarinic Acetylcholine Receptor Structure Detected by a Disulfide Scanning Strategy †

    Article • Biochemistry, March 2008, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, March 2008, Elsevier

    Dr Kenneth A. Jacobson

  341. Synthesis of Ethyl (1S,2R,3S,4S,5S)-2,3-O-(Isopropylidene)-4-Hydroxy-Bicyclo[3.1.0]Hexane-Carboxylate from L-Ribose: A Versatile Chiral Synthon for Preparation of Adenosine and P2 Receptor Ligands

    Article • Nucleosides Nucleotides & Nucleic Acids, February 2008, Taylor & Francis

    Dr Kenneth A. Jacobson

  342. UDP Is a Competitive Antagonist at the Human P2Y14 Receptor

    Article • Journal of Pharmacology and Experimental Therapeutics, February 2008, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  343. Toward Multivalent Signaling across G Protein-Coupled Receptors from Poly(amidoamine) Dendrimers

    Article • Bioconjugate Chemistry, February 2008, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  344. Synthesis and structure–activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor

    Article • Bioorganic & Medicinal Chemistry Letters, January 2008, Elsevier

    Dr Kenneth A. Jacobson

  345. Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates

    Article • Journal of Nanobiotechnology, January 2008, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  346. Erratum

    Article • Nucleosides Nucleotides & Nucleic Acids, January 2008, Taylor & Francis

    Dr Kenneth A. Jacobson

  347. Synthesis ofN6-Substituted 3′-Ureidoadenosine Derivatives as Highly Potent Agonists at the Mutant A3Adenosine Receptor

    Article • Nucleosides Nucleotides & Nucleic Acids, November 2007, Taylor & Francis

    Dr Kenneth A. Jacobson

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

    Article • Nucleosides Nucleotides & Nucleic Acids, November 2007, Taylor & Francis

    Dr Kenneth A. Jacobson

  349. Design, Synthesis, and Anti-Tumor Activity of 4′-Thionucleosides as Potent and Selective Agonists at the Human A3Adenosine Receptor

    Article • Nucleosides Nucleotides & Nucleic Acids, November 2007, Taylor & Francis

    Dr Kenneth A. Jacobson

  350. Protective roles of adenosine A1, A2A, and A3 receptors in skeletal muscle ischemia and reperfusion injury

    Article • AJP Heart and Circulatory Physiology, October 2007, American Physiological Society

    Dr Kenneth A. Jacobson

  351. Role of adenosine A3 receptors on CA1 hippocampal neurotransmission during oxygen–glucose deprivation episodes of different duration

    Article • Biochemical Pharmacology, September 2007, Elsevier

    Dr Kenneth A. Jacobson

  352. Emerging adenosine receptor agonists

    Article • Expert Opinion on Emerging Drugs, September 2007, Informa Healthcare

    Dr Kenneth A. Jacobson

  353. The Anti-Cancer Effect of A3 Adenosine Receptor Agonists: A Novel, Targeted Therapy

    Article • Immunology Endocrine & Metabolic Agents - Medicinal Chemistry, August 2007, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  354. Distinct Structural Changes in a G Protein-coupled Receptor Caused by Different Classes of Agonist Ligands

    Article • Journal of Biological Chemistry, July 2007, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  355. P2Y 1 Antagonists:  Combining Receptor-Based Modeling and QSAR for a Quantitative Prediction of the Biological Activity Based on Consensus Scoring

    Article • Journal of Medicinal Chemistry, July 2007, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  356. Effects of Soil Sample Grinding Intensity on Carbon Determination by High‐Temperature Combustion

    Article • Communications in Soil Science and Plant Analysis, July 2007, Taylor & Francis

    Dr Kenneth A. Jacobson

  357. Discovery of a New Nucleoside Template for Human A 3 Adenosine Receptor Ligands:  d -4‘-Thioadenosine Derivatives without 4‘-Hydroxymethyl Group as Highly Potent and Selective Antagonists

    Article • Journal of Medicinal Chemistry, July 2007, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  358. Barrier qualities of the mouse eye to topically applied drugs

    Article • Experimental Eye Research, July 2007, Elsevier

    Dr Kenneth A. Jacobson

  359. Probing the Binding Site of the A 1 Adenosine Receptor Reengineered for Orthogonal Recognition by Tailored Nucleosides †

    Article • Biochemistry, June 2007, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  360. Three-Dimensional Quantitative Structure−Activity Relationship of Nucleosides Acting at the A 3 Adenosine Receptor:  Analysis of Binding and Relative Efficacy

    Article • Journal of Chemical Information and Computer Sciences, May 2007, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  361. Structure−Activity Relationship of Uridine 5‘ - Diphosphoglucose Analogues as Agonists of the Human P2Y 14 Receptor

    Article • Journal of Medicinal Chemistry, May 2007, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  362. UDP acting at P2Y6 receptors is a mediator of microglial phagocytosis

    Article • Nature, April 2007, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  363. Structure−Activity Relationships of 2, N 6 ,5‘-Substituted Adenosine Derivatives with Potent Activity at the A 2B Adenosine Receptor

    Article • Journal of Medicinal Chemistry, April 2007, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  364. Neoceptors: reengineering GPCRs to recognize tailored ligands

    Article • Trends in Pharmacological Sciences, March 2007, Elsevier

    Dr Kenneth A. Jacobson

  365. Molecular Modeling of the Human P2Y 2 Receptor and Design of a Selective Agonist, 2‘-Amino-2‘-deoxy-2-thiouridine 5‘-Triphosphate

    Article • Journal of Medicinal Chemistry, March 2007, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  366. The ADP receptor P2Y1 mediates t-PA release in pigs during cardiac ischemia

    Article • Journal of Thrombosis and Thrombolysis, February 2007, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  367. Molecular dynamics simulation of the P2Y14 receptor. Ligand docking and identification of a putative binding site of the distal hexose moiety

    Article • Bioorganic & Medicinal Chemistry Letters, February 2007, Elsevier

    Dr Kenneth A. Jacobson

  368. Rapid identification of functionally critical amino acids in a G protein–coupled receptor

    Article • Nature Methods, January 2007, Nature

    Dr Kenneth A. Jacobson

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

    Article • Journal of Molecular Graphics and Modelling, December 2006, Elsevier

    Dr Kenneth A. Jacobson

  370. Computational prediction of homodimerization of the A3 adenosine receptor

    Article • Journal of Molecular Graphics and Modelling, December 2006, Elsevier

    Dr Kenneth A. Jacobson

  371. 2-Triazole-Substituted Adenosines:  A New Class of Selective A 3 Adenosine Receptor Agonists, Partial Agonists, and Antagonists

    Article • Journal of Medicinal Chemistry, December 2006, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  372. P2X purinergic receptor-mediated ionic current in cardiac myocytes of calsequestrin model of cardiomyopathy: implications for the treatment of heart failure

    Article • AJP Heart and Circulatory Physiology, October 2006, American Physiological Society

    Dr Kenneth A. Jacobson

  373. Defining the nucleotide binding sites of P2Y receptors using rhodopsin-based homology modeling

    Article • Journal of Computer-Aided Molecular Design, October 2006, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  374. Uridine-5′-triphosphate (UTP) reduces infarct size and improves rat heart function after myocardial infarct

    Article • Biochemical Pharmacology, October 2006, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, October 2006, Elsevier

    Dr Kenneth A. Jacobson

  376. Action of Nucleosides and Nucleotides at 7 Transmembrane-Spanning Receptors

    Article • Nucleosides Nucleotides & Nucleic Acids, October 2006, Taylor & Francis

    Dr Kenneth A. Jacobson

  377. Structure−Activity Relationships of Uridine 5‘-Diphosphate Analogues at the Human P2Y 6 Receptor

    Article • Journal of Medicinal Chemistry, September 2006, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  378. International Union of Pharmacology LVIII: Update on the P2Y G Protein-Coupled Nucleotide Receptors: From Molecular Mechanisms and Pathophysiology to Therapy

    Article • Pharmacological Reviews, September 2006, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry, July 2006, Elsevier

    Dr Kenneth A. Jacobson

  380. Structure−Activity Relationships of New 1 H -Imidazo[4,5- c ]quinolin-4-amine Derivatives as Allosteric Enhancers of the A 3 Adenosine Receptor

    Article • Journal of Medicinal Chemistry, June 2006, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  381. A Missense Mutation in the Seven-transmembrane Domain of the Human Ca2+ Receptor Converts a Negative Allosteric Modulator into a Positive Allosteric Modulator

    Article • Journal of Biological Chemistry, May 2006, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  382. Orthogonal Activation of the Reengineered A 3 Adenosine Receptor (Neoceptor) Using Tailored Nucleoside Agonists

    Article • Journal of Medicinal Chemistry, May 2006, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  383. Positive Inotropic Effects by Uridine Triphosphate (UTP) and Uridine Diphosphate (UDP) via P2Y2 and P2Y6 Receptors on Cardiomyocytes and Release of UTP in Man During Myocardial Infarction

    Article • Circulation Research, April 2006, Wolters Kluwer Health

    Dr Kenneth A. Jacobson

  384. (N)-methanocarba-2MeSADP (MRS2365) is a subtype-specific agonist that induces rapid desensitization of the P2Y1 receptor of human platelets

    Article • Journal of Thrombosis and Haemostasis, April 2006, Wiley

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry, March 2006, Elsevier

    Dr Kenneth A. Jacobson

  386. Progress in the pursuit of therapeutic adenosine receptor antagonists

    Article • Medicinal Research Reviews, March 2006, Wiley

    Dr Kenneth A. Jacobson

  387. Keynote review: Allosterism in membrane receptors

    Article • Drug Discovery Today, March 2006, Elsevier

    Dr Kenneth A. Jacobson

  388. Adenosine receptors as therapeutic targets

    Article • Nature Reviews Drug Discovery, March 2006, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  389. [32 P]2-iodo-N 6 -methyl-(N )-methanocarba-2′-deoxyadenosine-3′,5′-bisphosphate ([32 P]MRS2500), a novel radioligand for quantification of native P2Y1 receptors

    Article • British Journal of Pharmacology, March 2006, Wiley

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, February 2006, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry Letters, February 2006, Elsevier

    Dr Kenneth A. Jacobson

  392. Structure−Activity Relationships of 2-Chloro- N 6 -substituted-4‘-thioadenosine-5‘-uronamides as Highly Potent and Selective Agonists at the Human A 3 Adenosine Receptor

    Article • Journal of Medicinal Chemistry, January 2006, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  393. Nucleoside Prodrugs of A3 Adenosine Receptor Agonists and Antagonists

    Article • Collection of Czechoslovak Chemical Communications, January 2006, Institute of Organic Chemistry & Biochemistry

    Dr Kenneth A. Jacobson

  394. Article • Critical Care, January 2006, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  395. Semirational Design of (North)-Methanocarba Nucleosides as Dual Acting A 1 and A 3 Adenosine Receptor Agonists:  Novel Prototypes for Cardioprotection

    Article • Journal of Medicinal Chemistry, December 2005, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  396. Human P2Y 6 Receptor:  Molecular Modeling Leads to the Rational Design of a Novel Agonist Based on a Unique Conformational Preference

    Article • Journal of Medicinal Chemistry, December 2005, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, December 2005, Elsevier

    Dr Kenneth A. Jacobson

  398. New 8-substituted xanthiene derivatives as potent bronchodilators

    Article • Il Farmaco, November 2005, Elsevier

    Dr Kenneth A. Jacobson

  399. MRS2500 [2-Iodo-N6-methyl-(N)-methanocarba-2′-deoxyadenosine-3′,5′-bisphosphate], a Potent, Selective, and Stable Antagonist of the Platelet P2Y1 Receptor with Strong Antithrombotic Activity in Mice

    Article • Journal of Pharmacology and Experimental Therapeutics, October 2005, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  400. Purine Derivatives as Ligands for A3 Adenosine Receptors

    Article • Current Topics in Medicinal Chemistry, October 2005, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  401. Nucleoside Modification and Concerted Mutagenesis of the Human A3Adenosine Receptor to Probe Interactions Between the 2-Position of Adenosine Analogs and Gln167 in the Second Extracellular Loop

    Article • Nucleosides Nucleotides & Nucleic Acids, September 2005, Taylor & Francis

    Dr Kenneth A. Jacobson

  402. Identification of an Agonist-induced Conformational Change Occurring Adjacent to the Ligand-binding Pocket of the M3 Muscarinic Acetylcholine Receptor

    Article • Journal of Biological Chemistry, August 2005, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  403. Phospholipase C and cAMP-dependent positive inotropic effects of ATP in mouse cardiomyocytes via P2Y-like receptors

    Article • Journal of Molecular and Cellular Cardiology, August 2005, Elsevier

    Dr Kenneth A. Jacobson

  404. Amphiphilic pyridinium salts block TNFα/NFκB signaling and constitutive hypersecretion of interleukin-8 (IL-8) from cystic fibrosis lung epithelial cells

    Article • Biochemical Pharmacology, August 2005, Elsevier

    Dr Kenneth A. Jacobson

  405. 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

    Article • Purinergic Signalling, July 2005, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  406. Synthesis of pyridoxal phosphate derivatives with antagonist activity at the P2Y13 receptor

    Article • Biochemical Pharmacology, July 2005, Elsevier

    Dr Kenneth A. Jacobson, Dr. Katrin Sak

  407. “Reversine” and Its 2-Substituted Adenine Derivatives as Potent and Selective A 3 Adenosine Receptor Antagonists

    Article • Journal of Medicinal Chemistry, July 2005, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Blood, June 2005, American Society of Hematology

    Dr Kenneth A. Jacobson

  409. Synthesis of Novel Apio Carbocyclic Nucleoside Analogues as Selective A 3 Adenosine Receptor Agonists

    Article • The Journal of Organic Chemistry, June 2005, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  410. Role of adenosine A1 and A3 receptors in regulation of cardiomyocyte homeostasis after mitochondrial respiratory chain injury

    Article • AJP Heart and Circulatory Physiology, June 2005, American Physiological Society

    Dr Kenneth A. Jacobson

  411. Allosteric Modulation of the Adenosine Family of Receptors

    Article • Mini-Reviews in Medicinal Chemistry, June 2005, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  412. Pronounced Conformational Changes following Agonist Activation of the M3 Muscarinic Acetylcholine Receptor

    Article • Journal of Biological Chemistry, April 2005, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  413. SYNTHESIS OF 3′-UREIDOADENOSINE ANALOGUES AND THEIR BINDING AFFINITY TO THE A3ADENOSINE RECEPTOR

    Article • Nucleosides Nucleotides & Nucleic Acids, April 2005, Taylor & Francis

    Dr Kenneth A. Jacobson

  414. Molecular Recognition at Adenine Nucleotide (P2) Receptors in Platelets

    Article • Seminars in Thrombosis and Hemostasis, April 2005, Thieme Publishing Group

    Dr Kenneth A. Jacobson

  415. Involvement of uracil nucleotides in protection of cardiomyocytes from hypoxic stress

    Article • Biochemical Pharmacology, April 2005, Elsevier

    Dr Kenneth A. Jacobson

  416. D-4′-THIOADENOSINE DERIVATIVES AS HIGHLY POTENT AND SELECTIVE AGONISTS AT THE HUMAN A3ADENOSINE RECEPTOR

    Article • Nucleosides Nucleotides & Nucleic Acids, April 2005, Taylor & Francis

    Dr Kenneth A. Jacobson

  417. ( N )-Methanocarba 2, N 6 -Disubstituted Adenine Nucleosides as Highly Potent and Selective A 3 Adenosine Receptor Agonists

    Article • Journal of Medicinal Chemistry, March 2005, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry, February 2005, Elsevier

    Dr Kenneth A. Jacobson

  419. A Neoceptor Approach to Unraveling Microscopic Interactions between the Human A2A Adenosine Receptor and Its Agonists

    Article • Chemistry & Biology, February 2005, Elsevier

    Dr Kenneth A. Jacobson

  420. Design and synthesis of new bicyclic diketopiperazines as scaffolds for receptor probes of structurally diverse functionality

    Article • Organic & Biomolecular Chemistry, January 2005, Royal Society of Chemistry

    Dr Kenneth A. Jacobson

  421. The recently deorphanized GPR80 (GPR99) proposed to be the P2Y15 receptor is not a genuine P2Y receptor

    Article • Trends in Pharmacological Sciences, January 2005, Elsevier

    Dr Kenneth A. Jacobson

  422. The Cross-Species A3Adenosine-Receptor Antagonist MRS 1292 Inhibits Adenosine-Triggered Human Nonpigmented Ciliary Epithelial Cell Fluid Release and Reduces Mouse Intraocular Pressure

    Article • Current Eye Research, January 2005, Taylor & Francis

    Dr Kenneth A. Jacobson

  423. Techniques: Recent developments in computer-aided engineering of GPCR ligands using the human adenosine A3 receptor as an example

    Article • Trends in Pharmacological Sciences, January 2005, Elsevier

    Dr Kenneth A. Jacobson

  424. A New Synthetic Route to (North)-Methanocarba Nucleosides Designed as A 3 Adenosine Receptor Agonists

    Article • The Journal of Organic Chemistry, January 2005, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  425. A New Synthetic Route to (North)-Methanocarba Nucleosides Designed as A 3 Adenosine Receptor Agonists

    Article • The Journal of Organic Chemistry, January 2005, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  426. A Region in the Seven-transmembrane Domain of the Human Ca 2+ Receptor Critical for Response to Ca 2+

    Article • Journal of Biological Chemistry, December 2004, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  427. PURINE RECEPTORS: GPCR STRUCTURE AND AGONIST DESIGN

    Article • Molecular Interventions, December 2004, CLOCKSS Archive

    Dr Kenneth A. Jacobson

  428. Coronary artery reperfusion: The ADP receptor P2Y1 mediates early reactive hyperemia in vivo in pigs

    Article • Purinergic Signalling, December 2004, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  429. Random Mutagenesis of the M3 Muscarinic Acetylcholine Receptor Expressed in Yeast: IDENTIFICATION OF SECOND-SITE MUTATIONS THAT RESTORE FUNCTION TO A COUPLING-DEFICIENT MUTANT M3 RECEPTOR

    Article • Journal of Biological Chemistry, November 2004, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  430. Shift in purine/pyrimidine base recognition upon exchanging extracellular domains in P2Y1/6 chimeric receptors

    Article • Biochemical Pharmacology, November 2004, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry, November 2004, Elsevier

    Dr Kenneth A. Jacobson

  432. Antiaggregatory activity in human platelets of potent antagonists of the P2Y1 receptor

    Article • Biochemical Pharmacology, November 2004, Elsevier

    Dr Kenneth A. Jacobson

  433. 2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors

    Article • Biochemical Pharmacology, November 2004, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry Letters, October 2004, Elsevier

    Dr Kenneth A. Jacobson

  435. Architecture of P2Y Nucleotide Receptors:  Structural Comparison Based on Sequence Analysis, Mutagenesis, and Homology Modeling †

    Article • Journal of Medicinal Chemistry, October 2004, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  436. Induction of Novel Agonist Selectivity for the ADP-Activated P2Y1 Receptor Versus the ADP-Activated P2Y12 and P2Y13 Receptors by Conformational Constraint of an ADP Analog

    Article • Journal of Pharmacology and Experimental Therapeutics, September 2004, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  437. Stimulation of Xenopus P2Y1 receptor activates CFTR in A6 cells

    Article • Pflügers Archiv - European Journal of Physiology, July 2004, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  438. 2,2′-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding

    Article • Biochemical Pharmacology, July 2004, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry, June 2004, Elsevier

    Dr Kenneth A. Jacobson

  440. Digitoxin mimics gene therapy with CFTR and suppresses hypersecretion of IL-8 from cystic fibrosis lung epithelial cells

    Article • Proceedings of the National Academy of Sciences, May 2004, Proceedings of the National Academy of Sciences

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry, May 2004, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Life Sciences, May 2004, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, May 2004, Elsevier

    Dr Kenneth A. Jacobson

  444. Partial Agonists for A3 Adenosine Receptors

    Article • Current Topics in Medicinal Chemistry, April 2004, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  445. Molecular Recognition at Purine and Pyrimidine Nucleotide (P2) Receptors

    Article • Current Topics in Medicinal Chemistry, April 2004, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  446. Preface [Hot Topic: Receptors for Extracellular Nucleosides and Nucleotides (Guest Editor: Kenneth A. Jacobson)]

    Article • Current Topics in Medicinal Chemistry, April 2004, Bentham Science Publishers

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, March 2004, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry, February 2004, Elsevier

    Dr Kenneth A. Jacobson

  449. Northern ring conformation of methanocarba-adenosine 5?-triphosphate required for activation of P2X receptors

    Article • Drug Development Research, January 2004, Wiley

    Dr Kenneth A. Jacobson

  450. Design and Synthesis of A3Adenosine Receptor Ligands, 3′-Fluoro Analogues of Cl-IB-MECA

    Article • Nucleosides Nucleotides & Nucleic Acids, October 2003, Taylor & Francis

    Dr Kenneth A. Jacobson

  451. Design and Synthesis of A3Adenosine Receptor Ligands, 2′-Fluoro Analogues of Cl-IB-MECA

    Article • Nucleosides Nucleotides & Nucleic Acids, October 2003, Taylor & Francis

    Dr Kenneth A. Jacobson

  452. Coordinated Adenine Nucleotide Phosphohydrolysis and Nucleoside Signaling in Posthypoxic Endothelium

    Article • The Journal of Experimental Medicine, August 2003, Rockefeller University Press

    Dr Kenneth A. Jacobson

  453. N 6 -Substituted D-4‘-Thioadenosine-5‘-methyluronamides:  Potent and Selective Agonists at the Human A 3 Adenosine Receptor

    Article • Journal of Medicinal Chemistry, August 2003, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  454. A Conformationally Locked Analogue of the Anti-HIV Agent Stavudine. An Important Correlation between Pseudorotation and Maximum Amplitude

    Article • Journal of Medicinal Chemistry, July 2003, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  455. Corrigendum to ‘Design, Synthesis and Binding Affinity of 3′-Fluoro Analogues of C1-IB-MECA as Adenosine A3 Receptor Ligands’[Bioorg. Med. Chem. Lett. 13 (2003) 817]†

    Article • Bioorganic & Medicinal Chemistry Letters, June 2003, Elsevier

    Dr Kenneth A. Jacobson

  456. Synthesis of a Novel Conformationally Locked Carbocyclic Nucleoside Ring System

    Article • Organic Letters, May 2003, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, May 2003, Elsevier

    Dr Kenneth A. Jacobson

  458. Identification of Essential Residues Involved in the Allosteric Modulation of the Human A3 Adenosine Receptor

    Article • Molecular Pharmacology, May 2003, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  459. Extracellular nucleotides induce vasodilatation in human arteries via prostaglandins, nitric oxide and endothelium-derived hyperpolarising factor

    Article • British Journal of Pharmacology, April 2003, Wiley

    Dr Kenneth A. Jacobson

  460. Engineering of A3 adenosine and P2Y nucleotide receptors and their ligands

    Article • Drug Development Research, April 2003, Wiley

    Dr Kenneth A. Jacobson

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

    Article • Biochemical Pharmacology, March 2003, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Bioorganic & Medicinal Chemistry Letters, March 2003, Elsevier

    Dr Kenneth A. Jacobson

  463. 2-Phenylimidazo[2,1-i]purin-5-ones Structure–Activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors

    Article • Bioorganic & Medicinal Chemistry, February 2003, Elsevier

    Dr Kenneth A. Jacobson

  464. Dihydropyridines as inhibitors of capacitative calcium entry in leukemic HL-60 cells

    Article • Biochemical Pharmacology, February 2003, Elsevier

    Dr Kenneth A. Jacobson

  465. Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A1 and A3 adenosine receptors

    Article • Biochemical Pharmacology, February 2003, Elsevier

    Dr Kenneth A. Jacobson

  466. Characterization of the UDP-glucose receptor (re-named here the P2Y14 receptor) adds diversity to the P2Y receptor family

    Article • Trends in Pharmacological Sciences, February 2003, Elsevier

    Dr Kenneth A. Jacobson

  467. Quinazolines as adenosine receptor antagonists: SAR and selectivity for A2B receptors

    Article • Bioorganic & Medicinal Chemistry, January 2003, Elsevier

    Dr Kenneth A. Jacobson

  468. Article • Cellular and Molecular Neurobiology, January 2003, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  469. Article • Cellular and Molecular Neurobiology, January 2003, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  470. Article • Molecular and Cellular Biochemistry, January 2003, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  471. Molecular Modeling as a Tool to Investigate Molecular Recognition in P2Y Receptors

    Article • Current Pharmaceutical Design, December 2002, Bentham Science Publishers

    Dr Kenneth A. Jacobson

  472. Evidence for the recognition of non-nucleotide antagonists within the transmembrane domains of the human P2Y1receptor

    Article • Drug Development Research, December 2002, Wiley

    Dr Kenneth A. Jacobson

  473. Acyclic Analogues of Adenosine Bisphosphates as P2Y Receptor Antagonists:  Phosphate Substitution Leads to Multiple Pathways of Inhibition of Platelet Aggregation

    Article • Journal of Medicinal Chemistry, December 2002, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  474. A3 Adenosine Receptors in Human Astrocytoma Cells: Agonist-Mediated Desensitization, Internalization, and Down-Regulation

    Article • Molecular Pharmacology, December 2002, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  475. Quantitation of the P2Y1 Receptor with a High Affinity Radiolabeled Antagonist

    Article • Molecular Pharmacology, November 2002, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  476. Identification of Acidic Residues in the Extracellular Loops of the Seven-transmembrane Domain of the Human Ca2+ Receptor Critical for Response to Ca2+ and a Positive Allosteric Modulator

    Article • Journal of Biological Chemistry, September 2002, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  477. Purine and Pyrimidine (P2) Receptors as Drug Targets

    Article • Journal of Medicinal Chemistry, September 2002, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  478. Functionalized Congeners of Tyrosine-Based P2X7Receptor Antagonists:  Probing Multiple Sites for Linking and Dimerization

    Article • Bioconjugate Chemistry, September 2002, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • Journal of Medicinal Chemistry, August 2002, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  480. Synthesis, Biological Properties, and Molecular Modeling Investigation of the First Potent, Selective, and Water-Soluble Human A 3 Adenosine Receptor Antagonist

    Article • Journal of Medicinal Chemistry, August 2002, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  481. Imidazo[2,1- i ]purin-5-ones and Related Tricyclic Water-Soluble Purine Derivatives:  Potent A 2A - and A 3 -Adenosine Receptor Antagonists †

    Article • Journal of Medicinal Chemistry, August 2002, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  482. Extracellular Adenine Nucleotides Regulate Na+/H+ Exchanger NHE3 Activity in A6-NHE3 Transfectants by a cAMP/PKA-dependent Mechanism

    Article • The Journal of Membrane Biology, August 2002, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  483. Selective Allosteric Enhancement of Agonist Binding and Function at Human A3 Adenosine Receptors by a Series of Imidazoquinoline Derivatives

    Article • Molecular Pharmacology, July 2002, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  484. Structure−Activity Relationships at Human and Rat A 2B Adenosine Receptors of Xanthine Derivatives Substituted at the 1-, 3-, 7-, and 8-Positions

    Article • Journal of Medicinal Chemistry, May 2002, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  485. Adenine Nucleotide Analogues Locked in a Northern Methanocarba Conformation:  Enhanced Stability and Potency as P2Y 1 Receptor Agonists

    Article • Journal of Medicinal Chemistry, May 2002, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  486. 2-Chloro-N6-cyclopentyladenosine, adenosine A1 receptor agonist, antagonizes the adenosine A3 receptor

    Article • European Journal of Pharmacology, May 2002, Elsevier

    Dr Kenneth A. Jacobson

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

    Article • Journal of Biological Chemistry, March 2002, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  488. p53-Independent induction of Fas and apoptosis in leukemic cells by an adenosine derivative, Cl-IB-MECA

    Article • Biochemical Pharmacology, March 2002, Elsevier

    Dr Kenneth A. Jacobson

  489. Heteromultimeric P2X1/2 Receptors Show a Novel Sensitivity to Extracellular pH

    Article • Journal of Pharmacology and Experimental Therapeutics, February 2002, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Kenneth A. Jacobson

  490. Methanocarba Modification of Uracil and Adenine Nucleotides:  High Potency of Northern Ring Conformation at P2Y 1 , P2Y 2 , P2Y 4 , and P2Y 11 but Not P2Y 6 Receptors

    Article • Journal of Medicinal Chemistry, January 2002, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  491. Neoceptor Concept Based on Molecular Complementarity in GPCRs:  A Mutant Adenosine A 3 Receptor with Selectively Enhanced Affinity for Amine-Modified Nucleosides

    Article • Journal of Medicinal Chemistry, November 2001, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  492. Synthesis and purine receptor affinity of 6-oxopurine nucleosides and nucleotides containing (N)-methanocarba-pseudoribose rings

    Article • Bioorganic & Medicinal Chemistry Letters, September 2001, Elsevier

    Dr Kenneth A. Jacobson

  493. Angiotensin II-induced apoptosis in rat cardiomyocyte culture: a possible role of AT1 and AT2 receptors

    Article • Journal of Hypertension, September 2001, Wolters Kluwer Health

    Dr Kenneth A. Jacobson

  494. Acyclic and Cyclopropyl Analogues of Adenosine Bisphosphate Antagonists of the P2Y 1 Receptor:  Structure−Activity Relationships and Receptor Docking

    Article • Journal of Medicinal Chemistry, September 2001, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  495. Fluorosulfonyl- and Bis-(β-chloroethyl)amino-phenylamino Functionalized Pyrazolo[4,3- e ]1,2,4-triazolo[1,5- c ]pyrimidine Derivatives:  Irreversible Antagonists at the Human A 3 Adenosine Receptor and Molecular Modeling Studies

    Article • Journal of Medicinal Chemistry, August 2001, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  496. Constitutive Activation of A3 Adenosine Receptors by Site-Directed Mutagenesis

    Article • Biochemical and Biophysical Research Communications, June 2001, Elsevier

    Dr Kenneth A. Jacobson

  497. Activation of A3Adenosine Receptor Protects Against Doxorubicin-induced Cardiotoxicity

    Article • Journal of Molecular and Cellular Cardiology, June 2001, Elsevier

    Dr Kenneth A. Jacobson

  498. Ring-Constrained (N)-Methanocarba nucleosides as adenosine receptor agonists: independent 5′-Uronamide and 2′-deoxy modifications

    Article • Bioorganic & Medicinal Chemistry Letters, May 2001, Elsevier

    Dr Kenneth A. Jacobson

  499. RIBOSE MODIFIED NUCLEOSIDES AND NUCLEOTIDES AS LIGANDS FOR PURINE RECEPTORS

    Article • Nucleosides Nucleotides & Nucleic Acids, March 2001, Taylor & Francis

    Dr Kenneth A. Jacobson

  500. Structurally related nucleotides as selective agonists and antagonists at P2Y1 receptors

    Article • Il Farmaco, March 2001, Elsevier

    Dr Kenneth A. Jacobson

  501. [3H]MRS 1754, a selective antagonist radioligand for A2B adenosine receptors

    Article • Biochemical Pharmacology, March 2001, Elsevier

    Dr Kenneth A. Jacobson

  502. Synthesis Using Ring Closure Metathesis and Effect on Nucleoside Transport of a (N)-Methanocarba S -(4-Nitrobenzyl)thioinosine Derivative

    Article • Organic Letters, February 2001, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  503. Structure−Activity Relationships of Pyridoxal Phosphate Derivatives as Potent and Selective Antagonists of P2X 1 Receptors

    Article • Journal of Medicinal Chemistry, February 2001, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  504. Roles of BCL-2 and Caspase 3 in the Adenosine A3

    Article • Journal of Molecular Neuroscience, January 2001, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  505. PURINES 2000 meeting: Biochemical, pharmacological and clinical perspectives

    Article • Drug Development Research, January 2001, Wiley

    Dr Kenneth A. Jacobson

  506. Probing adenosine and P2 receptors: Design of novel purines and nonpurines as selective ligands

    Article • Drug Development Research, January 2001, Wiley

    Dr Kenneth A. Jacobson

  507. Potent P2X7 receptor antagonists: Tyrosyl derivatives synthesized using a sequential parallel synthetic approach

    Article • Drug Development Research, January 2001, Wiley

    Dr Kenneth A. Jacobson

  508. Article • Molecular and Cellular Biochemistry, January 2001, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  509. Adenosine A1 and A3 receptors: Distinct cardioprotection

    Article • Drug Development Research, January 2001, Wiley

    Dr Kenneth A. Jacobson

  510. Actions of a series of PPADS analogs at P2X1 and P2X3 receptors

    Article • Drug Development Research, January 2001, Wiley

    Dr Kenneth A. Jacobson

  511. Activation of A 3 Adenosine Receptor Induces Calcium Entry and Chloride Secretion in A 6 Cells

    Article • The Journal of Membrane Biology, November 2000, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  512. Inhibition of ecto-apyrase and ecto-ATPase by pyridoxal phosphate-related compounds

    Article • Drug Development Research, November 2000, Wiley

    Dr Kenneth A. Jacobson

  513. Site-directed mutagenesis studies of human A2A adenosine receptors

    Article • Biochemical Pharmacology, September 2000, Elsevier

    Dr Kenneth A. Jacobson

  514. In search of selective P2 receptor ligands: interaction of dihydropyridine derivatives at recombinant rat P2X2 receptors

    Article • Journal of the Autonomic Nervous System, July 2000, Elsevier

    Dr Kenneth A. Jacobson

  515. Methanocarba Analogues of Purine Nucleosides as Potent and Selective Adenosine Receptor Agonists

    Article • Journal of Medicinal Chemistry, June 2000, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  516. Induction of Apoptosis in Rat Cardiocytes by A3 Adenosine Receptor Activation and Its Suppression by Isoproterenol

    Article • Experimental Cell Research, May 2000, Elsevier

    Dr Kenneth A. Jacobson

  517. Synthesis, Biological Activity, and Molecular Modeling of Ribose-Modified Deoxyadenosine Bisphosphate Analogues as P2Y 1 Receptor Ligands

    Article • Journal of Medicinal Chemistry, March 2000, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  518. Anilide Derivatives of an 8-Phenylxanthine Carboxylic Congener Are Highly Potent and Selective Antagonists at Human A 2B Adenosine Receptors

    Article • Journal of Medicinal Chemistry, March 2000, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  519. Activation of the A 3 adenosine receptor affects cell cycle progression and cell growth

    Article • Naunyn-Schmiedeberg s Archives of Pharmacology, February 2000, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  520. Acyclic Analogues of Deoxyadenosine 3‘,5‘-Bisphosphates as P2Y1 Receptor Antagonists

    Article • Journal of Medicinal Chemistry, February 2000, American Chemical Society (ACS)

    Carola Gallo-Rodriguez, Dr Kenneth A. Jacobson

  521. The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family

    Article • Bioorganic & Medicinal Chemistry Letters, January 2000, Elsevier

    Dr Kenneth A. Jacobson

  522. Purification and recognition of recombinant mouse P2X1 receptors expressed in a baculovirus system

    Article • Drug Development Research, January 2000, Wiley

    Dr Kenneth A. Jacobson

  523. Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptors

    Article • Drug Development Research, January 2000, Wiley

    Dr Kenneth A. Jacobson

  524. Pyran template approach to the design of novel A3 adenosine receptor antagonists

    Article • Drug Development Research, December 1999, Wiley

    Dr Kenneth A. Jacobson

  525. Selective A 3 Adenosine Receptor Antagonists:  Water-Soluble 3,5-Diacyl-1,2,4-trialkylpyridinium Salts and Their Oxidative Generation from Dihydropyridine Precursors

    Article • Journal of Medicinal Chemistry, October 1999, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  526. Chiral Resolution and Stereospecificity of 6-Phenyl-4-phenylethynyl- 1,4-dihydropyridines as Selective A 3 Adenosine Receptor Antagonists

    Article • Journal of Medicinal Chemistry, August 1999, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  527. Acyl-hydrazide derivatives of a xanthine carboxylic congener (XCC) as selective antagonists at human A2B adenosine receptors

    Article • Drug Development Research, August 1999, Wiley

    Dr Kenneth A. Jacobson

  528. Functionalized Congeners of 1,4-Dihydropyridines as Antagonist Molecular Probes for A 3 Adenosine Receptors

    Article • Bioconjugate Chemistry, July 1999, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  529. Characterization of “Mini-Nucleotides” as P2X Receptor Agonists in Rat Cardiomyocyte Cultures. An Integrated Synthetic, Biochemical, and Theoretical Study

    Article • Journal of Medicinal Chemistry, July 1999, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  530. The Role of Amino Acids in Extracellular Loops of the Human P2Y1 Receptor in Surface Expression and Activation Processes

    Article • Journal of Biological Chemistry, May 1999, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  531. Structure−Activity Relationships of Bisphosphate Nucleotide Derivatives as P2Y 1 Receptor Antagonists and Partial Agonists

    Article • Journal of Medicinal Chemistry, May 1999, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  532. 1,3-dialkylxanthine derivatives having high potency as antagonists at human A2B adenosine receptors

    Article • Drug Development Research, May 1999, Wiley

    Dr Kenneth A. Jacobson

  533. Role of the Extracellular Loops of G Protein-Coupled Receptors in Ligand Recognition:  A Molecular Modeling Study of the Human P2Y 1 Receptor

    Article • Biochemistry, March 1999, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  534. Protection against ischemic damage by adenosine amine congener, a potent and selective adenosine A1 receptor agonist

    Article • European Journal of Pharmacology, March 1999, Elsevier

    Dr Kenneth A. Jacobson

  535. Synthesis, CoMFA Analysis, and Receptor Docking of 3,5-Diacyl-2,4-Dialkylpyridine Derivatives as Selective A 3 Adenosine Receptor Antagonists

    Article • Journal of Medicinal Chemistry, February 1999, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  536. Chronic administration of adenosine A3 receptor agonist and cerebral ischemia: neuronal and glial effects

    Article • European Journal of Pharmacology, February 1999, Elsevier

    Dr Kenneth A. Jacobson

  537. Article • APOPTOSIS, January 1999, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  538. Induction of Apoptosis in Cardiac Myocytes by an A3Adenosine Receptor Agonist

    Article • Experimental Cell Research, September 1998, Elsevier

    Dr Kenneth A. Jacobson

  539. Synthesis and Biological Activity of a New Series of N 6 -Arylcarbamoyl, 2-(Ar)alkynyl- N 6 -arylcarbamoyl, and N 6 -Carboxamido Derivatives of Adenosine-5‘- N -ethyluronamide as A 1 and A 3 Adenosine Receptor Agonists

    Article • Journal of Medicinal Chemistry, August 1998, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  540. Structure−Activity Relationships and Molecular Modeling of 3,5-Diacyl-2,4-dialkylpyridine Derivatives as Selective A 3 Adenosine Receptor Antagonists

    Article • Journal of Medicinal Chemistry, August 1998, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  541. Derivatives of the Triazoloquinazoline Adenosine Antagonist (CGS 15943) Having High Potency at the Human A 2B and A 3 Receptor Subtypes

    Article • Journal of Medicinal Chemistry, July 1998, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  542. Activation of the A2A adenosine receptor inhibits nitric oxide production in glial cells

    Article • FEBS Letters, June 1998, Wiley

    Dr Kenneth A. Jacobson

  543. A physiological role of the adenosine A 3 receptor: Sustained cardioprotection

    Article • Proceedings of the National Academy of Sciences, June 1998, Proceedings of the National Academy of Sciences

    Dr Kenneth A. Jacobson

  544. Activation and desensitization of rat A3-adenosine receptors by selective adenosine derivatives and xanthine-7-ribosides

    Article • Drug Development Research, June 1998, Wiley

    Dr Kenneth A. Jacobson

  545. A Pyridoxine Cyclic Phosphate and Its 6-Azoaryl Derivative Selectively Potentiate and Antagonize Activation of P2X 1 Receptors

    Article • Journal of Medicinal Chemistry, June 1998, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  546. Competitive and selective antagonism of P2Y1 receptors by N 6 -methyl 2′-deoxyadenosine 3′,5′-bisphosphate

    Article • British Journal of Pharmacology, May 1998, Wiley

    Dr Kenneth A. Jacobson

  547. Apoptosis by 2-chloro-2′-deoxy-adenosine and 2-chloro-adenosine in human peripheral blood mononuclear cells

    Article • Neurochemistry International, May 1998, Elsevier

    Dr Kenneth A. Jacobson

  548. Adenosine A3 receptors: novel ligands and paradoxical effects

    Article • Trends in Pharmacological Sciences, May 1998, Elsevier

    Dr Kenneth A. Jacobson

  549. Human P2Y 1 Receptor:  Molecular Modeling and Site-Directed Mutagenesis as Tools To Identify Agonist and Antagonist Recognition Sites

    Article • Journal of Medicinal Chemistry, April 1998, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  550. Direct Activation of Cystic Fibrosis Transmembrane Conductance Regulator Channels by 8-Cyclopentyl-1,3-dipropylxanthine (CPX) and 1,3-Diallyl-8-cyclohexylxanthine (DAX)

    Article • Journal of Biological Chemistry, March 1998, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  551. Flavonoid Derivatives as Adenosine Receptor Antagonists:  A Comparison of the Hypothetical Receptor Binding Site Based on a Comparative Molecular Field Analysis Model

    Article • Journal of Medicinal Chemistry, January 1998, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  552. Deoxyadenosine Bisphosphate Derivatives as Potent Antagonists at P2Y 1 Receptors

    Article • Journal of Medicinal Chemistry, January 1998, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  553. The A3Adenosine Receptor Mediates Cell Spreading, Reorganization of Actin Cytoskeleton, and Distribution of Bcl-xL: Studies in Human Astroglioma Cells

    Article • Biochemical and Biophysical Research Communications, December 1997, Elsevier

    Dr Kenneth A. Jacobson

  554. New base-altered adenosine analogues: Synthesis and affinity at adenosine A1 and A2A receptors

    Article • Bioorganic & Medicinal Chemistry Letters, December 1997, Elsevier

    Dr Kenneth A. Jacobson

  555. Riboflavin: Inhibitory effects on receptors, G-proteins, and adenylate cyclase

    Article • Drug Development Research, October 1997, Wiley

    Dr Kenneth A. Jacobson

  556. Regulation of A1 adenosine receptors by amiodarone and electrical stimulation in rat myocardial cells in vitro

    Article • Biochemical Pharmacology, September 1997, Elsevier

    Dr Kenneth A. Jacobson

  557. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists

    Article • Neuropharmacology, September 1997, Elsevier

    Dr Kenneth A. Jacobson

  558. Structure−Activity Relationships of 4-(Phenylethynyl)-6-phenyl-1,4- dihydropyridines as Highly Selective A 3 Adenosine Receptor Antagonists

    Article • Journal of Medicinal Chemistry, August 1997, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  559. Mutagenesis Reveals Structure−Activity Parallels between Human A 2A Adenosine Receptors and Biogenic Amine G Protein-Coupled Receptors

    Article • Journal of Medicinal Chemistry, August 1997, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  560. Differential effects of flavonoids on testosterone-metabolizing cytochrome P450s

    Article • Life Sciences, July 1997, Elsevier

    Dr Kenneth A. Jacobson

  561. 8-Cyclopentyl-1,3-dipropylxanthine and Other Xanthines Differentially Bind to the Wild-Type and ΔF508 Mutant First Nucleotide Binding Fold (NBF-1) Domains of the Cystic Fibrosis Transmembrane Conductance Regulator

    Article • Biochemistry, May 1997, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  562. Towards a revised nomenclature for P1 and P2 receptors

    Article • Trends in Pharmacological Sciences, March 1997, Elsevier

    Dr Kenneth A. Jacobson

  563. Adenosine A3 receptor agonist-induced neurotoxicity in rat cerebellar granule neurons

    Article • Drug Development Research, March 1997, Wiley

    Dr Kenneth A. Jacobson

  564. Adenosine A3Receptor Agonists Protect HL-60 and U-937 Cells from Apoptosis Induced by A3Antagonists

    Article • Biochemical and Biophysical Research Communications, March 1997, Elsevier

    Dr Kenneth A. Jacobson

  565. Postischemic administration of adenosine amine congener (ADAC): analysis of recovery in gerbils

    Article • European Journal of Pharmacology, December 1996, Elsevier

    Dr Kenneth A. Jacobson

  566. Activation of A3 adenosine receptors on human eosinophils elevates intracellular calcium

    Article • Blood, November 1996, American Society of Hematology

    Dr Kenneth A. Jacobson

  567. Activation of phosphoinositide breakdown and elevation of intracellular calcium in a rat RBL-2H3 mast cell line by adenosine analogs: Involvement of A3-adenosine receptors?

    Article • Drug Development Research, September 1996, Wiley

    Dr Kenneth A. Jacobson

  568. Site-directed mutagenesis of the human adenosine A2A receptor. Critical involvement of Glu13 in agonist recognition

    Article • European Journal of Pharmacology, August 1996, Elsevier

    Dr Kenneth A. Jacobson

  569. Hemodynamic effects and histamine release elicited by the selective adenosine A3 receptor agonist 2-Cl-IB-MECA in conscious rats

    Article • European Journal of Pharmacology, July 1996, Elsevier

    Dr Kenneth A. Jacobson

  570. Effect of Adenosine on Na + and Cl − Currents in A 6 Monolayers. Receptor Localization and Messenger Involvement

    Article • The Journal of Membrane Biology, June 1996, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  571. Reduction of postischemic brain damage and memory deficits following treatment with the selective adenosine A1 receptor agonist

    Article • European Journal of Pharmacology, April 1996, Elsevier

    Dr Kenneth A. Jacobson

  572. Induction of Apoptosis in HL-60 Human Promyelocytic Leukemia Cells by Adenosine A3Receptor Agonists

    Article • Biochemical and Biophysical Research Communications, April 1996, Elsevier

    Dr Kenneth A. Jacobson

  573. Adenosine receptor ligands: differences with acute versus chronic treatment

    Article • Trends in Pharmacological Sciences, March 1996, Elsevier

    Dr Kenneth A. Jacobson

  574. Induction of Apoptosis in HL-60 Human Promyelocytic Leukemia Cells by Adenosine A3Receptor Agonists

    Article • Biochemical and Biophysical Research Communications, February 1996, Elsevier

    Dr Kenneth A. Jacobson

  575. Tetrahydrobenzothiophenone Derivatives as a Novel Class of Adenosine Receptor Antagonists †

    Article • Journal of Medicinal Chemistry, January 1996, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  576. Synthesis and Biological Activities of Flavonoid Derivatives as A 3 Adenosine Receptor Antagonists

    Article • Journal of Medicinal Chemistry, January 1996, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  577. Molecular recognition in adenosine receptors

    Article • January 1996, Elsevier

    Dr Kenneth A. Jacobson

  578. Molecular architecture of G protein-coupled receptors

    Article • Drug Development Research, January 1996, Wiley

    Dr Kenneth A. Jacobson

  579. Interactions of Flavonoids and Other Phytochemicals with Adenosine Receptors

    Article • Journal of Medicinal Chemistry, January 1996, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  580. Interaction of 1,4-Dihydropyridine and Pyridine Derivatives with Adenosine Receptors:  Selectivity for A 3 Receptors

    Article • Journal of Medicinal Chemistry, January 1996, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  581. Derivatives of the Triazoloquinazoline Adenosine Antagonist (CGS15943) Are Selective for the Human A 3 Receptor Subtype

    Article • Journal of Medicinal Chemistry, January 1996, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  582. 6-Phenyl-1,4-dihydropyridine Derivatives as Potent and Selective A 3 Adenosine Receptor Antagonists

    Article • Journal of Medicinal Chemistry, January 1996, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  583. Cerebral ischemia in gerbils: effects of acute and chronic treatment with adenosine A2A receptor agonist and antagonist

    Article • European Journal of Pharmacology, December 1995, Elsevier

    Dr Kenneth A. Jacobson

  584. Comparative molecular field analysis of selective A3 adenosine receptor agonists

    Article • Bioorganic & Medicinal Chemistry, October 1995, Elsevier

    Dr Kenneth A. Jacobson

  585. Section Review Central & Peripheral Nervous Systems: P2-Purinoceptors: Advances and therapeutic opportunities

    Article • Expert Opinion on Investigational Drugs, October 1995, Informa Healthcare

    Dr Kenneth A. Jacobson

  586. Chronic NMDA receptor stimulation: therapeutic implications of its effect on adenosine A1 receptors

    Article • European Journal of Pharmacology, September 1995, Elsevier

    Dr Kenneth A. Jacobson

  587. Adenosine: a Prototherapeutic Concept in Neurodegeneration

    Article • Annals of the New York Academy of Sciences, September 1995, Wiley

    Dr Kenneth A. Jacobson

  588. Stimulation by Alkylxanthines of Chloride Efflux in CFPAC-1 Cells Does Not Involve A1 Adenosine Receptors

    Article • Biochemistry, July 1995, American Chemical Society (ACS)

    Carola Gallo-Rodriguez, Dr Kenneth A. Jacobson

  589. Site-directed Mutagenesis Identifies Residues Involved in Ligand Recognition in the Human A2a Adenosine Receptor

    Article • Journal of Biological Chemistry, June 1995, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Kenneth A. Jacobson

  590. Erratum

    Article • Biochemical and Biophysical Research Communications, May 1995, Elsevier

    Dr Kenneth A. Jacobson

  591. Erratum

    Article • Biochemical and Biophysical Research Communications, April 1995, Elsevier

    Dr Kenneth A. Jacobson

  592. Presence of Both A1 and A2a Adenosine Receptors in Human Cells and Their Interaction

    Article • Biochemical and Biophysical Research Communications, March 1995, Elsevier

    Dr Kenneth A. Jacobson

  593. The effects of adenosine A3 receptor stimulation on seizures in mice

    Article • European Journal of Pharmacology, February 1995, Elsevier

    Dr Kenneth A. Jacobson

  594. Molecular probes for muscarinic receptors: Functionalized congeners of selective muscarinic antagonists

    Article • Life Sciences, February 1995, Elsevier

    Dr Kenneth A. Jacobson

  595. Selective Ligands for Rat A3 Adenosine Receptors: Structure-Activity Relationships of 1,3-Dialkylxanthine 7-Riboside Derivatives

    Article • Journal of Medicinal Chemistry, November 1994, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  596. 2-Substitution of N6-Benzyladenosine-5'-uronamides Enhances Selectivity for A3 Adenosine Receptors

    Article • Journal of Medicinal Chemistry, October 1994, American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  597. Species differences in ligand affinity at central A3-adenosine receptors

    Article • Drug Development Research, September 1994, Wiley

    Dr Kenneth A. Jacobson

  598. Adenosine A3 receptor stimulation and cerebral ischemia

    Article • European Journal of Pharmacology, September 1994, Elsevier

    Dr Kenneth A. Jacobson

  599. Characterization of adenosine receptors in intact cultured heart cells

    Article • Biochemical Pharmacology, August 1994, Elsevier

    Dr Kenneth A. Jacobson

  600. A Selective Agonist Affinity Label for A3 Adenosine Receptors

    Article • Biochemical and Biophysical Research Communications, August 1994, Elsevier

    Dr Kenneth A. Jacobson

  601. Molecular modeling of adenosine receptors. The ligand binding site on the rat adenosine A2A receptor

    Article • European Journal of Pharmacology Molecular Pharmacology, June 1994, Elsevier

    Dr Kenneth A. Jacobson

  602. Chronic administration of selective adenosine A1 receptor agonist or antagonist in cerebral ischemia

    Article • European Journal of Pharmacology, April 1994, Elsevier

    Dr Kenneth A. Jacobson

  603. Structure activity relationships for derivatives of adenosine-5?-triphosphate as agonists at P2 purinoceptors: Heterogeneity within P2x and P2y subtypes

    Article • Drug Development Research, March 1994, Wiley

    Dr Kenneth A. Jacobson

  604. Chronic adenosine A1 receptor agonist and antagonist: effect on receptor density and induced seizures in mice

    Article • European Journal of Pharmacology, February 1994, Elsevier

    Dr Kenneth A. Jacobson

  605. Adenosine Receptor Prodrugs: Synthesis and Biological Activity of Derivatives of Potent, ArSelective Agonists

    Article • Journal of Pharmaceutical Sciences, January 1994, Elsevier

    Dr Kenneth A. Jacobson

  606. A role for central A3‐adenosine receptors

    Article • FEBS Letters, December 1993, Wiley

    Carola Gallo-Rodriguez, Dr Kenneth A. Jacobson

  607. Effects of N6-cyclopentyl adenosine and 8-cyclopentyl-1,3-dipropylxanthine on induced seizures in mice

    Article • European Journal of Pharmacology, November 1993, Elsevier

    Dr Kenneth A. Jacobson

  608. Effects of chronic administration of adenosine A1 receptor agonist and antagonist on spatial learning and memory

    Article • European Journal of Pharmacology, November 1993, Elsevier

    Dr Kenneth A. Jacobson

  609. Effects of combinations of methylxanthines and adenosine analogs on locomotor activity in control and chronic caffeine-treated mice

    Article • Drug Development Research, October 1993, Wiley

    Dr Kenneth A. Jacobson

  610. Solubilized Rabbit Striatal A2a-Adenosine Receptors: Stability and Antagonist Binding

    Article • Archives of Biochemistry and Biophysics, September 1993, Elsevier

    Dr Kenneth A. Jacobson

  611. Chronic caffeine alters the density of adenosine, adrenergic, cholinergic, GABA, and serotonin receptors and calcium channels in mouse brain

    Article • Cellular and Molecular Neurobiology, June 1993, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  612. 8‐(3‐Chlorostyryl)caffeine (CSC) is a selective A2‐adenosine antagonist in vitro and in vivo

    Article • FEBS Letters, May 1993, Wiley

    Carola Gallo-Rodriguez, Dr Kenneth A. Jacobson

  613. Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists

    Article • Journal of Medicinal Chemistry, May 1993, American Chemical Society (ACS)

    Carola Gallo-Rodriguez, Dr Kenneth A. Jacobson

  614. Locomotor activity in mice during chronic treatment with caffeine and withdrawal

    Article • Pharmacology Biochemistry and Behavior, January 1993, Elsevier

    Dr Kenneth A. Jacobson

  615. 2-[2-[4-[2-[2-[1,3-Dihydro-1,1-bis(4-hydroxyphenyl)-3-oxo-5-isobenzofuranthioureidyl]ethylaminocarbonyl]ethyl]phenyl] ethylamino]-5?-N-ethylcarboxamidoadenosine (FITC-APEC): A fluorescent ligand for A2a-adenosine receptors

    Article • Journal of Fluorescence, December 1992, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  616. A1 adenosine-receptor antagonists activate chloride efflux from cystic fibrosis cells.

    Article • Proceedings of the National Academy of Sciences, June 1992, Proceedings of the National Academy of Sciences

    Dr Kenneth A. Jacobson

  617. Penetration of adenosine antagonists into mouse brain as determined by ex vivo binding

    Article • Biochemical Pharmacology, February 1992, Elsevier

    Dr Kenneth A. Jacobson

  618. High affinity acylating antagonists for muscarinic receptors

    Article • Life Sciences, January 1992, Elsevier

    Dr Kenneth A. Jacobson

  619. Characterization of Human Striatal A2-Adenosine Receptors Using Radioligand Binding and Photoaffinity Labeling

    Article • Journal of Receptor Research, January 1992, Taylor & Francis

    Dr Kenneth A. Jacobson

  620. Apparent heterogeneity of cardiac A 1 adenosine receptors as revealed by radioligand binding experiments on N-ethylmaleimide-treated membranes

    Article • Naunyn-Schmiedeberg s Archives of Pharmacology, December 1991, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  621. Novel therapeutics acting via purine receptors

    Article • Biochemical Pharmacology, May 1991, Elsevier

    Dr Kenneth A. Jacobson

  622. [3H]XAC (xanthine amine congener) is a radioligand for A2-adenosine receptors in rabbit striatum

    Article • Neurochemistry International, January 1991, Elsevier

    Dr Kenneth A. Jacobson

  623. Purification and characterization of bovine cerebral cortex A1 adenosine receptor1

    Article • Archives of Biochemistry and Biophysics, December 1990, Elsevier

    Dr Kenneth A. Jacobson

  624. Improvement of cold tolerance by selective A1 adenosine receptor antagonists in rats

    Article • Pharmacology Biochemistry and Behavior, September 1990, Elsevier

    Dr Kenneth A. Jacobson

  625. Positron emission tomographic (PET) imaging of a peptide receptor in vivo using a general prosthetic group methodology: 18F-labeled insulin

    Article • European Journal of Pharmacology, July 1990, Elsevier

    Dr Kenneth A. Jacobson

  626. Improving cold resistance by selective A1 adenosine receptor antagonist in rats

    Article • European Journal of Pharmacology, July 1990, Elsevier

    Dr Kenneth A. Jacobson

  627. Characterization of the locomotor depression produced by an A2 -selective adenosine agonist

    Article • FEBS Letters, February 1990, Wiley

    Dr Kenneth A. Jacobson

  628. [79] Probing adenosine receptors using biotinylated purine derivatives

    Article • January 1990, Elsevier

    Dr Kenneth A. Jacobson

  629. Radioligand Binding Assays for Adenosine Receptors

    Article • January 1990, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  630. Affinity chromatography of the bovine cerebral cortex A1 adenosine receptor

    Article • FEBS Letters, November 1989, Wiley

    Dr Kenneth A. Jacobson

  631. Seizures induced by methylxanthines, potential cognitive enhancers in dementia syndromes

    Article • March 1989, Springer Science + Business Media

    Dr Kenneth A. Jacobson

  632. Potent convulsant actions of the adenosine receptor antagonist, xanthine amine congener (XAC)

    Article • Life Sciences, January 1989, Elsevier

    Dr Kenneth A. Jacobson

  633. 8-substituted xanthines as antagonists at A1- and A2-adenosine receptors

    Article • Biochemical Pharmacology, October 1988, Elsevier

    Dr Kenneth A. Jacobson

  634. A prosthetic group for the rapid introduction of fluorine into peptides and functionalized drugs

    Article • Journal of Fluorine Chemistry, June 1988, Elsevier

    Dr Kenneth A. Jacobson

  635. Autoradiographic localization of mouse brain adenosine receptors with an antagonist ([3H]xanthine amine congener) ligand probe

    Article • Neuroscience Letters, March 1988, Elsevier

    Dr Kenneth A. Jacobson

  636. Non-xanthine heterocycles: Activity as antagonists of A1 and A2-adenosine receptors

    Article • Biochemical Pharmacology, February 1988, Elsevier

    Dr Kenneth A. Jacobson

  637. Adenosine analogs with covalently attached lipids have enhanced potency at A1 -adenosine receptors

    Article • FEBS Letters, December 1987, Wiley

    Dr Kenneth A. Jacobson

  638. Autoradiographic localization of adenosine A1 receptors in rat brain using [3H]XCC, a functionalized congener of 1,3-dipropylxanthine

    Article • Neuroscience Letters, October 1987, Elsevier

    Dr Kenneth A. Jacobson

  639. Molecular probes for extracellular adenosine receptors

    Article • Biochemical Pharmacology, May 1987, Elsevier

    Dr Kenneth A. Jacobson

  640. Liquid chromatographic assay for cerebrospinal fluid normetanephrine

    Article • Life Sciences, April 1987, Elsevier

    Dr Kenneth A. Jacobson

  641. New high-performance liquid chromatographic procedure for the detection and quantification of β-phenylethylamine

    Article • Journal of Chromatography B Biomedical Sciences and Applications, January 1987, Elsevier

    Dr Kenneth A. Jacobson

  642. Species differences in structure-activity relationships of adenosine agonists and xanthine antagonists at brain A1 adenosine receptors

    Article • FEBS Letters, December 1986, Wiley

    Dr Kenneth A. Jacobson

  643. N6-Functionalized congeners of adenosine with high potency at A2-adenosine receptors: Potential ligands for affinity chromatography

    Article • Biochemical and Biophysical Research Communications, May 1986, Elsevier

    Dr Kenneth A. Jacobson

  644. A [3 H]amine congener of 1,3-dipropyl-8-phenylxanthine

    Article • FEBS Letters, April 1986, Wiley

    Dr Kenneth A. Jacobson

  645. Functionalized congeners of 1,3-dipropyl-8-phenylxanthine: Potent antagonists for adenosine receptors that modulate membrane adenylate cyclase in pheochromocytoma cells, platelets and fat cells

    Article • Life Sciences, March 1986, Elsevier

    Dr Kenneth A. Jacobson

  646. Liquid chromatographic assay for cerebrospinal fluid serotonin

    Article • Life Sciences, February 1986, Elsevier

    Dr Kenneth A. Jacobson

  647. Simultaneous determination of histamine and Nτ-methylhistamine with high-performance liquid chromatography using electrochemical detection

    Article • Analytical Biochemistry, January 1986, Elsevier

    Dr Kenneth A. Jacobson

  648. Electrochemical detection of biogenic amines following acylation by N-hydroxysuccinimide esters

    Article • FEBS Letters, September 1985, Wiley

    Dr Kenneth A. Jacobson

  649. Probing the adenosine receptor with adenosine and xanthine biotin conjugates

    Article • FEBS Letters, May 1985, Wiley

    Dr Kenneth A. Jacobson

  650. Visual methods for the nanomolar detection of electrophilic reagents

    Article • Journal of Biochemical and Biophysical Methods, November 1983, Elsevier

    Dr Kenneth A. Jacobson

  651. Characterization of catecholamine-polypeptide conjugates

    Article • European Polymer Journal, January 1983, Elsevier

    Dr Kenneth A. Jacobson

  652. Modified Nucleosides as Selective Modulators of Adenosine Receptors for Therapeutic Use

    Article • Wiley

    Dr Kenneth A. Jacobson

  653. Exploring the Role of N6Substituents in Potent Dual Acting 5CEthyltetrazolyladenosine Derivatives: Synthesis Binding, Functional Assays, and Antinociceptive Effects in Mice

    Article • American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  654. N6Substituted 5NMethylcarbamoyl-4-selenoadenosines as Potent and Selective A3 Adenosine Receptor Agonists with Unusual Sugar Puckering and Nucleobase Orientation

    Article • American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

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

    Article • American Chemical Society (ACS)

    Dr Kenneth A. Jacobson

  657. Adenosine Receptors

    Article • Springer Science + Business Media

    Dr Kenneth A. Jacobson