P2X and P2Y Receptors

Kenneth Jacobson serves as Chief of the Laboratory of Bioorganic Chemistry and the Molecular Recognition Section at the National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health in Bethesda, Maryland, USA. Dr. Jacobson is a medicinal chemist with interests in the structure and pharmacology of G-proteincoupled receptors, in particular receptors for adenosine and for purine and pyrimidine nucleotides. P2X and P2Y Receptors

[1]  J. Bajorath,et al.  Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold. , 2010, Journal of medicinal chemistry.

[2]  K. Jacobson,et al.  Quantification of Gi-Mediated Inhibition of Adenylyl Cyclase Activity Reveals That UDP Is a Potent Agonist of the Human P2Y14 Receptor , 2009, Molecular Pharmacology.

[3]  Younis Baqi,et al.  Interaction of New, Very Potent Non-Nucleotide Antagonists with Arg256 of the Human Platelet P2Y12 Receptor , 2009, Journal of Pharmacology and Experimental Therapeutics.

[4]  E. Gouaux,et al.  Crystal structure of the ATP-gated P2X4 ion channel in the closed state , 2009, Nature.

[5]  C. Müller,et al.  Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling. , 2009, Journal of medicinal chemistry.

[6]  G. Reiser,et al.  Structure and ligand-binding site characteristics of the human P2Y11 nucleotide receptor deduced from computational modelling and mutational analysis. , 2007, The Biochemical journal.

[7]  Stefano Costanzi,et al.  Defining the nucleotide binding sites of P2Y receptors using rhodopsin-based homology modeling , 2006, J. Comput. Aided Mol. Des..

[8]  Eric A. Barnard,et al.  International Union of Pharmacology LVIII: Update on the P2Y G Protein-Coupled Nucleotide Receptors: From Molecular Mechanisms and Pathophysiology to Therapy , 2006, Pharmacological Reviews.

[9]  K. Jacobson,et al.  (N)‐methanocarba‐2MeSADP (MRS2365) is a subtype‐specific agonist that induces rapid desensitization of the P2Y1 receptor of human platelets , 2006, Journal of thrombosis and haemostasis : JTH.

[10]  K. Jacobson,et al.  [32P]2‐iodo‐N6‐methyl‐(N)‐methanocarba‐2′‐deoxyadenosine‐3′,5′‐bisphosphate ([32P]MRS2500), a novel radioligand for quantification of native P2Y1 receptors , 2006, British journal of pharmacology.

[11]  C. Müller,et al.  Synthesis and preliminary evaluation of [3H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptors. , 2005, Bioorganic & medicinal chemistry letters.

[12]  J. Gever,et al.  Discovery and Synthesis of a Novel and Selective Drug-Like P2X1 Antagonist. , 2005 .

[13]  G. Schmalzing,et al.  Synthesis and Structure−Activity Relationships of Suramin-Derived P2Y11 Receptor Antagonists with Nanomolar Potency , 2005 .

[14]  G. Schmalzing,et al.  Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist , 2005, Neuropharmacology.

[15]  M. Williams,et al.  [3H]A-317491, a Novel High-Affinity Non-Nucleotide Antagonist That Specifically Labels Human P2X2/3 and P2X3 Receptors , 2004, Journal of Pharmacology and Experimental Therapeutics.

[16]  H. Nakata,et al.  Hetero‐oligomerization between adenosine A1 and P2Y1 receptors in living cells: Formation of ATP‐sensitive adenosine receptors , 2003 .

[17]  G. Schmalzing,et al.  The suramin analogue NF279 is a novel and potent antagonist selective for the P2X1 receptor , 2000, Neuropharmacology.

[18]  W. Stühmer,et al.  Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors , 1999, Neuropharmacology.

[19]  R. North,et al.  Trinitrophenyl-substituted nucleotides are potent antagonists selective for P2X1, P2X3, and heteromeric P2X2/3 receptors. , 1998, Molecular pharmacology.

[20]  K. Starke,et al.  P2-purinoceptor antagonists: II. Blockade of P2-purinoceptor subtypes and ecto-nucleotidases by compounds related to Evans blue and trypan blue , 1996, Naunyn-Schmiedeberg's Archives of Pharmacology.

[21]  G. Reiser,et al.  Hetero-oligomerization of the P2Y11 receptor with the P2Y1 receptor controls the internalization and ligand selectivity of the P2Y11 receptor. , 2008, The Biochemical journal.