Literature DB >> 18445527

P2Y1 receptor antagonists as novel antithrombotic agents.

Jeffrey A Pfefferkorn1, Chulho Choi, Thomas Winters, Robert Kennedy, Liguo Chi, Lisa A Perrin, Gina Lu, Yun-Wen Ping, Tom McClanahan, Richard Schroeder, Michael T Leininger, Andrew Geyer, Sabine Schefzick, James Atherton.   

Abstract

The P2Y(1) and P2Y(12) purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y(1) knockout studies as well as from nucleotide-based small molecule P2Y(1) antagonists has suggested that the antagonism of this receptor may offer a novel and effective method for the treatment of thrombotic disorders. Herein, we report the identification and optimization of a series of non-nucleotide P2Y(1) antagonists that are potent and orally bioavailable.

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Year:  2008        PMID： 18445527     DOI： 10.1016/j.bmcl.2008.04.028

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  17 in total

Review 1.  G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions.

Authors:  Kenneth A Jacobson; Ramachandran Balasubramanian; Francesca Deflorian; Zhan-Guo Gao
Journal:  Purinergic Signal       Date:  2012-02-29       Impact factor: 3.765

Review 2.  The role of P2Y₁₂ receptor and activated platelets during inflammation.

Authors:  Elisabetta Liverani; Laurie E Kilpatrick; Alexander Y Tsygankov; Satya P Kunapuli
Journal:  Curr Drug Targets       Date:  2014       Impact factor: 3.465

Review 3.  P2Y nucleotide receptors: promise of therapeutic applications.

Authors:  Kenneth A Jacobson; Jean-Marie Boeynaems
Journal:  Drug Discov Today       Date:  2010-06-02       Impact factor: 7.851

4.  Pharmacochemistry of the platelet purinergic receptors.

Authors:  Kenneth A Jacobson; Francesca Deflorian; Shilpi Mishra; Stefano Costanzi
Journal:  Purinergic Signal       Date:  2011-02-18       Impact factor: 3.765

5.  Trichinella spiralis secreted enzymes regulate nucleotide-induced mast cell activation and release of mouse mast cell protease 1.

Authors:  Holly C Afferson; Emily Eleftheriou; Murray E Selkirk; Kleoniki Gounaris
Journal:  Infect Immun       Date:  2012-08-13       Impact factor: 3.441

6.  P2 receptors and platelet function.

Authors:  Béatrice Hechler; Christian Gachet
Journal:  Purinergic Signal       Date:  2011-07-27       Impact factor: 3.765

7.  Molecular Structure of P2Y Receptors: Mutagenesis, Modeling, and Chemical Probes.

Authors:  Kenneth A Jacobson; M P Suresh Jayasekara; Stefano Costanzi
Journal:  Wiley Interdiscip Rev Membr Transp Signal       Date:  2012-09-12

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

Authors:  Stefano Costanzi; T Santhosh Kumar; Ramachandran Balasubramanian; T Kendall Harden; Kenneth A Jacobson
Journal:  Bioorg Med Chem       Date:  2012-07-03       Impact factor: 3.641

Review 9.  Involvement of P2 receptors in hematopoiesis and hematopoietic disorders, and as pharmacological targets.

Authors:  Kelly Juliana Filippin; Kamylla F S de Souza; Roberto Theodoro de Araujo Júnior; Heron Fernandes Vieira Torquato; Dhébora Albuquerque Dias; Eduardo Benedetti Parisotto; Alice Teixeira Ferreira; Edgar J Paredes-Gamero
Journal:  Purinergic Signal       Date:  2019-12-20       Impact factor: 3.765

10.  Development of selective agonists and antagonists of P2Y receptors.

Authors:  Kenneth A Jacobson; Andrei A Ivanov; Sonia de Castro; T Kendall Harden; Hyojin Ko
Journal:  Purinergic Signal       Date:  2008-07-04       Impact factor: 3.765
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