Drug-like antagonists of P2Y receptors — from lead identification to drug development

Conroy, Sean and Kindon, Nicholas and Kellam, Barrie and Stocks, Michael (2016) Drug-like antagonists of P2Y receptors — from lead identification to drug development. Journal of Medicinal Chemistry . ISSN 1520-4804

[img] PDF - Repository staff only until 14 July 2017. - Requires a PDF viewer such as GSview, Xpdf or Adobe Acrobat Reader
Download (1MB)


P2Y receptors are expressed in virtually all cells and tissue types and mediate an astonishing array of biological functions, including platelet aggregation, smooth muscle cell proliferation, and immune regulation. The P2Y receptors belong to the G protein-coupled receptor superfamily and are composed of eight members encoded by distinct genes that can be subdivided into two groups on the basis of their coupling to specific G-proteins. Extensive research has been undertaken to find modulators of P2Y receptors, although to date only a limited number of small-molecule P2Y receptor antagonists have been approved by drug/medicines agencies. This Perspective reviews the known P2Y receptor antagonists, highlighting oral drug-like receptor antagonists, and considers future opportunities for the development of small molecules for clinical evaluation.

Item Type: Article
Additional Information: This is the author's version of a submitted work that was subsequently accepted for publication in the Journal of Medicinal Chemistry, c2016 American Chemical Society. To access the final edited and published work see http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b01972
Schools/Departments: University of Nottingham UK Campus > Faculty of Medicine and Health Sciences
University of Nottingham UK Campus > Faculty of Science
Identification Number: https://doi.org/10.1021/acs.jmedchem.5b01972
Depositing User: Eprints, Support
Date Deposited: 02 Aug 2016 13:32
Last Modified: 22 Sep 2016 05:46
URI: http://eprints.nottingham.ac.uk/id/eprint/35643

Actions (Archive Staff Only)

Edit View Edit View