From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor

Kindon, Nicholas and Davis, Andrew and Dougall, Iain and Dixon, John and Johnson, Timothy and Walters, Iain and Thom, Steve and McKechnie, Kenneth and Meghani, Premji and Stocks, Michael (2017) From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor. Bioorganic & Medicinal Chemistry Letters . ISSN 1464-3405 (In Press)

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Abstract

The G protein-coupled P2Y2 receptor, activated by ATP and UTP has been reported as a potential drug target for a wide range of important clinical conditions, such as tumor metastasis, kidney disorders, and in the treatment of inflammatory conditions. However, pharmacological studies on this receptor have been impeded by the limited reported availability of stable, potent and selective P2Y2R antagonists. This article describes the design and synthesis of AR-C118925, a potent and selective non-nucleotide antagonist of the P2Y2 receptor discovered using the endogenous P2Y2R agonist UTP as the chemical starting point.

Item Type: Article
Keywords: P2Y2; Purinergic; AR-C118925; P2; Antagonist
Schools/Departments: University of Nottingham, UK > Faculty of Science > School of Pharmacy
Identification Number: 10.1016/j.bmcl.2017.09.043
Depositing User: Eprints, Support
Date Deposited: 27 Sep 2017 08:42
Last Modified: 16 Dec 2017 22:40
URI: http://eprints.nottingham.ac.uk/id/eprint/46762

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