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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

General Review Article

P2Y6R: A Promising New Target in Inflammatory Diseases and Advances in its Antagonists

Author(s): Yuanhui Wang, Yuanyuan Pei, Yongfang Yao, Weyland Cheng, Yinchao Li* and Yongtao Duan*

Volume 30, Issue 19, 2023

Published on: 23 September, 2022

Page: [2209 - 2224] Pages: 16

DOI: 10.2174/0929867329666220614100218

Price: $65


P2Y receptors (P2YRs) are G protein-coupled receptors that are activated by extracellular nucleotides. The P2Y6 receptor (P2Y6R) is specifically activated by UDP, causing PKC activation and intracellular calcium ion release through the PLC pathway. Based on receptor tissue distribution and related pathways, several studies have reported that P2Y6R plays a physiological role in mediating inflammation, which suggests that P2Y6R could be a promising molecular target for the treatment of inflammatory diseases. In the past ten years, several P2Y6R antagonists have been discovered as new therapeutic strategies for inflammatory diseases. In this article, we systematically summarize the role of P2Y6R in inflammation and highlight the anti-inflammatory mechanism of a key P2Y6R antagonist, MRS2578. Insight into recent progress on the discovery of P2Y6R antagonists is also discussed.

Keywords: P2Y6R, inflammation, antagonist, mechanism, nucleotides, therapeutic strategies.

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