The role of P2YR in cardiovascular diseases and recent development of P2YR antagonists.

Drug Discov Today

Department of Pharmacology, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, PR China. Electronic address:

Published: March 2020

As a member of the P2Y receptor family with a typical 7-transmembrane structure, P2Y purinergic receptor (P2YR) belongs to the G-protein-coupled nucleotide receptor activating the phospholipase-C signaling pathway. P2YR is widely involved in a range of human diseases, including atherosclerosis and other cardiovascular diseases, gradually attracting attention owing to its inappropriate or excessive activation. In addition, it was reported that P2YR might regulate inflammatory responses by governing the maturation and secretion of proinflammatory cytokines. Hence, several P2YR antagonists have been subjected to evaluation as new therapeutic strategies in recent years. This review was aimed at summarizing the role of P2YR in the pathogenesis of cardiovascular diseases, with an insight into the recent progress on discovery of P2YR antagonists.

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http://dx.doi.org/10.1016/j.drudis.2019.12.015DOI Listing

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