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The role of P2Y6R in cardiovascular diseases and recent development of P2Y6R antagonists.
Drug Discovery Today ( IF 7.4 ) Pub Date : 2020-01-08 , DOI: 10.1016/j.drudis.2019.12.015
Mengze Zhou 1 , Weiwei Wang 2 , Yehong Li 1 , Qian Zhang 1 , Hui Ji 1 , Huanqiu Li 2 , Qinghua Hu 1
Affiliation  

As a member of the P2Y receptor family with a typical 7-transmembrane structure, P2Y6 purinergic receptor (P2Y6R) belongs to the G-protein-coupled nucleotide receptor activating the phospholipase-C signaling pathway. P2Y6R 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 P2Y6R might regulate inflammatory responses by governing the maturation and secretion of proinflammatory cytokines. Hence, several P2Y6R antagonists have been subjected to evaluation as new therapeutic strategies in recent years. This review was aimed at summarizing the role of P2Y6R in the pathogenesis of cardiovascular diseases, with an insight into the recent progress on discovery of P2Y6R antagonists.

中文翻译:

P2Y6R 在心血管疾病中的作用和 P2Y6R 拮抗剂的最新发展。

P2Y6 嘌呤能受体 (P2Y6R) 作为 P2Y 受体家族的一员,具有典型的 7 跨膜结构,属于激活磷脂酶 C 信号通路的 G 蛋白偶联核苷酸受体。P2Y6R广泛参与一系列人类疾病,包括动脉粥样硬化和其他心血管疾病,因其不适当或过度激活而逐渐引起人们的关注。此外,据报道,P2Y6R 可能通过控制促炎细胞因子的成熟和分泌来调节炎症反应。因此,近年来,几种 P2Y6R 拮抗剂作为新的治疗策略受到了评估。本综述旨在总结 P2Y6R 在心血管疾病发病机制中的作用,并深入了解 P2Y6R 拮抗剂的最新发现进展。
更新日期:2020-04-20
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