The role of P2Y6R in cardiovascular diseases and recent development of P2Y6R antagonists

作者：Zhou, Mengze; Wang, Weiwei; Li, Yehong; Zhang, Qian; Ji, Hui; Li, Huanqiu^*; Hu, Qinghua^*

来源：Drug Discovery Today, 2020, 25(3): 568-573.

DOI：10.1016/j.drudis.2019.12.015

• VASCULAR SMOOTH-MUSCLE
• PURINERGIC RECEPTORS
• NUCLEOTIDE RECEPTORS
• URIDINE-DIPHOSPHATE
• ENDOTHELIAL-CELLS
• PROSTAGLANDIN E-2
• P2Y RECEPTORS
• MYOGENIC TONE
• ATHEROSCLEROSIS
• ACTIVATION

As a member of the P2Y receptor family with a typical 7-transmembrane structure, P2Y(6) purinergic receptor (P2Y(6)R) belongs to the G-protein-coupled nucleotide receptor activating the phospholipase-C signaling pathway. P2Y(6)R 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 P2Y(6)R might regulate inflammatory responses by governing the maturation and secretion of proinflammatory cytokines. Hence, several P2Y(6)R antagonists have been subjected to evaluation as new therapeutic strategies in recent years. This review was aimed at summarizing the role of P2Y(6)R in the pathogenesis of cardiovascular diseases, with an insight into the recent progress on discovery of P2Y(6)R antagonists.

• 单位
  苏州大学; 中国药科大学