关于P2Y2受体核苷酸激动剂的当前知识。
Current knowledge on the nucleotide agonists for the P2Y2 receptor.
作者信息
Xu Pengfei, Feng Xi, Luan Hongyu, Wang Jubo, Ge Raoling, Li Zhiyu, Bian Jinlei
机构信息
Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China; Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China.
Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China.
出版信息
Bioorg Med Chem. 2018 Jan 15;26(2):366-375. doi: 10.1016/j.bmc.2017.11.043. Epub 2017 Dec 2.
P2Y receptors are G-protein-coupled receptors (GPCRs) for extracellular nucleotides. There are eight mammalian P2Y receptor subtypes (P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13, and P2Y14). P2Y2 receptors are widely expressed and play important roles in multiple functionalities. Diquafosol tetrasodium, known as INS365, which was the first P2Y2 receptor agonists that had been approved in April 2010 and launched in Japan by Santen Pharmaceuticals. Besides, a series of similar agonists for the P2Y2 receptor are undergoing development to cure different diseases related to the P2Y2 receptor. This article illustrated the structure and functions of the P2Y2 receptor and focused on several kinds of agonists about their molecular structures, research progress and chemical synthesis methods. Last but not the least, we summarized the structures-activity relationship (SAR) of agonists for the P2Y2 receptor and expected more efficient agonists for the P2Y2 receptor.
P2Y受体是细胞外核苷酸的G蛋白偶联受体（GPCRs）。哺乳动物有八种P2Y受体亚型（P2Y1、P2Y2、P2Y4、P2Y6、P2Y11、P2Y12、P2Y13和P2Y14）。P2Y2受体广泛表达，在多种功能中发挥重要作用。双异丙酚四钠，即INS365，是2010年4月获批并由参天制药在日本推出的首个P2Y2受体激动剂。此外，一系列类似的P2Y2受体激动剂正在研发中，用于治疗与P2Y2受体相关的不同疾病。本文阐述了P2Y2受体的结构和功能，并重点介绍了几种激动剂的分子结构、研究进展和化学合成方法。最后但同样重要的是，我们总结了P2Y2受体激动剂的构效关系（SAR），并期待有更高效的P2Y2受体激动剂。
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