Patil Renukadevi, Fells James I, Szabó Erzsébet, Lim Keng G, Norman Derek D, Balogh Andrea, Patil Shivaputra, Strobos Jur, Miller Duane D, Tigyi Gábor J
Departments of Pharmaceutical Sciences and ‡Physiology, The University of Tennessee Health Science Center , Memphis, Tennessee 894 Union Avenue 38163 United States.
J Med Chem. 2014 Aug 28;57(16):7136-40. doi: 10.1021/jm5007116. Epub 2014 Aug 12.
Lysophosphatidic acid (LPA) is a growth factor-like mediator and a ligand for multiple GPCR. The LPA2 GPCR mediates antiapoptotic and mucosal barrier-protective effects in the gut. We synthesized sulfamoyl benzoic acid (SBA) analogues that are the first specific agonists of LPA2, some with subnanomolar activity. We developed an experimental SAR that is supported and rationalized by computational docking analysis of the SBA compounds into the LPA2 ligand-binding pocket.
溶血磷脂酸（LPA）是一种生长因子样介质，也是多种G蛋白偶联受体（GPCR）的配体。LPA2 GPCR在肠道中介导抗凋亡和黏膜屏障保护作用。我们合成了氨磺酰苯甲酸（SBA）类似物，它们是LPA2的首批特异性激动剂，其中一些具有亚纳摩尔活性。我们通过将SBA化合物对接至LPA2配体结合口袋进行计算分析，建立了一个得到支持且合理的实验性构效关系。
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