Design and synthesis of sulfamoyl benzoic acid analogues with subnanomolar agonist activity specific to the LPA2 receptor.
Design and synthesis of sulfamoyl benzoic acid analogues with subnanomolar agonist activity specific to the LPA2 receptor.
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DOI：
10.1021/jm5007116
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发表时间：
2014-08-28
影响因子：
7.3
通讯作者：
Tigyi GJ
中科院分区：
文献类型：
--
作者：
Patil R;Fells JI;Szabó E;Lim KG;Norman DD;Balogh A;Patil S;Strobos J;Miller DD;Tigyi GJ
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.
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影响因子：
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