The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators

…, Z Wang, M Wanska, J Greenberg, J Weiszmann…

文献索引：Wang, Yingcai; Jiao, Xianyun; Kayser, Frank; Liu, Jiwen; Wang, Zhongyu; Wanska, Malgorzata; Greenberg, Joanne; Weiszmann, Jennifer; Ge, Hongfei; Tian, Hui; Wong, Simon; Schwandner, Ralf; Lee, Taeweon; Li, Yang Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 2 p. 493 - 498

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被引用次数: 45

摘要

Free fatty acid receptor 2 (FFA2) is a G-protein coupled receptor for which only short-chain fatty acids (SCFAs) have been reported as endogenous ligands. We describe the discovery and optimization of phenylacetamides as allosteric agonists of FFA2. These novel ligands can suppress adipocyte lipolysis in vitro and reduce plasma FFA levels in vivo, suggesting that these allosteric modulators can serve as pharmacological tools for exploring the ...