Department of Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett. 2010 Jan 15;20(2):493-8. doi: 10.1016/j.bmcl.2009.11.112. Epub 2009 Nov 26.
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 potential function of FFA2 in various disease conditions.
游离脂肪酸受体 2（FFA2）是一种 G 蛋白偶联受体，目前仅报道短链脂肪酸（SCFAs）是其内源性配体。我们描述了苯乙酰胺作为 FFA2 别构激动剂的发现和优化。这些新型配体可以在体外抑制脂肪细胞的脂解作用，并降低体内游离脂肪酸水平，这表明这些别构调节剂可以作为药理学工具，用于探索 FFA2 在各种疾病状态下的潜在功能。
