|
|||||
|
|
The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators |
|
| Authors: | Yingcai Wang Xianyun Jiao Frank Kayser Jiwen Liu Zhongyu Wang Malgorzata Wanska Joanne Greenberg Jennifer Weiszmann Hongfei Ge Hui Tian Simon Wong Ralf Schwandner Taeweon Lee Yang Li |
| Affiliation: | 1. Department of Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA;2. Department of Metabolic Disorders, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA;3. Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA;4. Amgen Research GmbH, Regensburg, Germany |
| Abstract: | 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. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |