Li Ang, Yang Duxiao, Zhu Mengyuan, Tsai Keng-chang, Xiao Kun-hong, Yu Xiao, Sun Jinpeng, Du Lupei
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.
Department of Biochemistry & Molecular Biology, School of Medicine, Shandong University, Jinan, Shandong 250012, China.
Future Med Chem. 2015;7(18):2429-37. doi: 10.4155/fmc.15.160. Epub 2015 Dec 14.
Free fatty acid 4 (FFA4) (GPR120) receptor functions as a receptor for unsaturated long-chain free fatty acids by regulating the secretion of glucagon-like peptide-1 and suppressing the inflammatory process, in which these two distinct biological functions are modulated by two signaling pathways, Gq and β-arrestin2, respectively.
By using pharmacophore modeling and virtual screening methods, several compounds are found with excellent activities for agonizing FFA4 receptor. It needs to be noted that among them, some molecules demonstrate appealing β-arrestin2-biased properties for the FFA4 receptor.
These compounds may serve as the useful toolkits for detecting differential biased mechanism and developing new candidate therapeutic agents of the FFA4 receptor.
游离脂肪酸4（FFA4）（GPR120）受体作为不饱和长链游离脂肪酸的受体，通过调节胰高血糖素样肽-1的分泌和抑制炎症过程发挥作用，其中这两种不同的生物学功能分别由Gq和β-抑制蛋白2这两条信号通路调节。
通过药效团建模和虚拟筛选方法，发现了几种对FFA4受体具有优异激动活性的化合物。需要注意的是，其中一些分子对FFA4受体表现出有吸引力的β-抑制蛋白2偏向性特性。
这些化合物可作为检测差异偏向机制和开发FFA4受体新候选治疗药物的有用工具。
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