Department of Genomic Drug Discovery Science, Graduate School of Pharmaceutical Sciences, Kyoto University, Japan.
J Pharmacol Sci. 2010;112(1):19-24. doi: 10.1254/jphs.09r09fm.
Utilizing the human genome database, the recently developed G-protein-coupled receptors (GPCRs) deorphanizing strategy successfully identified multiple receptors of free fatty acids (FFAs). FFAs have been demonstrated to act as ligands of several GPCRs (FFAR1, FFAR2, FFAR3, and GPR120). These fatty acid receptors are proposed to play critical roles in various types of physiological homeostases. FFAR1 and GPR120 are activated by medium- and long-chain FFAs. In contrast, FFAR2 and FFAR3 are activated by short-chain FFAs. It has been elucidated that these four receptors are expressed in the gastrointestinal tract and have many essential roles as sensors of FFA. In this review, we summarize the physiological and pharmacological function of the receptors in the gastrointestinal tract.
利用人类基因组数据库，最近开发的 G 蛋白偶联受体（GPCR）去孤儿化策略成功鉴定了多种游离脂肪酸（FFAs）的受体。FFAs 已被证明可作为几种 GPCR（FFAR1、FFAR2、FFAR3 和 GPR120）的配体。这些脂肪酸受体被认为在各种类型的生理稳态中发挥关键作用。FFAR1 和 GPR120 被中链和长链 FFAs 激活。相比之下，FFAR2 和 FFAR3 被短链 FFAs 激活。已经阐明，这四个受体在胃肠道中表达，并且作为 FFA 的传感器具有许多重要作用。在这篇综述中，我们总结了胃肠道中这些受体的生理和药理学功能。
