Department of Integrative Medical Sciences, Northeast Ohio Medical University, 4209 State Route 44, Rootstown, OH 44272, United States.
Biochem Pharmacol. 2013 Dec 1;86(11):1517-24. doi: 10.1016/j.bcp.2013.08.015. Epub 2013 Aug 26.
Accumulating data have shown that bile acids are important cell signaling molecules, which may activate several signaling pathways to regulate biological processes. Bile acids are endogenous ligands for the farnesoid X receptor (FXR) and TGR5, a G-protein coupled receptor. Gain- and loss-of-function studies have demonstrated that both FXR and TGR5 play important roles in regulating lipid and carbohydrate metabolism and inflammatory responses. Importantly, activation of FXR or TGR5 lowers hepatic triglyceride levels and inhibits inflammation. Such properties of FXR or TGR5 have indicated that these two bile acid receptors are ideal targets for treatment of non-alcoholic fatty liver disease, one of the major health concerns worldwide. In this article, we will focus on recent advances on the role of both FXR and TGR5 in regulating hepatic triglyceride metabolism and inflammatory responses under normal and disease conditions.
越来越多的证据表明,胆汁酸是重要的细胞信号分子,它可以通过激活多种信号通路来调节生物过程。胆汁酸是法尼醇 X 受体(FXR)和 G 蛋白偶联受体 TGR5 的内源性配体。功能获得和功能丧失研究表明,FXR 和 TGR5 均在调节脂质和碳水化合物代谢以及炎症反应中发挥重要作用。重要的是,FXR 或 TGR5 的激活可以降低肝甘油三酯水平并抑制炎症。FXR 或 TGR5 的这些特性表明,这两种胆汁酸受体是治疗非酒精性脂肪性肝病的理想靶点,非酒精性脂肪性肝病是全球主要的健康关注点之一。本文将重点介绍 FXR 和 TGR5 在正常和疾病状态下调节肝甘油三酯代谢和炎症反应的最新进展。