title: TGR5, Not Only a Metabolic Regulator.
abstract: G-protein-coupled bile acid receptor, Gpbar1 (TGR5), is a member of G-protein-coupled receptor (GPCR) superfamily. High levels of TGR5 mRNA were detected in several tissues such as small intestine, stomach, liver, lung, especially in placenta and spleen. TGR5 is not only the receptor for bile acids, but also the receptor for multiple selective synthetic agonists such as 6α-ethyl-23(S)-methyl-cholic acid (6-EMCA, INT-777) and a series of 4-benzofuranyloxynicotinamde derivatives to regulate different signaling pathways such as nuclear factor κB (NF-κB), AKT, and extracellular signal-regulated kinases (ERK). TGR5, as a metabolic regulator, is involved in energy homeostasis, bile acid homeostasis, as well as glucose metabolism. More recently, our group and others have extended the functions of TGR5 to more than metabolic regulation, which include inflammatory response, cancer and liver regeneration. These findings highlight TGR5 as a potential drug target for different diseases. This review summarizes the basic information of TGR5 and its new functions.
authors.affiliation: State Key Laboratory of Chemical Resource Engineering, College of Life Science and Technology, Beijing University of Chemical Technology Beijing, China.
authors.forename: Cong
authors.initials: C
authors.lastname: Guo
authors.affiliation: Key Laboratory of Receptors-Mediated Gene Regulation and Drug Discovery, School of Medicine, Henan UniversityKaifeng, China; Key Laboratory of Molecular Pathology, School of Basic Medical Science, Inner Mongolia Medical UniversityHohhot, China.
authors.forename: Wei-Dong
authors.initials: WD
authors.lastname: Chen
authors.affiliation: State Key Laboratory of Chemical Resource Engineering, College of Life Science and Technology, Beijing University of Chemical Technology Beijing, China.
authors.forename: Yan-Dong
authors.initials: YD
authors.lastname: Wang
keywords: GPCR; Gpbar1; TGR5; bile acids; receptor