Dear Editor,Takeda G protein-coupled receptor 5(TGR5),also known as G protein-coupled bile acids(BAs)receptor 1(GPBAR1),1 belongs to the class A GPCR subfamily.The major TGR5-dependent actions of BAs include maintaini...Dear Editor,Takeda G protein-coupled receptor 5(TGR5),also known as G protein-coupled bile acids(BAs)receptor 1(GPBAR1),1 belongs to the class A GPCR subfamily.The major TGR5-dependent actions of BAs include maintaining energy homeostasis,regulating glucose/lipids metabolism,as well as immunosuppressive properties.2 TGR5 is identified as a potential therapeutic target for protecting hepatocytes from bile acid overload,preventing atherosclerosis,and inhibiting macrophage inflammation due to its critical role in bile acid sensitization.Thus,elucidation of structural characteristics of TGR5 and its activation mechanism would benefit the discovery of therapeutic drugs for these metabolic disorders.展开更多
基金supported by the National Natural Science Foundation of China(Project No.31971218)Shenzhen Science and Technology Innovation Committee(Projects No.JCYJ20180307151618765 and JCYJ20180508163206306).R.R.was also supported in part by Kobilka Institute of Innovative Drug Discovery and Presidential Fellowship at the Chinese University of Hong Kong,Shenzhen.G.C.was supported in part by Ganghong Young Scholar Fund.
文摘Dear Editor,Takeda G protein-coupled receptor 5(TGR5),also known as G protein-coupled bile acids(BAs)receptor 1(GPBAR1),1 belongs to the class A GPCR subfamily.The major TGR5-dependent actions of BAs include maintaining energy homeostasis,regulating glucose/lipids metabolism,as well as immunosuppressive properties.2 TGR5 is identified as a potential therapeutic target for protecting hepatocytes from bile acid overload,preventing atherosclerosis,and inhibiting macrophage inflammation due to its critical role in bile acid sensitization.Thus,elucidation of structural characteristics of TGR5 and its activation mechanism would benefit the discovery of therapeutic drugs for these metabolic disorders.
