Abstract

TGR5 (also known as GPBAR1, M-BAR, BG37, hGPCR19, and AXOR 109) is a specific membrane Gprotein- coupled receptor (GPCR) of bile acids (BAs). It has recently become an attractive therapeutic target for the prevention and/or the treatment of obesity and its highly associated Type II diabetes and metabolic syndrome. It has also been implicated in many other inflammatory, cardiovascular, neurological, and hepatic diseases. This review briefly describes the biological rationale of TGR5 as an attractive therapeutic target and summarizes some recent efforts on the development of TGR5 modulators.

Keywords: G-protein-coupled receptor (GPCR), bile acids, TGR5, TGR5 modulators, obesity, Type II diabetes, metabolic syndrome