TGR5 as a therapeutic target for treating obesity.
TGR5 (also known as GPBAR1, M-BAR, BG37, hGPCR19, and AXOR 109) is a specific membrane G-protein-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.
Zhong
Min
M
Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA. mzhong@presidiopharma.com
D001647:Bile Acids and Salts; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D008024:Ligands; D009765:Obesity / Q000150:complications / Q000188:drug therapy*; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects*; D013329:Structure-Activity Relationship
D001647:Bile Acids and Salts; C473772:GPBAR1 protein, human; D008024:Ligands; D043562:Receptors, G-Protein-Coupled