Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 10, Issue 4, Pages 386-396Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/156802610790980576
Keywords
G-protein-coupled receptor (GPCR); bile acids; TGR5; TGR5 modulators; obesity; Type II diabetes; metabolic syndrome
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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.
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