TGR5 Agonists, A Promising Target to Tackle Metabolic Disorders

来源 :2011年第一届内分泌与代谢大会 | 被引量 : 0次 | 上传用户:markhero
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  TGR5 (also known as GPBAR1, M-BAR, BG37, hGPCR19, and AXOR 109) is a G protein-coupled receptor (GPCR) activated by bile acids (BAs).TGR5 activation result in a stimulation of glucagon-like protein 1 production in enteroendocrine cells and activates thyroid hormone in brown adipose tissue and muscle, through the stimulation of type 2 iodothyronine deiodinase (D2).Through its insulinotropic effects, TGR5 may improve glucose homeostasis; through the activation of D2, it will stimulate energy expenditure and protec.t against the onset of metabolic disorders.lncretin-based therapies have shown promise in the treatment of type 2 diabetes.Here we will review our current understanding of TGR5 as a target to induce both glucagon-like peptide-1 (GLP-1) secretion and energy expenditure and discuss the potential of this drugable target for the treatment of metabolic disorders.
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