期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 10, 页码 1849-1852出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.04.011
关键词
TGR5; TGR5 agonist; GPBAR1; GLP1 secretion; Type 2 diabetes; Sitagliptin; DPP-4 inhibitor
资金
- Zydus Research Centre, Cadila Healthcare Ltd. [568]
TGR5 is a member of G protein-coupled receptor (GPCR) superfamily, a promising molecular target for metabolic diseases. Activation of TGR5 promotes secretion of glucagon-like peptide-1 (GLP-1), which activates insulin secretion. A series of 2-thio-imidazole derivatives have been identified as novel, potent and orally efficacious TGR5 agonists. Compound 4d, a novel TGR5 agonist, in combination with Sitagliptin, a DPP-4 inhibitor, has demonstrated an adequate GLP-1 secretion and glucose lowering effect in animal models, suggesting a potential clinical option in treatment of type-2 diabetes. (C)2018C)2018 Elsevier Ltd. All rights reserved.
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