| Literature DB >> 29655980 |
Sameer Agarwal1, Santosh Sasane2, Jeevan Kumar2, Prashant Deshmukh3, Hitesh Bhayani3, Poonam Giri3, Suresh Giri3, Shubhangi Soman4, Neelima Kulkarni4, Mukul Jain3.
Abstract
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.Entities:
Keywords: DPP-4 inhibitor; GLP1 secretion; GPBAR1; Sitagliptin; TGR5; TGR5 agonist; Type 2 diabetes
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Year: 2018 PMID： 29655980 DOI： 10.1016/j.bmcl.2018.04.011
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823