doi: 10.1016/j.bmcl.2018.01.013.
Epub 2018 Jan 12.
Discovery of a novel potent GPR40 full agonist
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- PMID: 29366647
- DOI: 10.1016/j.bmcl.2018.01.013
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Discovery of a novel potent GPR40 full agonist
Bioorg Med Chem Lett.
.
Abstract
Compound 12 is a GPR40 agonist that realizes the full magnitude of efficacy possible via GPR40 receptor agonism. In vitro and in vivo studies demonstrated superior glucose lowering by 12 compared to fasiglifam (TAK-875), in a glucose dependent manner. The enhanced efficacy observed with the full agonist 12 was associated with both direct and indirect stimulation of insulin secretion.
Keywords: GPCR; GPR40 full agonist; GSIS; Insulin secretagogues; Type 2 diabetes mellitus.
Copyright © 2018 Elsevier Ltd. All rights reserved.
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