G-protein coupled receptor 40 (GPR40) has been considered to be an attractive drug target for the treatment of type 2 diabetes because of its role in free fatty acids-mediated enhancement of glucose-stimulated insulin secretion (GSIS) from pancreatic β-cells. A series of indole-5-propanoic acid compounds were synthesized, and their GPR40 agonistic activities were evaluated by nuclear factor of activated T-cells reporter assay and GSIS assay in the MIN-6 insulinoma cells. Three compounds, (EC = 58.6 nM), (EC = 37.8 nM), and (EC = 9.4 nM), were identified as potent GPR40 agonists with good GSIS effects.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5733302 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.7b00460 | DOI Listing |
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