Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 4, Issue 5, Pages 441-445Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml4000673
Keywords
Type 2 diabetes; free fatty acid receptor; TUG-770; insulin secretagogue; FFA1 agonist; GPR40 agonist
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Funding
- Danish Council for Independent Researchl Technology and Production [09-070364]
- Danish Council of Strategic Research [11-116196]
- Canadian Institutes of Health Research
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Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic beta-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing.
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