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Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.

ABSTRACT: Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-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.

SUBMITTER: Christiansen E

PROVIDER: S-EPMC3654565 | biostudies-literature | 2013 May

REPOSITORIES: biostudies-literature

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Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.

Christiansen Elisabeth E Hansen Steffen V F SV Urban Christian C Hudson Brian D BD Wargent Edward T ET Grundmann Manuel M Jenkins Laura L Zaibi Mohamed M Stocker Claire J CJ Ullrich Susanne S Kostenis Evi E Kassack Matthias U MU Milligan Graeme G Cawthorne Michael A MA Ulven Trond T

ACS medicinal chemistry letters 20130408 5

Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-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. ...[more]

PMID: 23687558

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