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

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

  • ACS Med Chem Lett. 2013 May 9;4(5):441-445. doi: 10.1021/ml4000673.
Elisabeth Christiansen 1,  Steffen V F Hansen,  Christian Urban,  Brian D Hudson,  Edward T Wargent,  Manuel Grundmann,  Laura Jenkins,  Mohamed Zaibi,  Claire J Stocker,  Susanne Ullrich,  Evi Kostenis,  Matthias U Kassack,  Graeme Milligan,  Michael A Cawthorne,  Trond Ulven
Affiliations

Affiliation

  • 1 Department of Physics, Chemistry and Pharmacy, University of Southern Denmark , Campusvej 55, DK-5230 Odense M, Denmark.
PMID: 23687558 DOI: 10.1021/ml4000673
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.

Keywords

FFA1 agonist; GPR40 agonist; TUG-770; Type 2 diabetes; free fatty acid receptor; insulin secretagogue.

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