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.

• Authors: Elisabeth Christiansen, 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
• Journal: ACS medicinal chemistry letters (ACS Med Chem Lett) Vol. 4 Issue 5 Pg. 441-445 (May 09 2013) ISSN: 1948-5875 [Print] United States
• PMID: 23687558 (Publication Type: Journal Article)