title: 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.affiliation: Department of Physics, Chemistry and Pharmacy, University of Southern Denmark , Campusvej 55, DK-5230 Odense M, Denmark.
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Christiansen
authors.forename: Steffen V F
authors.initials: SV
authors.lastname: Hansen
authors.forename: Christian
authors.initials: C
authors.lastname: Urban
authors.forename: Brian D
authors.initials: BD
authors.lastname: Hudson
authors.forename: Edward T
authors.initials: ET
authors.lastname: Wargent
authors.forename: Manuel
authors.initials: M
authors.lastname: Grundmann
authors.forename: Laura
authors.initials: L
authors.lastname: Jenkins
authors.forename: Mohamed
authors.initials: M
authors.lastname: Zaibi
authors.forename: Claire J
authors.initials: CJ
authors.lastname: Stocker
authors.forename: Susanne
authors.initials: S
authors.lastname: Ullrich
authors.forename: Evi
authors.initials: E
authors.lastname: Kostenis
authors.forename: Matthias U
authors.initials: MU
authors.lastname: Kassack
authors.forename: Graeme
authors.initials: G
authors.lastname: Milligan
authors.forename: Michael A
authors.initials: MA
authors.lastname: Cawthorne
authors.forename: Trond
authors.initials: T
authors.lastname: Ulven
keywords: FFA1 agonist; GPR40 agonist; TUG-770; Type 2 diabetes; free fatty acid receptor; insulin secretagogue