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

[Image: see text] 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 ph...

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Detalles Bibliográficos
Autores principales: Christiansen, Elisabeth, Hansen, Steffen V. F., Urban, Christian, Hudson, Brian D., Wargent, Edward T., Grundmann, Manuel, Jenkins, Laura, Zaibi, Mohamed, Stocker, Claire J., Ullrich, Susanne, Kostenis, Evi, Kassack, Matthias U., Milligan, Graeme, Cawthorne, Michael A., Ulven, Trond
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2013
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3654565/
https://www.ncbi.nlm.nih.gov/pubmed/23687558
http://dx.doi.org/10.1021/ml4000673
Descripción
Sumario:[Image: see text] 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.

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