Discovery of TUG-770: a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist for treatment of type 2 diabetes

Christiansen, E. et al. (2013) Discovery of TUG-770: a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist for treatment of type 2 diabetes. ACS Medicinal Chemistry Letters, 4(5), pp. 441-445. (doi: 10.1021/ml4000673)

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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.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Jenkins, Mrs Laura and Hudson, Dr Brian and Milligan, Professor Graeme
Authors: Christiansen, E., Hansen, S.V.F., Urban, C., Hudson, B.D., Wargent, E.T., Grundmann, M., Jenkins, L., Zaibi, M., Stocker, C.J., Ullrich, S., Kostenis, E., Kassack, M.U., Milligan, G., Cawthorne, M.A., and Ulven, T.
College/School:College of Medical Veterinary and Life Sciences > Institute of Molecular Cell and Systems Biology
Journal Name:ACS Medicinal Chemistry Letters
Publisher:American Chemical Society
ISSN:1948-5875
ISSN (Online):1948-5875
Copyright Holders:Copyright © 2013 American Chemical Society
First Published:First published in ACS Medicinal Chemistry Letters
Publisher Policy:Reproduced in accordance with the copyright policy of the publisher

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