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Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties

Christiansen, E. et al. (2012) Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. Journal of Medicinal Chemistry, 55 (14). pp. 6624-6628. ISSN 0022-2623 (doi:10.1021/jm3002026)

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Abstract

FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage on 5. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.

Item Type:Article
Status:Published
Refereed:Yes
Glasgow Author(s):Hudson, Dr Brian and Milligan, Prof Graeme
Authors: Christiansen, E., Due-Hansen, M.E., Urban, C., Grundmann, M., Schröder, R., Hudson, B.D., Milligan, G., Cawthorne, M.A., Kostenis, E., Kassack, M.U., and Ulven, T.
College/School:College of Medical Veterinary and Life Sciences > Institute of Molecular Cell and Systems Biology
Journal Name:Journal of Medicinal Chemistry
ISSN:0022-2623
Published Online:25 June 2012

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Project CodeAward NoProject NamePrincipal InvestigatorFunder's NameFunder RefLead Dept
589821Identification of novel FFA1 and GPR120 ligands and their use in elucidating the pharmacology, function, and clinical utility of these receptors in the treatment of obesity and diabetesBrian HudsonCanadian Institutes of Health ResearchCIHRRI MOLECULAR CELL & SYSTEMS BIOLOGY