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Discovery of a potent and selective GPR120 agonist

Shimpukade, B., Hudson, B.D., Hogaard, C.K., Milligan, G., and Ulven, T. (2012) Discovery of a potent and selective GPR120 agonist. Journal of Medicinal Chemistry, 55 (9). pp. 4511-4515. ISSN 0022-2623 (doi:10.1021/jm300215x)

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Abstract

GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for treatment of type 2 diabetes and metabolic diseases. Further investigation is however hindered by the lack of suitable receptor modulators. Screening of FFA1 ligands provided a lead with moderate activity on GPR120 and moderate selectivity over FFA1. Optimization led to the discovery of the first potent and selective GPR120 agonist.

Item Type:Article
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Hudson, Dr Brian and Milligan, Prof Graeme
Authors: Shimpukade, B., Hudson, B.D., Hogaard, C.K., Milligan, G., and Ulven, T.
Subjects:Q Science > QD Chemistry
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:23 April 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