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. (doi:10.1021/jm300215x)
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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.
|Glasgow Author(s) Enlighten ID:||Hudson, Dr Brian and Milligan, Professor 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|
|Published Online:||23 April 2012|