Discovery of a potent and selective GPR120 agonist (original) (raw)
Shimpukade, B., Hudson, B.D. 
ORCID: https://orcid.org/0000-0001-7059-0091, Hogaard, C.K., Milligan, G. ORCID: https://orcid.org/0000-0002-6946-3519 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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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: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| 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 > School of Molecular Biosciences |
| Journal Name: | Journal of Medicinal Chemistry |
| ISSN: | 0022-2623 |
| Published Online: | 23 April 2012 |
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