Bharat Shimpukade, B. Hudson, Christine Kiel Hovgaard
May 2, 2012
Citations
6
Influential Citations
150
Citations
Quality indicators
Journal
Journal of medicinal chemistry
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.