A Gpr120 Selective Agonist Improves Insulin Resistance and Chronic Inflammation

It is well known that the omega-3 fatty acids (ω3-FAs) contained in fish oils can exert potent anti-inflammatory effects 1-4. ω3-FAs are commonly consumed as fish products, dietary supplements, and pharmaceuticals and a number of health benefits have been ascribed to them, including a reduction in plasma triglyceride levels, amelioration of atherosclerosis, and increased insulin sensitivity 5-7. We reported that Gpr120 is the functional receptor/ sensor for these fatty acids and that ω3-FAs produce robust anti-inflammatory, insulin sensitizing effects, both in vivo and in vitro in a Gpr120-dependent manner 8. Indeed, human genetic variants in the Gpr120 gene had been described which predispose to obesity and diabetes 9. However, the amount of fish oils which would have to be consumed to sustain chronic agonism of Gpr120 is too high to be practical, and, thus, a high affinity, small molecule Gpr120 agonist would be of potential clinical benefit. Accordingly, Gpr120 is a widely studied drug discovery target within the pharmaceutical industry. Gpr40 is another Users may view, print, copy, and download text and data-mine the content in such documents, for the purposes of academic research, subject always to the full Conditions of use:http://www.nature.com/authors/editorial_policies/license.html#term