Molecular Pharmacology of GPR 120 Selective Agonists

http://www.sciencedirect.com/science/article/pii/S0014299915300911

GPR 120 agonist is another candidate for Diabetics.

Abstract

Free Fatty Acid 4 receptor (FFA4 receptor or GPR120), a rhodopsin-like G protein coupled receptor (GPCR) subfamily member, is a receptor that senses specific fatty acids such as ω-3 fatty acid in fish oil or the endogenous signaling lipid, PHASA. FFA4 receptor is enriched in lung, colon and adipose tissue but is also detected in many other tissues and cells.

 

The activation of FFA4 receptor has multiple effects, including but not limited to inhibition of inflammation, improving insulin sensitivity and adipogenesis, and regulating hormone secretion from the gastro-intestinal system and pancreatic islets.

The important role of FFA4 receptor in maintaining metabolic homeostasis strongly indicates the great potential of selective FFA4 receptor agonizts to treat diabetes and inflammation.

 

In this review, we summarize recent research progress in the physiological and biochemical studies of FFA4 receptor and highlight its underlying signaling mechanisms and ligand identification to assist future research to exploit FFA4 receptor as a drug target.

 

Keywords

• GPR120;
• Glucose metabolism;
• Lipid;
• Arrestin;
• Biased signaling

http://molpharm.aspetjournals.org/content/84/5/710.full.pdf+html?sid=824be494-56be-4c5d-8660-5c68f12844b7



http://www.jbc.org/content/289/29/20345.full.pdf+html?sid=98b94460-9bca-47ff-9ff2-4cd5cc880639



http://basicmed.med.ncku.edu.tw/public/project/1439-1412238024-1.pdf