FFA4 receptor (GPR120): A hot target for the development of anti-diabetic therapies

• Published in: European journal of pharmacology Vol. 763; no. Pt B; pp. 160 - 168
• Main Authors: Liu, Hong-Da, Wang, Wen-bo, Xu, Zhi-gang, Liu, Chang-hong, He, Dong-fang, Du, Lv-Pei, Li, Min-Yong, Yu, Xiao, Sun, Jin-peng
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 15.09.2015
• Subjects: Amino Acid Sequence; Animals; Arrestin; Arrestin - metabolism; Biased signaling; Drug Discovery - methods; Glucose metabolism; GPR120; Humans; Hypoglycemic Agents - pharmacology; Lipid; Molecular Sequence Data; Molecular Targeted Therapy - methods; Receptors, G-Protein-Coupled - chemistry; Receptors, G-Protein-Coupled - genetics; Receptors, G-Protein-Coupled - metabolism; Signal Transduction - drug effects; Glucose metabolism; Biased signaling; Arrestin; GPR120; Lipid
• ISSN: 0014-2999; 1879-0712; 1879-0712
• DOI: 10.1016/j.ejphar.2015.06.028

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.