title: FFA4 receptor (GPR120): A hot target for the development of anti-diabetic therapies.
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.
authors.affiliation: Key Laboratory Experimental Teratology of the Ministry of Education and Department of Biochemistry and Molecular Biology, Shandong University, School of Medicine, Jinan, Shandong, China; Qilu Hospital of Shandong University, Jinan, Shandong, China; Shandong Provincial School Key Laboratory for Protein Science of Chronic Degenerative Diseases, Jinan, Shandong, China.
authors.forename: Hong-Da
authors.initials: HD
authors.lastname: Liu
authors.affiliation: Key Laboratory Experimental Teratology of the Ministry of Education and Department of Biochemistry and Molecular Biology, Shandong University, School of Medicine, Jinan, Shandong, China; Shandong Provincial School Key Laboratory for Protein Science of Chronic Degenerative Diseases, Jinan, Shandong, China.
authors.forename: Wen-bo
authors.initials: WB
authors.lastname: Wang
authors.affiliation: Shandong Provincial Key Laboratory of Animal Cells and Developmental Biology, Shandong University School of Life Sciences, Jinan, Shandong, China. Electronic address: xuzg@sdu.edu.cn.
authors.forename: Zhi-gang
authors.initials: ZG
authors.lastname: Xu
authors.affiliation: Department of Digestive Diseases, Qianfoshan Hospital of Shandong Province, Jinan, Shandong 250100, China.
authors.forename: Chang-hong
authors.initials: CH
authors.lastname: Liu
authors.affiliation: Key Laboratory Experimental Teratology of the Ministry of Education and Department of Biochemistry and Molecular Biology, Shandong University, School of Medicine, Jinan, Shandong, China; Shandong Provincial School Key Laboratory for Protein Science of Chronic Degenerative Diseases, Jinan, Shandong, China.
authors.forename: Dong-fang
authors.initials: DF
authors.lastname: He
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology of Natural Products (MOE), School of Pharmacy, Shandong University, Jinan, Shandong, China.
authors.forename: Lv-Pei
authors.initials: LP
authors.lastname: Du
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology of Natural Products (MOE), School of Pharmacy, Shandong University, Jinan, Shandong, China.
authors.forename: Min-Yong
authors.initials: MY
authors.lastname: Li
authors.affiliation: Qilu Hospital of Shandong University, Jinan, Shandong, China; Shandong Provincial School Key Laboratory for Protein Science of Chronic Degenerative Diseases, Jinan, Shandong, China. Electronic address: yuxiao@sdu.edu.cn.
authors.forename: Xiao
authors.initials: X
authors.lastname: Yu
authors.affiliation: Key Laboratory Experimental Teratology of the Ministry of Education and Department of Biochemistry and Molecular Biology, Shandong University, School of Medicine, Jinan, Shandong, China; Shandong Provincial School Key Laboratory for Protein Science of Chronic Degenerative Diseases, Jinan, Shandong, China. Electronic address: sunjinpeng@sdu.edu.cn.
authors.forename: Jin-peng
authors.initials: JP
authors.lastname: Sun
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D019393:Arrestin / Q000378:metabolism; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D008969:Molecular Sequence Data; D058990:Molecular Targeted Therapy / Q000379:methods*; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D019393:Arrestin; D007004:Hypoglycemic Agents; D043562:Receptors, G-Protein-Coupled
keywords: Arrestin; Biased signaling; GPR120; Glucose metabolism; Lipid