FFA4 receptor (GPR120): A hot target for the development of anti-diabetic therapies
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...
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| Published in | European journal of pharmacology Vol. 763; no. Pt B; pp. 160 - 168 |
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| Main Authors | , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
Netherlands
Elsevier B.V
15.09.2015
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| Subjects | |
| Online Access | Get full text |
| ISSN | 0014-2999 1879-0712 1879-0712 |
| DOI | 10.1016/j.ejphar.2015.06.028 |
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| 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. |
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| AbstractList | 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. 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.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. |
| Author | Wang, Wen-bo Liu, Hong-Da Li, Min-Yong Xu, Zhi-gang Sun, Jin-peng Liu, Chang-hong He, Dong-fang Yu, Xiao Du, Lv-Pei |
| Author_xml | – sequence: 1 givenname: Hong-Da surname: Liu fullname: Liu, Hong-Da organization: Key Laboratory Experimental Teratology of the Ministry of Education and Department of Biochemistry and Molecular Biology, Shandong University, School of Medicine, Jinan, Shandong, China – sequence: 2 givenname: Wen-bo surname: Wang fullname: Wang, Wen-bo organization: Key Laboratory Experimental Teratology of the Ministry of Education and Department of Biochemistry and Molecular Biology, Shandong University, School of Medicine, Jinan, Shandong, China – sequence: 3 givenname: Zhi-gang surname: Xu fullname: Xu, Zhi-gang email: xuzg@sdu.edu.cn organization: Shandong Provincial Key Laboratory of Animal Cells and Developmental Biology, Shandong University School of Life Sciences, Jinan, Shandong, China – sequence: 4 givenname: Chang-hong surname: Liu fullname: Liu, Chang-hong organization: Department of Digestive Diseases, Qianfoshan Hospital of Shandong Province, Jinan, Shandong 250100, China – sequence: 5 givenname: Dong-fang surname: He fullname: He, Dong-fang organization: Key Laboratory Experimental Teratology of the Ministry of Education and Department of Biochemistry and Molecular Biology, Shandong University, School of Medicine, Jinan, Shandong, China – sequence: 6 givenname: Lv-Pei surname: Du fullname: Du, Lv-Pei organization: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology of Natural Products (MOE), School of Pharmacy, Shandong University, Jinan, Shandong, China – sequence: 7 givenname: Min-Yong surname: Li fullname: Li, Min-Yong organization: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology of Natural Products (MOE), School of Pharmacy, Shandong University, Jinan, Shandong, China – sequence: 8 givenname: Xiao surname: Yu fullname: Yu, Xiao email: yuxiao@sdu.edu.cn organization: Qilu Hospital of Shandong University, Jinan, Shandong, China – sequence: 9 givenname: Jin-peng surname: Sun fullname: Sun, Jin-peng email: sunjinpeng@sdu.edu.cn organization: Key Laboratory Experimental Teratology of the Ministry of Education and Department of Biochemistry and Molecular Biology, Shandong University, School of Medicine, Jinan, Shandong, China |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/26123847$$D View this record in MEDLINE/PubMed |
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| Snippet | 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... |
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| SubjectTerms | 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 |
| Title | FFA4 receptor (GPR120): A hot target for the development of anti-diabetic therapies |
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