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KMID : 0606920210290010022
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Biomolecules & Therapeutics
2021 Volume.29 No. 1 p.22 ~ p.30
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Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
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Son So-Eun
Kim Nam-Jung
Im Dong-Soon
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Abstract
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Till the 21st century, fatty acids were considered as merely building blocks for triglycerides, phospholipids, or cholesteryl esters. However, the discovery of G protein-coupled receptors (GPCRs) for free fatty acids at the beginning of the 21st century challenged that idea and paved way for a new field of research, merged into the field of receptor pharmacology for intercellular lipid mediators. Among the GPCRs for free fatty acids, free fatty acid receptor 4 (FFA4, also known as GPR120) recognizes long-chain polyunsaturated fatty acids such as DHA and EPA. It is significant in drug discovery because it regulates obesity-induced metaflammation and GLP-1 secretion. Our study reviews information on newly developed FFA4 agonists and their application in pathophysiologic studies and drug discovery. It also offers a potency comparison of the FFA4 agonists in an AP-TGF-α shedding assay.
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KEYWORD
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GPR120, FFA4, G protein-coupled receptor, Agonist, Drug development
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