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Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science

Biomolecules & Therapeutics 2021년 29권 1호 p.22 ~ 30
손소은, 김남중, 임동순,
소속 상세정보
손소은 ( Son So-Eun ) - Kyung Hee University College of Pharmacy Department of Pharmacy
김남중 ( Kim Nam-Jung ) - Kyung Hee University College of Pharmacy Department of Pharmacy
임동순 ( Im Dong-Soon ) - Kyung Hee University College of Pharmacy Department of Pharmacy

Abstract


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.

키워드

GPR120; FFA4; G protein-coupled receptor; Agonist; Drug development

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