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

ABSTRACT: Till the 21^st 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 21^st 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-? shedding assay.

SUBMITTER: Son SE

PROVIDER: S-EPMC7771848 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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

Son So-Eun SE Kim Nam-Jung NJ Im Dong-Soon DS

Biomolecules & therapeutics 20210101 1

Till the 21<sup>st</sup> 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 21<sup>st</sup> 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 k ...[more]

PMID: 33372166

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