Biomol Ther.  2021 Jan;29(1):22-30. 10.4062/biomolther.2020.213.

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

• Son SE
• Kim NJ
• Im DS

• KMID: 2510121
• DOI: http://doi.org/10.4062/biomolther.2020.213

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-α shedding assay.

Keyword

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