Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
10.4062/biomolther.2020.213
- Author:
So-Eun SON
1
;
Nam-Jung KIM
;
Dong-Soon IM
Author Information
1. Department of Pharmacy, College of Pharmacy, and Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University, Seoul 02447, Republic of Korea
- Publication Type:Review
- From:Biomolecules & Therapeutics
2021;29(1):22-30
- CountryRepublic of Korea
- Language:English
-
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.
