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

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-alpha shedding assay.

Automated summary

The discovery of G protein-coupled receptors (GPCRs) for free fatty acids in the early 21st century led to a new field of research and significant implications for drug discovery. Free fatty acid receptor 4 (FFA4, GPR120) plays a crucial role in regulating obesity-induced metaflammation and GLP-1 secretion, making it an important target for drug development. Various FFA4 agonists have been developed and studied for their potential applications in pathophysiology and drug discovery.