Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science

  • Son, So-Eun (Department of Pharmacy, College of Pharmacy, and Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University) ;
  • Kim, Nam-Jung (Department of Pharmacy, College of Pharmacy, and Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University) ;
  • Im, Dong-Soon (Department of Pharmacy, College of Pharmacy, and Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University)
  • Received : 2020.11.25
  • Accepted : 2020.11.30
  • Published : 2021.01.01
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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.

Keywords

References

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