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

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 n...

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Autores principales: Son, So-Eun, Kim, Nam-Jung, Im, Dong-Soon
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Korean Society of Applied Pharmacology 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7771848/
https://www.ncbi.nlm.nih.gov/pubmed/33372166
http://dx.doi.org/10.4062/biomolther.2020.213
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author Son, So-Eun
Kim, Nam-Jung
Im, Dong-Soon
author_facet Son, So-Eun
Kim, Nam-Jung
Im, Dong-Soon
author_sort Son, So-Eun
collection PubMed
description 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.
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spelling pubmed-77718482021-01-01 Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science Son, So-Eun Kim, Nam-Jung Im, Dong-Soon Biomol Ther (Seoul) Review 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. The Korean Society of Applied Pharmacology 2021-01-01 2021-01-01 /pmc/articles/PMC7771848/ /pubmed/33372166 http://dx.doi.org/10.4062/biomolther.2020.213 Text en Copyright © 2021, The Korean Society of Applied Pharmacology This is an open-access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/4.0) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review
Son, So-Eun
Kim, Nam-Jung
Im, Dong-Soon
Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
title Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
title_full Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
title_fullStr Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
title_full_unstemmed Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
title_short Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
title_sort development of free fatty acid receptor 4 (ffa4/gpr120) agonists in health science
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7771848/
https://www.ncbi.nlm.nih.gov/pubmed/33372166
http://dx.doi.org/10.4062/biomolther.2020.213
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