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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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Formato: | Online Artículo Texto |
Lenguaje: | English |
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The Korean Society of Applied Pharmacology
2021
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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. |
format | Online Article Text |
id | pubmed-7771848 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | The Korean Society of Applied Pharmacology |
record_format | MEDLINE/PubMed |
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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