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Structural insights into endothelin receptor signalling
Endothelins and their receptors, type A (ET(A)) and type B (ET(B)), modulate vital cellular processes, including growth, survival, invasion and angiogenesis, through multiple G proteins. This review highlights the structural determinations of these receptors by X-ray crystallography and cryo-electro...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Oxford University Press
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10533325/ https://www.ncbi.nlm.nih.gov/pubmed/37491722 http://dx.doi.org/10.1093/jb/mvad055 |
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author | Shihoya, Wataru Sano, Fumiya K Nureki, Osamu |
author_facet | Shihoya, Wataru Sano, Fumiya K Nureki, Osamu |
author_sort | Shihoya, Wataru |
collection | PubMed |
description | Endothelins and their receptors, type A (ET(A)) and type B (ET(B)), modulate vital cellular processes, including growth, survival, invasion and angiogenesis, through multiple G proteins. This review highlights the structural determinations of these receptors by X-ray crystallography and cryo-electron microscopy, and their activation mechanisms by endothelins. Explorations of the conformational changes upon receptor activation have provided insights into the unique G-protein coupling feature of the endothelin receptors. The review further delves into the binding modes of the clinical antagonist and the inverse agonists. These findings significantly contribute to understanding the mechanism of G-protein activation and have potential implications for drug development, particularly in the context of vasodilatory antagonists and agonists targeting the endothelin receptors. |
format | Online Article Text |
id | pubmed-10533325 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | Oxford University Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-105333252023-09-28 Structural insights into endothelin receptor signalling Shihoya, Wataru Sano, Fumiya K Nureki, Osamu J Biochem JB Review Endothelins and their receptors, type A (ET(A)) and type B (ET(B)), modulate vital cellular processes, including growth, survival, invasion and angiogenesis, through multiple G proteins. This review highlights the structural determinations of these receptors by X-ray crystallography and cryo-electron microscopy, and their activation mechanisms by endothelins. Explorations of the conformational changes upon receptor activation have provided insights into the unique G-protein coupling feature of the endothelin receptors. The review further delves into the binding modes of the clinical antagonist and the inverse agonists. These findings significantly contribute to understanding the mechanism of G-protein activation and have potential implications for drug development, particularly in the context of vasodilatory antagonists and agonists targeting the endothelin receptors. Oxford University Press 2023-07-26 /pmc/articles/PMC10533325/ /pubmed/37491722 http://dx.doi.org/10.1093/jb/mvad055 Text en © The Author(s) 2023. Published by Oxford University Press on behalf of the Japanese Biochemical Society. https://creativecommons.org/licenses/by-nc/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (https://creativecommons.org/licenses/by-nc/4.0/), which permits non-commercial re-use, distribution, and reproduction in any medium, provided the original work is properly cited. For commercial re-use, please contact journals.permissions@oup.com |
spellingShingle | JB Review Shihoya, Wataru Sano, Fumiya K Nureki, Osamu Structural insights into endothelin receptor signalling |
title | Structural insights into endothelin receptor signalling |
title_full | Structural insights into endothelin receptor signalling |
title_fullStr | Structural insights into endothelin receptor signalling |
title_full_unstemmed | Structural insights into endothelin receptor signalling |
title_short | Structural insights into endothelin receptor signalling |
title_sort | structural insights into endothelin receptor signalling |
topic | JB Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10533325/ https://www.ncbi.nlm.nih.gov/pubmed/37491722 http://dx.doi.org/10.1093/jb/mvad055 |
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