Advances in the allostery of angiotensin II type 1 receptor

Angiotensin II type 1 receptor (AT1R) is a promising therapeutic target for cardiovascular diseases. Compared with orthosteric ligands, allosteric modulators attract considerable attention for drug development due to their unique advantages of high selectivity and safety. However, no allosteric modu...

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Detalles Bibliográficos
Autores principales: Zhang, Xi, Zhang, Suli, Wang, Meili, Chen, Hao, Liu, Huirong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2023
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10276441/
https://www.ncbi.nlm.nih.gov/pubmed/37330563
http://dx.doi.org/10.1186/s13578-023-01063-x
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author Zhang, Xi
Zhang, Suli
Wang, Meili
Chen, Hao
Liu, Huirong
author_facet Zhang, Xi
Zhang, Suli
Wang, Meili
Chen, Hao
Liu, Huirong
author_sort Zhang, Xi
collection PubMed
description Angiotensin II type 1 receptor (AT1R) is a promising therapeutic target for cardiovascular diseases. Compared with orthosteric ligands, allosteric modulators attract considerable attention for drug development due to their unique advantages of high selectivity and safety. However, no allosteric modulators of AT1R have been applied in clinical trials up to now. Except for the classical allosteric modulators of AT1R such as antibody, peptides and amino acids, cholesterol and biased allosteric modulators, there are non-classical allosteric modes including the ligand-independent allosteric mode, and allosteric mode of biased agonists and dimers. In addition, finding the allosteric pockets based on AT1R conformational change and interaction interface of dimers are the future of drug design. In this review, we summarize the different allosteric mode of AT1R, with a view to contribute to the development and utilization of drugs targeting AT1R allostery.
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spelling pubmed-102764412023-06-18 Advances in the allostery of angiotensin II type 1 receptor Zhang, Xi Zhang, Suli Wang, Meili Chen, Hao Liu, Huirong Cell Biosci Review Angiotensin II type 1 receptor (AT1R) is a promising therapeutic target for cardiovascular diseases. Compared with orthosteric ligands, allosteric modulators attract considerable attention for drug development due to their unique advantages of high selectivity and safety. However, no allosteric modulators of AT1R have been applied in clinical trials up to now. Except for the classical allosteric modulators of AT1R such as antibody, peptides and amino acids, cholesterol and biased allosteric modulators, there are non-classical allosteric modes including the ligand-independent allosteric mode, and allosteric mode of biased agonists and dimers. In addition, finding the allosteric pockets based on AT1R conformational change and interaction interface of dimers are the future of drug design. In this review, we summarize the different allosteric mode of AT1R, with a view to contribute to the development and utilization of drugs targeting AT1R allostery. BioMed Central 2023-06-17 /pmc/articles/PMC10276441/ /pubmed/37330563 http://dx.doi.org/10.1186/s13578-023-01063-x Text en © The Author(s) 2023 https://creativecommons.org/licenses/by/4.0/Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) . The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/ (https://creativecommons.org/publicdomain/zero/1.0/) ) applies to the data made available in this article, unless otherwise stated in a credit line to the data.
spellingShingle Review
Zhang, Xi
Zhang, Suli
Wang, Meili
Chen, Hao
Liu, Huirong
Advances in the allostery of angiotensin II type 1 receptor
title Advances in the allostery of angiotensin II type 1 receptor
title_full Advances in the allostery of angiotensin II type 1 receptor
title_fullStr Advances in the allostery of angiotensin II type 1 receptor
title_full_unstemmed Advances in the allostery of angiotensin II type 1 receptor
title_short Advances in the allostery of angiotensin II type 1 receptor
title_sort advances in the allostery of angiotensin ii type 1 receptor
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10276441/
https://www.ncbi.nlm.nih.gov/pubmed/37330563
http://dx.doi.org/10.1186/s13578-023-01063-x
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