Advances in the allostery of angiotensin II type 1 receptor.
Allosteric pocket
Allostery
Angiotensin II type 1 receptor
Biased ligands
Conformation
Dimers
Journal
Cell & bioscience
ISSN: 2045-3701
Titre abrégé: Cell Biosci
Pays: England
ID NLM: 101561195
Informations de publication
Date de publication:
17 Jun 2023
17 Jun 2023
Historique:
received:
30
12
2022
accepted:
31
05
2023
medline:
18
6
2023
pubmed:
18
6
2023
entrez:
17
6
2023
Statut:
epublish
Résumé
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.
Identifiants
pubmed: 37330563
doi: 10.1186/s13578-023-01063-x
pii: 10.1186/s13578-023-01063-x
pmc: PMC10276441
doi:
Types de publication
Journal Article
Review
Langues
eng
Pagination
110Subventions
Organisme : National Natural Science Foundation of China
ID : 91539205
Organisme : National Natural Science Foundation of China
ID : 81900415
Informations de copyright
© 2023. The Author(s).
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