Structural insights into endothelin receptor signalling.
G-protein-coupled receptor
endothelin
structural biology
vascular system
Journal
Journal of biochemistry
ISSN: 1756-2651
Titre abrégé: J Biochem
Pays: England
ID NLM: 0376600
Informations de publication
Date de publication:
29 Sep 2023
29 Sep 2023
Historique:
received:
15
05
2023
revised:
19
06
2023
accepted:
01
07
2023
medline:
4
10
2023
pubmed:
26
7
2023
entrez:
26
7
2023
Statut:
ppublish
Résumé
Endothelins and their receptors, type A (ETA) and type B (ETB), 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.
Identifiants
pubmed: 37491722
pii: 7231117
doi: 10.1093/jb/mvad055
pmc: PMC10533325
doi:
Substances chimiques
Endothelins
0
Receptors, Endothelin
0
Types de publication
Review
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
317-325Subventions
Organisme : AMED
ID : JP23ama121012
Organisme : Platform Project for Supporting Drug Discovery and Life Science Research
Organisme : The Uehara Memorial Foundation
Organisme : The Takeda Science Foundation
Organisme : ONO Medical Research Foundation
Organisme : JSPS KAKENHI
ID : 22H02751
Organisme : Platform for Drug Discovery, Informatics and Structural Life Science by the Ministry of Education, Culture, Sports, Science and Technology (MEXT)
Informations de copyright
© The Author(s) 2023. Published by Oxford University Press on behalf of the Japanese Biochemical Society.
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