Structural Insights into Endothelin Receptor Signaling

Endothelins and their receptors, ETA and 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 the...

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Vydané v:Journal of biochemistry (Tokyo) Ročník 174; číslo 4; s. 317
Hlavní autori: Shihoya, Wataru, Sano, Fumiya K, Nureki, Osamu
Médium: Journal Article
Jazyk:English
Vydavateľské údaje: England 01.10.2023
Predmet:
SBDD
Endothelin
Vascular system
Structural biology
G-protein-coupled receptor
ISSN:1756-2651, 1756-2651
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Shrnutí:Endothelins and their receptors, ETA and 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.
Bibliografia:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
content type line 23
ObjectType-Review-1
ISSN:1756-2651
1756-2651
DOI:10.1093/jb/mvad055