Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation

Signalling through the endothelin receptor ETB, a class A GPCR, induces nitric oxide-mediated vasorelaxation. Here the authors present the crystal structures of the human ETB receptor bound to the peptide hormone endothelin-3 and in complex with the ETB-selective partial agonist IRL1620 and discuss...

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Autores principales: Wataru Shihoya, Tamaki Izume, Asuka Inoue, Keitaro Yamashita, Francois Marie Ngako Kadji, Kunio Hirata, Junken Aoki, Tomohiro Nishizawa, Osamu Nureki
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2018
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Acceso en línea:https://doaj.org/article/a2d527b16f98446e9ee5dcdca8a86e97
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Sumario:Signalling through the endothelin receptor ETB, a class A GPCR, induces nitric oxide-mediated vasorelaxation. Here the authors present the crystal structures of the human ETB receptor bound to the peptide hormone endothelin-3 and in complex with the ETB-selective partial agonist IRL1620 and discuss mechanistic implications for receptor activation.