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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Main Authors: Wataru Shihoya, Tamaki Izume, Asuka Inoue, Keitaro Yamashita, Francois Marie Ngako Kadji, Kunio Hirata, Junken Aoki, Tomohiro Nishizawa, Osamu Nureki
Format: Article
Language:English
Published: Nature Portfolio 2018-11-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-018-07094-0
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author Wataru Shihoya
Tamaki Izume
Asuka Inoue
Keitaro Yamashita
Francois Marie Ngako Kadji
Kunio Hirata
Junken Aoki
Tomohiro Nishizawa
Osamu Nureki
author_facet Wataru Shihoya
Tamaki Izume
Asuka Inoue
Keitaro Yamashita
Francois Marie Ngako Kadji
Kunio Hirata
Junken Aoki
Tomohiro Nishizawa
Osamu Nureki
author_sort Wataru Shihoya
collection DOAJ
description 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.
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spelling doaj.art-a2d527b16f98446e9ee5dcdca8a86e972022-12-21T18:03:52ZengNature PortfolioNature Communications2041-17232018-11-019111110.1038/s41467-018-07094-0Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activationWataru Shihoya0Tamaki Izume1Asuka Inoue2Keitaro Yamashita3Francois Marie Ngako Kadji4Kunio Hirata5Junken Aoki6Tomohiro Nishizawa7Osamu Nureki8Department of Biological Sciences, Graduate School of Science, The University of TokyoDepartment of Biological Sciences, Graduate School of Science, The University of TokyoGraduate School of Pharmaceutical Sciences, Tohoku UniversityDepartment of Biological Sciences, Graduate School of Science, The University of TokyoGraduate School of Pharmaceutical Sciences, Tohoku UniversityRIKEN SPring-8 CenterGraduate School of Pharmaceutical Sciences, Tohoku UniversityDepartment of Biological Sciences, Graduate School of Science, The University of TokyoDepartment of Biological Sciences, Graduate School of Science, The University of TokyoSignalling 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.https://doi.org/10.1038/s41467-018-07094-0
spellingShingle Wataru Shihoya
Tamaki Izume
Asuka Inoue
Keitaro Yamashita
Francois Marie Ngako Kadji
Kunio Hirata
Junken Aoki
Tomohiro Nishizawa
Osamu Nureki
Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation
Nature Communications
title Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation
title_full Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation
title_fullStr Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation
title_full_unstemmed Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation
title_short Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation
title_sort crystal structures of human etb receptor provide mechanistic insight into receptor activation and partial activation
url https://doi.org/10.1038/s41467-018-07094-0
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