Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation

Agonists of the orexin receptor 2 (OX2R) show promise in the treatment of narcolepsy. Cryo-EM structures of active-state OX2R bound to an endogenous peptide agonist and a small-molecule agonist suggest a molecular mechanism that rationalizes both receptor activation and inhibition.

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Autores principales:	Chuan Hong, Noel J. Byrne, Beata Zamlynny, Srivanya Tummala, Li Xiao, Jennifer M. Shipman, Andrea T. Partridge, Christina Minnick, Michael J. Breslin, Michael T. Rudd, Shawn J. Stachel, Vanessa L. Rada, Jeffrey C. Kern, Kira A. Armacost, Scott A. Hollingsworth, Julie A. O’Brien, Dawn L. Hall, Terrence P. McDonald, Corey Strickland, Alexei Brooun, Stephen M. Soisson, Kaspar Hollenstein
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/71020c0fdeec442e80fbd53a66967a19
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spelling	oai:doaj.org-article:71020c0fdeec442e80fbd53a66967a192021-12-02T10:44:18ZStructures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation10.1038/s41467-021-21087-62041-1723https://doaj.org/article/71020c0fdeec442e80fbd53a66967a192021-02-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-21087-6https://doaj.org/toc/2041-1723Agonists of the orexin receptor 2 (OX2R) show promise in the treatment of narcolepsy. Cryo-EM structures of active-state OX2R bound to an endogenous peptide agonist and a small-molecule agonist suggest a molecular mechanism that rationalizes both receptor activation and inhibition.Chuan HongNoel J. ByrneBeata ZamlynnySrivanya TummalaLi XiaoJennifer M. ShipmanAndrea T. PartridgeChristina MinnickMichael J. BreslinMichael T. RuddShawn J. StachelVanessa L. RadaJeffrey C. KernKira A. ArmacostScott A. HollingsworthJulie A. O’BrienDawn L. HallTerrence P. McDonaldCorey StricklandAlexei BroounStephen M. SoissonKaspar HollensteinNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-11 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Chuan Hong Noel J. Byrne Beata Zamlynny Srivanya Tummala Li Xiao Jennifer M. Shipman Andrea T. Partridge Christina Minnick Michael J. Breslin Michael T. Rudd Shawn J. Stachel Vanessa L. Rada Jeffrey C. Kern Kira A. Armacost Scott A. Hollingsworth Julie A. O’Brien Dawn L. Hall Terrence P. McDonald Corey Strickland Alexei Brooun Stephen M. Soisson Kaspar Hollenstein Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation
description	Agonists of the orexin receptor 2 (OX2R) show promise in the treatment of narcolepsy. Cryo-EM structures of active-state OX2R bound to an endogenous peptide agonist and a small-molecule agonist suggest a molecular mechanism that rationalizes both receptor activation and inhibition.
format	article
author	Chuan Hong Noel J. Byrne Beata Zamlynny Srivanya Tummala Li Xiao Jennifer M. Shipman Andrea T. Partridge Christina Minnick Michael J. Breslin Michael T. Rudd Shawn J. Stachel Vanessa L. Rada Jeffrey C. Kern Kira A. Armacost Scott A. Hollingsworth Julie A. O’Brien Dawn L. Hall Terrence P. McDonald Corey Strickland Alexei Brooun Stephen M. Soisson Kaspar Hollenstein
author_facet	Chuan Hong Noel J. Byrne Beata Zamlynny Srivanya Tummala Li Xiao Jennifer M. Shipman Andrea T. Partridge Christina Minnick Michael J. Breslin Michael T. Rudd Shawn J. Stachel Vanessa L. Rada Jeffrey C. Kern Kira A. Armacost Scott A. Hollingsworth Julie A. O’Brien Dawn L. Hall Terrence P. McDonald Corey Strickland Alexei Brooun Stephen M. Soisson Kaspar Hollenstein
author_sort	Chuan Hong
title	Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation
title_short	Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation
title_full	Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation
title_fullStr	Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation
title_full_unstemmed	Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation
title_sort	structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/71020c0fdeec442e80fbd53a66967a19
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Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation

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