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

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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Detalles Bibliográficos
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
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Acceso en línea:https://doaj.org/article/71020c0fdeec442e80fbd53a66967a19
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Sumario: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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