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An alerting structure: human orexin receptor 1

Nature Structural & Molecular Biology volume 23, pages 265–266 (2016)Cite this article

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Structures of the human orexin receptor 1 (hOX1R) bound to a selective drug and the dual (hOX1R- and hOX2R-targeting) antagonist suvorexant reveal molecular mechanisms of selectivity in orexin-receptor subtypes.

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Figure 1: Crystal structures of the human orexin receptor 1 (hOX1R, PDB 4ZJ8)5 and human orexin receptor 2 (hOX2R, PDB 4S0V)13 bound to the anti-insomnia drug suvorexant.
Figure 2: Comparison of the orthosteric binding sites of hOX1R and hOX2R.

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Authors and Affiliations

  1. Daniel Wacker and Bryan L. Roth are at the Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA.,

    Daniel Wacker & Bryan L Roth

  2. Bryan L. Roth is also at the Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA, and at the National Institute of Mental Health Psychoactive Drug Screening Program (NIMH PDSP), School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA.,

    Bryan L Roth

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  1. Daniel Wacker
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  2. Bryan L Roth
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Correspondence to Bryan L Roth.

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Wacker, D., Roth, B. An alerting structure: human orexin receptor 1. Nat Struct Mol Biol 23, 265–266 (2016). https://doi.org/10.1038/nsmb.3198

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