Skip to main content
U.S. Department of Energy
Office of Scientific and Technical Information

Crystal structure of the human OX[subscript 2] orexin receptor bound to the insomnia drug suvorexant

Journal Article · · Nature
DOI:https://doi.org/10.1038/nature14035· OSTI ID:1177437

Abstract not provided

Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
OTHERNIGMS
OSTI ID:
1177437
Journal Information:
Nature, Journal Name: Nature Journal Issue: 03, 2015 Vol. 518
Country of Publication:
United States
Language:
ENGLISH

References (47)

Characterisation of the binding of [ 3 H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor journal January 2004
Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution in Escherichia coli journal January 2014
Activation and allosteric modulation of a muscarinic acetylcholine receptor journal November 2013
PRODRG : a tool for high-throughput crystallography of protein–ligand complexes journal July 2004
Structure of the agonist-bound neurotensin receptor journal October 2012
Discovery of the Dual Orexin Receptor Antagonist [(7 R )-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2 H -1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia journal July 2010
Hypocretin (orexin) deficiency in human narcolepsy journal January 2000
Structure-based discovery of  2-adrenergic receptor ligands journal April 2009
Promotion of sleep by targeting the orexin system in rats, dogs and humans journal January 2007
Orexin Receptor Type-1 Couples Exclusively to Pertussis Toxin-Insensitive G-Proteins, While Orexin Receptor Type-2 Couples to Both Pertussis Toxin-Sensitive and -Insensitive G-Proteins journal January 2003
Fitting molecular fragments into electron density journal December 2007
Narcolepsy in orexin Knockout Mice journal August 1999
Crystallizing membrane proteins using lipidic mesophases journal April 2009
Safety and efficacy of suvorexant during 1-year treatment of insomnia with subsequent abrupt treatment discontinuation: a phase 3 randomised, double-blind, placebo-controlled trial journal May 2014
LIGPLOT: a program to generate schematic diagrams of protein-ligand interactions journal January 1995
Features and development of Coot journal March 2010
[20] Processing of X-ray diffraction data collected in oscillation mode book January 1997
Crystal Structure of an Archaeal Glycogen Synthase: INSIGHTS INTO OLIGOMERIZATION AND SUBSTRATE BINDING OF EUKARYOTIC GLYCOGEN SYNTHASES journal November 2005
TLSMD web server for the generation of multi-group TLS models journal January 2006
Mapping the Binding Pocket of Dual Antagonist Almorexant to Human Orexin 1 and Orexin 2 Receptors: Comparison with the Selective OX 1 Antagonist SB-674042 and the Selective OX 2 Antagonist N -Ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]- N -pyridin-3-ylmethyl-acetamide (EMPA) journal April 2010
Structure and dynamics of the M3 muscarinic acetylcholine receptor journal February 2012
Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor journal January 2010
Conformational analysis of N,N-disubstituted-1,4-diazepane orexin receptor antagonists and implications for receptor binding journal June 2009
PHENIX: a comprehensive Python-based system for macromolecular structure solution journal January 2010
Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor: EMPA: a selective antagonist of the OX2 receptor journal April 2009
Extending the Applicability of the Nonlinear Poisson−Boltzmann Equation:  Multiple Dielectric Constants and Multivalent Ions journal July 2001
MolProbity : all-atom structure validation for macromolecular crystallography journal December 2009
Phaser crystallographic software journal July 2007
Crystallizing Membrane Proteins for Structure Determination: Use of Lipidic Mesophases journal June 2009
The Sleep Disorder Canine Narcolepsy Is Caused by a Mutation in the Hypocretin (Orexin) Receptor 2 Gene journal August 1999
The hypocretins/orexins: integrators of multiple physiological functions: Orexins integrate physiological functions journal December 2013
Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists journal September 2011
GPCR Engineering Yields High-Resolution Structural Insights into  2-Adrenergic Receptor Function journal October 2007
Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists journal October 2010
Structure of a β1-adrenergic G-protein-coupled receptor journal June 2008
Rapid Context-Dependent Ligand Desolvation in Molecular Docking journal August 2010
Crystal structure of the µ-opioid receptor bound to a morphinan antagonist journal March 2012
Comparative Performance Assessment of the Conformational Model Generators Omega and Catalyst:  A Large-Scale Survey on the Retrieval of Protein-Bound Ligand Conformations journal July 2006
The G-Protein-Coupled Receptors in the Human Genome Form Five Main Families. Phylogenetic Analysis, Paralogon Groups, and Fingerprints journal June 2003
Structure of a nanobody-stabilized active state of the β2 adrenoceptor journal January 2011
AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibility journal December 2009
Activation of the β 2 -Adrenergic Receptor Involves Disruption of an Ionic Lock between the Cytoplasmic Ends of Transmembrane Segments 3 and 6 journal May 2001
DSX : A Knowledge-Based Scoring Function for the Assessment of Protein–Ligand Complexes journal October 2011
Amino and Carboxyl Terminal Modifications to Facilitate the Production and Purification of a G Protein-Coupled Receptor journal October 1995
Discovery and development of orexin receptor antagonists as therapeutics for insomnia: Development of orexin receptor antagonists for insomnia journal December 2013
Orexins and Orexin Receptors: A Family of Hypothalamic Neuropeptides and G Protein-Coupled Receptors that Regulate Feeding Behavior journal February 1998
Automated Docking Screens: A Feasibility Study journal September 2009

Similar Records

Structure and ligand-binding mechanism of the human OX[subscript 1] and OX[subscript 2] orexin receptors
Journal Article · Tue May 10 00:00:00 EDT 2016 · Nature Structural & Molecular Biology · OSTI ID:1252768

Agonist-bound structure of the human P2Y[subscript 12] receptor
Journal Article · Wed Apr 30 00:00:00 EDT 2014 · Nature · OSTI ID:1179486

Structure of the human P2Y[subscript 12] receptor in complex with an antithrombotic drug
Journal Article · Thu Jul 10 00:00:00 EDT 2014 · Nature · OSTI ID:1131360

Related Subjects