skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: 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

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

References (46)

PRODRG : a tool for high-throughput crystallography of protein–ligand complexes journal July 2004
The G-Protein-Coupled Receptors in the Human Genome Form Five Main Families. Phylogenetic Analysis, Paralogon Groups, and Fingerprints journal June 2003
Crystallizing Membrane Proteins for Structure Determination: Use of Lipidic Mesophases journal June 2009
Structure of a nanobody-stabilized active state of the β2 adrenoceptor journal January 2011
Crystal structure of the µ-opioid receptor bound to a morphinan antagonist journal March 2012
Activation and allosteric modulation of a muscarinic acetylcholine receptor journal November 2013
Fitting molecular fragments into electron density journal December 2007
AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibility journal December 2009
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
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
Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists journal October 2010
MolProbity : all-atom structure validation for macromolecular crystallography journal December 2009
DSX : A Knowledge-Based Scoring Function for the Assessment of Protein–Ligand Complexes journal October 2011
Conformational analysis of N,N-disubstituted-1,4-diazepane orexin receptor antagonists and implications for receptor binding journal June 2009
Features and development of Coot journal March 2010
Orexins and Orexin Receptors: A Family of Hypothalamic Neuropeptides and G Protein-Coupled Receptors that Regulate Feeding Behavior journal February 1998
Crystal Structure of an Archaeal Glycogen Synthase: INSIGHTS INTO OLIGOMERIZATION AND SUBSTRATE BINDING OF EUKARYOTIC GLYCOGEN SYNTHASES journal November 2005
Promotion of sleep by targeting the orexin system in rats, dogs and humans journal January 2007
PHENIX: a comprehensive Python-based system for macromolecular structure solution journal January 2010
Hypocretin (orexin) deficiency in human narcolepsy journal January 2000
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
TLSMD web server for the generation of multi-group TLS models journal January 2006
Extending the Applicability of the Nonlinear Poisson−Boltzmann Equation:  Multiple Dielectric Constants and Multivalent Ions journal July 2001
Rapid Context-Dependent Ligand Desolvation in Molecular Docking journal August 2010
Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists journal September 2011
Amino and Carboxyl Terminal Modifications to Facilitate the Production and Purification of a G Protein-Coupled Receptor journal October 1995
Structure of the agonist-bound neurotensin receptor journal October 2012
GPCR Engineering Yields High-Resolution Structural Insights into  2-Adrenergic Receptor Function journal October 2007
Structure and dynamics of the M3 muscarinic acetylcholine receptor journal February 2012
Structure-based discovery of  2-adrenergic receptor ligands journal April 2009
LIGPLOT: a program to generate schematic diagrams of protein-ligand interactions journal January 1995
Automated Docking Screens: A Feasibility Study journal September 2009
Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution in Escherichia coli journal January 2014
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
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
Crystallizing membrane proteins using lipidic mesophases journal April 2009
Discovery and development of orexin receptor antagonists as therapeutics for insomnia: Development of orexin receptor antagonists for insomnia journal December 2013
Narcolepsy in orexin Knockout Mice journal August 1999
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
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
[20] Processing of X-ray diffraction data collected in oscillation mode book January 1997
Structure of a β1-adrenergic G-protein-coupled receptor journal June 2008
Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor journal January 2010
Phaser crystallographic software journal July 2007
Characterisation of the binding of [ 3 H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor journal January 2004

Similar Records

Related Subjects