RDF/XMLNTriplesTurtleShow queryShare
SubjectPredicateObject
http://purl.uniprot.org/citations/26950369http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/26950369http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/26950369http://www.w3.org/2000/01/rdf-schema#comment"The orexin (also known as hypocretin) G protein-coupled receptors (GPCRs) regulate sleep and other behavioral functions in mammals, and are therapeutic targets for sleep and wake disorders. The human receptors hOX1R and hOX2R, which are 64% identical in sequence, have overlapping but distinct physiological functions and potential therapeutic profiles. We determined structures of hOX1R bound to the OX1R-selective antagonist SB-674042 and the dual antagonist suvorexant at 2.8-Å and 2.75-Å resolution, respectively, and used molecular modeling to illuminate mechanisms of antagonist subtype selectivity between hOX1R and hOX2R. The hOX1R structures also reveal a conserved amphipathic α-helix, in the extracellular N-terminal region, that interacts with orexin-A and is essential for high-potency neuropeptide activation at both receptors. The orexin-receptor crystal structures are valuable tools for the design and development of selective orexin-receptor antagonists and agonists."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.org/dc/terms/identifier"doi:10.1038/nsmb.3183"xsd:string
http://purl.uniprot.org/citations/26950369http://purl.org/dc/terms/identifier"doi:10.1038/nsmb.3183"xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Clark L."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Clark L."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Brautigam C.A."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Brautigam C.A."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Shao Z."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Shao Z."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Yin J."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Yin J."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Rosenbaum D.M."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Rosenbaum D.M."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Babaoglu K."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Babaoglu K."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Gotter A.L."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Gotter A.L."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Winrow C.J."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Winrow C.J."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Scheuermann T.H."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Scheuermann T.H."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Coleman P.J."xsd:string
http://purl.uniprot.org/citations/26950369http://purl.uniprot.org/core/author"Coleman P.J."xsd:string