Property Summary

NCBI Gene PubMed Count 61
Grant Count 24
R01 Count 17
Funding $2,009,264.44
PubMed Score 24.90
PubTator Score 71.19

Knowledge Summary

Patent (7,542)

MLP Assay (2)

AID Type Active / Inconclusive / Inactive Description
624050 confirmatory 25 / 0 / 188 Counterscreen assay for antagonists of the orexin 1 receptor (OX1R; HCRTR1): Fluorescence-based cell-based dose response assay for antagonists of the orexin 2 receptor (OX2R; HCRTR2), run by assay provider
624051 confirmatory 51 / 0 / 162 Counterscreen assay for antagonists of the orexin 1 receptor (OX1R; HCRTR1): Homogeneous Time Resolved Fluorescence (HTRF)-based cell-based dose response assay for antagonists of the orexin 2 receptor (OX2R; HCRTR2), run by assay provider

Gene RIF (47)

PMID Text
26950369 The study determined structures of OX1R bound to the OX1R-selective antagonist SB-674042 and the dual antagonist suvorexant at 2.8-A and 2.75-A resolution and explored mechanisms of antagonist the subtype selectivity between OX1R and OX2R.
26653627 Heart failure patients with minor allele for rs7767652, upstream of hypocretin (orexin) receptor-2 (HCRTR2), were less likely to have improved left ventricular function and a lower prevalence of ejection fraction >35%
26555080 Rapid-onset obesity with hypothalamic dysfunction, hypoventilation, and autonomic dysregulation is highly unlikely to be caused by mutations in the exons of the HCRTR2 gene.
26289589 the nonsynonymous rs2653349 single nucleotide polymorphism (SNP) (located on the gene that encodes orexin [hypocretin] receptor 2) was selected as the most notable SNP associated with Fagerstrom Test for Nicotine Dependence.
26136476 Antibodies from vaccine-associated narcolepsy sera cross-reacted with both influenza nucleoprotein and hypocretin receptor 2.
25533960 using lipid-mediated crystallization and protein engineering with a novel fusion chimaera, the structure of the human OX2R bound to suvorexant at 2.5 A resolution is solved
25398231 our meta-analysis provides genetic evidence for a role of HCRTR2 in cluster headache
25212464 Decrease in Ox expression with normal human maturation and aging. This may contribute to changes in sleep regulation during development and with aging.
24969517 The genotypic and allelic frequencies of the rs2653349 polymorphism were different between Alzheimer's disease patients and controls. The carriage of the G allele was associated with an increased AD risk.
24599460 Orexinergic innervation and expression of genes encoding OX2R receptor are upregulated in transgenic mice at dusk.
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AA Sequence

MSGTKLEDSPPCRNWSSASELNETQEPFLNPTDYDDEEFLRYLWREYLHPKEYEWVLIAGYIIVFVVALI      1 - 70
GNVLVCVAVWKNHHMRTVTNYFIVNLSLADVLVTITCLPATLVVDITETWFFGQSLCKVIPYLQTVSVSV     71 - 140
SVLTLSCIALDRWYAICHPLMFKSTAKRARNSIVIIWIVSCIIMIPQAIVMECSTVFPGLANKTTLFTVC    141 - 210
DERWGGEIYPKMYHICFFLVTYMAPLCLMVLAYLQIFRKLWCRQIPGTSSVVQRKWKPLQPVSQPRGPGQ    211 - 280
PTKSRMSAVAAEIKQIRARRKTARMLMIVLLVFAICYLPISILNVLKRVFGMFAHTEDRETVYAWFTFSH    281 - 350
WLVYANSAANPIIYNFLSGKFREEFKAAFSCCCLGVHHRQEDRLTRGRTSTESRKSLTTQISNFDNISKL    351 - 420
SEQVVLTSISTLPAANGAGPLQNW                                                  421 - 444
//

Text Mined References (62)

PMID Year Title
26950369 2016 Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors.
26653627 2015 Systems Genomics Identifies a Key Role for Hypocretin/Orexin Receptor-2 in Human Heart Failure.
26555080 2016 Absence of mutations in HCRT, HCRTR1 and HCRTR2 in patients with ROHHAD.
26289589 2015 Associations between the orexin (hypocretin) receptor 2 gene polymorphism Val308Ile and nicotine dependence in genome-wide and subsequent association studies.
26136476 2015 Antibodies to influenza nucleoprotein cross-react with human hypocretin receptor 2.
25533960 2015 Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant.
25398231 2015 Cluster headache and the hypocretin receptor 2 reconsidered: a genetic association study and meta-analysis.
25231870 2014 Parent-of-origin-specific allelic associations among 106 genomic loci for age at menarche.
25212464 2015 Changes in orexin (hypocretin) neuronal expression with normal aging in the human hypothalamus.
24969517 2014 Is HCRTR2 a genetic risk factor for Alzheimer's disease?
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