Property Summary

NCBI Gene PubMed Count 61
Grant Count 22
R01 Count 15
Funding $2,730,112.53
PubMed Score 138.33
PubTator Score 70.97

Knowledge Summary

Patent (3,259)

Expression

MLP Assay (9)

AID Type Active / Inconclusive / Inactive Description
434989 screening 1389 / 0 / 324747 Fluorescence-based cell-based primary high throughput screening assay to identify antagonists of the orexin 1 receptor (OX1R; HCRTR1)
435008 summary 0 / 0 / 0 Summary of the probe development effort to identify antagonists of the orexin 1 receptor (OX1R; HCRTR1)
485270 screening 5750 / 0 / 320386 FRET-based cell-based primary high throughput screening assay to identify antagonists of the orexin 1 receptor (OX1R; HCRTR1)
492963 screening 421 / 0 / 674 Fluorescence-based cell-based high throughput confirmation assay for antagonists of the orexin 1 receptor (OX1R; HCRTR1)
492964 screening 883 / 0 / 924 Homogeneous Time Resolved Fluorescence (HTRF)-based cell-based high throughput confirmation assay for antagonists of the orexin 1 receptor (OX1R; HCRTR1)
504699 confirmatory 161 / 0 / 86 Fluorescence-based cell-based high throughput dose response assay for antagonists of the orexin 1 receptor (OX1R; HCRTR1)
504701 confirmatory 228 / 0 / 19 Homogeneous Time Resolved Fluorescence (HTRF)-based cell-based high throughput dose response assay for antagonists of the orexin 1 receptor (OX1R; HCRTR1)
624409 confirmatory 10 / 0 / 18 Late stage assay for the probe development effort for antagonists of the orexin 1 receptor (OX1R; HCRTR1): Fluorescence-based cell-based dose response assay for antagonists of the orexin 1 receptor (OX1R; HCRTR1)
624410 confirmatory 25 / 0 / 3 Late stage assay for the probe development effort 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 1 receptor (OX1R; HCRTR1)

Gene RIF (52)

PMID Text
26950369 This 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.
26555080 Rapid-onset obesity with hypothalamic dysfunction, hypoventilation, and autonomic dysregulation is highly unlikely to be caused by mutations in the exons of the HCRTR1 gene.
26459696 the orexinA/OX1 receptor axis has a significant pro-survival function in adrenal cells.
25957175 Results from homology and docking modeling show two alternative binding modes for orexin-A into orexin 1 receptor in concordance with what is known of G protein coupled receptors activation in general and the mutational data.
25866368 OX1R and KOR heterodimerize, and this heterodimer associates with Galphas, leading to increased protein kinase A (PKA) signaling pathway activity, including upregulation of intracellular cAMP levels.
25857454 OX1R signaling can attenuate KOR-mediated reduction of cellular cAMP levels while enhancing KOR-mediated beta-arrestin recruitment and p38 activation.
25677777 Data suggest that interaction between the nociceptin/nociceptin receptor system and the orexin/orexin receptor system in neurons of the hypothalamus positively and negatively modulate complex and integrated responses to stress. [REVIEW]
25515760 Orexin A upregulates the protein expression of OX1R and enhances the proliferation of SGC-7901 gastric cancer cells through the ERK signaling pathway.
25212464 Decrease in Ox expression with normal human maturation and aging. This may contribute to changes in sleep regulation during development and with aging.
25132134 Orexin receptor binding was strongly dependent on the extracellular Ca(2+) concentration.
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AA Sequence

MEPSATPGAQMGVPPGSREPSPVPPDYEDEFLRYLWRDYLYPKQYEWVLIAAYVAVFVVALVGNTLVCLA      1 - 70
VWRNHHMRTVTNYFIVNLSLADVLVTAICLPASLLVDITESWLFGHALCKVIPYLQAVSVSVAVLTLSFI     71 - 140
ALDRWYAICHPLLFKSTARRARGSILGIWAVSLAIMVPQAAVMECSSVLPELANRTRLFSVCDERWADDL    141 - 210
YPKIYHSCFFIVTYLAPLGLMAMAYFQIFRKLWGRQIPGTTSALVRNWKRPSDQLGDLEQGLSGEPQPRA    211 - 280
RAFLAEVKQMRARRKTAKMLMVVLLVFALCYLPISVLNVLKRVFGMFRQASDREAVYACFTFSHWLVYAN    281 - 350
SAANPIIYNFLSGKFREQFKAAFSCCLPGLGPCGSLKAPSPRSSASHKSLSLQSRCSISKISEHVVLTSV    351 - 420
TTVLP                                                                     421 - 425
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Text Mined References (64)

PMID Year Title
26950369 2016 Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors.
26555080 2016 Absence of mutations in HCRT, HCRTR1 and HCRTR2 in patients with ROHHAD.
26459696 2015 Orexin-A regulates cell apoptosis in human H295R adrenocortical cells via orexin receptor type 1 through the AKT signaling pathway.
25957175 2015 Modeling of the OX1R-orexin-A complex suggests two alternative binding modes.
25866368 2015 Heterodimerization of human orexin receptor 1 and kappa opioid receptor promotes protein kinase A/cAMP-response element binding protein signaling via a G?s-mediated mechanism.
25857454 2015 The orexin 1 receptor modulates kappa opioid receptor function via a JNK-dependent mechanism.
25677777 2015 The neuronal circuit between nociceptin/orphanin FQ and hypocretins/orexins coordinately modulates stress-induced analgesia and anxiety-related behavior.
25515760 2015 Orexin A upregulates the protein expression of OX1R and enhances the proliferation of SGC-7901 gastric cancer cells through the ERK signaling pathway.
25212464 2015 Changes in orexin (hypocretin) neuronal expression with normal aging in the human hypothalamus.
25132134 2014 Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery.
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