Property Summary

NCBI Gene PubMed Count 47
Grant Count 23
R01 Count 18
Funding $4,034,822
PubMed Score 555.57
PubTator Score 334.43

Knowledge Summary

Patent (25,069)

Expression

  Differential Expression (11)

Disease log2 FC p
posterior fossa group B ependymoma -2.300 0.000
astrocytoma -1.200 0.000
glioblastoma -1.600 0.000
osteosarcoma 1.374 0.000
group 3 medulloblastoma -2.400 0.002
atypical teratoid/rhabdoid tumor -1.900 0.000
adult high grade glioma -1.500 0.006
pilocytic astrocytoma -2.000 0.000
ovarian cancer 1.100 0.000
pituitary cancer 1.100 0.000
psoriasis 4.000 0.000

MLP Assay (15)

AID Type Active / Inconclusive / Inactive Description
1788 other 0 / 0 / 0 Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity
434974 screening 0 / 0 / 0 Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen
504381 other 0 / 0 / 0 Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Set 2
624355 other 0 / 0 / 0 Late stage results from the probe development efforts to identify dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and nuclear factor NF-kappa-B (NF-kB): Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs
624406 other 0 / 0 / 0 Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs
686924 other 0 / 0 / 1 ML347 Eurofin Panel Assay for BMP Inhibitor (Probe Compound)
686925 other 0 / 0 / 1 ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound)
686926 other 0 / 0 / 1 ML354 Eurofin Panel Assay for PAR4 Antagonists Inhibitor (Probe Compound)
686927 other 0 / 0 / 1 ML353 Eurofin Panel Assay for mGlu5 SAM Inhibitor (Probe Compound)
743249 screening 1 / 0 / 0 Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM)
More...

Gene RIF (36)

PMID Text
26915454 Decrease in histamine H3 receptor function was linked to epileptic activity in the hippocampus and temporal neocortex of patients with pharmacoresistant mesial temporal lobe epilepsy.
25098339 Molecular modelling studies, including molecular dynamic simulations and calculation of Gibbs energy of solvation of hH3R and hH4R, were studied.
24835231 The polymorphisms of HNMT and HRH3 were irrelevant with breast cancer in the present study.
24493592 Report synthesis/functional characterization of imbutamine analogs as histamine H3 agonists.
23713487 The A280V mutation reduces the signalling efficacy of the human H3 receptor; this effect may be relevant to the pathophysiology of disorders associated with the mutation
23677734 In this review, we focus on the role of histamine and its receptors in the treatment of Alzheimer's disease.
23647606 the anatomical localization of Hreceptors suggests a complex interaction that could both enhance and inhibit dopaminergic neurotransmission; tt is conceivable that Hreceptors can moderate the development and maintenance of drug addiction.
22885137 study identified novel functional properties in terms of voltage sensitivities and deactivation rates, which differed between the histamine hH3445, hH3365, and H4 receptors
22870296 ZEL-H16 is a novel and potent nonimidazole agonist of H3R, which might serve as a pharmacological tool for future investigations or as possible therapeutic agent of H3R.
22860191 [review] The H1, H2, and H3 receptors are all involved in recovery of neurological function when extracellular histamine is gradually increasing, after cerebral ischemia.
More...

AA Sequence

MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNN      1 - 70
FFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAV     71 - 140
SYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTP    141 - 210
FLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEA    211 - 280
AVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRL    281 - 350
SRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR    351 - 420
RAFTKLLCPQKLKIQPHSSLEHCWK                                                 421 - 445
//

Text Mined References (48)

PMID Year Title
26915454 2016 Pharmacoresistant temporal lobe epilepsy modifies histamine turnover and H3 receptor function in the human hippocampus and temporal neocortex.
25098339 2014 Sodium binding to hH3R and hH 4R--a molecular modeling study.
24835231 2014 Associations of polymorphisms in histidine decarboxylase, histamine N-methyltransferase and histamine receptor H3 genes with breast cancer.
24493592 2014 Synthesis and functional characterization of imbutamine analogs as histamine H3 and H4 receptor ligands.
23713487 2013 A single-point mutation (Ala280Val) in the third intracellular loop alters the signalling properties of the human histamine H? receptor stably expressed in CHO-K1 cells.
23677734 2013 The neglected role of histamine in Alzheimer's disease.
23647606 2013 Histamine H? receptors, the complex interaction with dopamine and its implications for addiction.
23535732 2013 Identification of 23 new prostate cancer susceptibility loci using the iCOGS custom genotyping array.
22885137 2012 Voltage sensitivities and deactivation kinetics of histamine H? and H? receptors.
22870296 2012 Identification and characterization of ZEL-H16 as a novel agonist of the histamine H3 receptor.
More...