Property Summary

NCBI Gene PubMed Count 66
Grant Count 36
R01 Count 24
Funding $11,741,984.72
PubMed Score 1579.66
PubTator Score 82.90

Knowledge Summary

Patent (10,472)

Expression

  Differential Expression (1)

Disease log2 FC p
psoriasis 3.300 0.000

MLP Assay (17)

AID Type Active / Inconclusive / Inactive Description
1788 other 0 / 0 / 0 Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity
1921 other 2 / 0 / 0 Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator: 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
652083 other 0 / 0 / 0 Late-stage results from the probe development effort to identify antagonists of OPRK1: CEREP radiometric-based biochemical counterscreen panel assay
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)
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Gene RIF (51)

PMID Text
26475619 High constitutive Akt2 activity in U937 promonocytes: effective reduction of Akt2 phosphorylation by the histamine H2-receptor and the beta2-adrenergic receptor
25922853 Lack of Association between rs2067474 Polymorphism in Histamine Receptor H2 Gene and Breast Cancer in Chinese Han Population
25664905 Thus, the results in the initial study were due to the degradation of histamine in skeletal muscle by ascorbate, because the histaminergic vasodilatation was unaffected by N-acetylcysteine.
25192644 Cimetidine reversed the exercise-induced improvement in learning and memory in rats. Central histamine H2 receptors play an important role in mediating the beneficial effects of forced exercise on learning and memory.
24980224 upregulated on T regs following seasonal pollen exposure; allergen immunotherapy had no impact on the expression
24530738 The inhibitory effects of histamine on reactive oxygen species production in whole blood phagocytes are caused by H2R rather than H4R histamine receptors.
24236486 But carriers of one or three copies of HRH1 (5% of individuals), HRH2 (1.1%) and HRH4 genes (0.9%) were also identified.
23677734 In this review, we focus on the role of histamine and its receptors in the treatment of Alzheimer's disease.
23465664 HR signaling through cyclic AMP and exchange protein directly activated by cyclic AMP was required for the histamine effect on LPS-induced monocyte-derived dendritic cells responses
23280118 rs2607474 GG homozygote confers a significantly increased risk for age- and inflammation-related DAPK and CDH1 methylation in gastric epithelium.
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AA Sequence

MAPNGTASSFCLDSTACKITITVVLAVLILITVAGNVVVCLAVGLNRRLRNLTNCFIVSLAITDLLLGLL      1 - 70
VLPFSAIYQLSCKWSFGKVFCNIYTSLDVMLCTASILNLFMISLDRYCAVMDPLRYPVLVTPVRVAISLV     71 - 140
LIWVISITLSFLSIHLGWNSRNETSKGNHTTSKCKVQVNEVYGLVDGLVTFYLPLLIMCITYYRIFKVAR    141 - 210
DQAKRINHISSWKAATIREHKATVTLAAVMGAFIICWFPYFTAFVYRGLRGDDAINEVLEAIVLWLGYAN    211 - 280
SALNPILYAALNRDFRTGYQQLFCCRLANRNSHKTSLRSNASQLSRTQSREPRQQEEKPLKLQVWSGTEV    281 - 350
TAPQGATDR                                                                 351 - 359
//

Text Mined References (69)

PMID Year Title
26475619 2016 High constitutive Akt2 activity in U937 promonocytes: effective reduction of Akt2 phosphorylation by the histamine H2-receptor and the ?2-adrenergic receptor.
25922853 2015 Lack of Association between rs2067474 Polymorphism in Histamine Receptor H2 Gene and Breast Cancer in Chinese Han Population.
25664905 2015 Effect of antioxidants on histamine receptor activation and sustained postexercise vasodilatation in humans.
25192644 2014 The role of the central histaminergic receptors in the exercise-induced improvements of the spatial learning and memory in rats.
24980224 Histamine type 2 receptor expression on peripheral blood regulatory lymphocytes in patients with allergic rhinitis treated with specific immunotherapy.
24530738 2014 Role of histamine receptors in the effects of histamine on the production of reactive oxygen species by whole blood phagocytes.
24236486 2013 Variability in histamine receptor genes HRH1, HRH2 and HRH4 in patients with hypersensitivity to NSAIDs.
23677734 2013 The neglected role of histamine in Alzheimer's disease.
23465664 2013 Histamine receptor 2 modifies dendritic cell responses to microbial ligands.
23280118 2013 Influence of HRH2 promoter polymorphism on aberrant DNA methylation of DAPK and CDH1 in the gastric epithelium.
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