Property Summary

NCBI Gene PubMed Count 155
Grant Count 443
R01 Count 247
Funding $51,744,469.63
PubMed Score 1193.28
PubTator Score 925.00

Knowledge Summary

Patent (48,655)

Expression

  Differential Expression (8)

Disease log2 FC p
osteosarcoma -1.870 0.000
atypical teratoid / rhabdoid tumor 1.200 0.003
glioblastoma 1.100 0.002
medulloblastoma, large-cell 1.400 0.000
Breast cancer -3.100 0.029
group 4 medulloblastoma -1.100 0.009
ductal carcinoma in situ -1.500 0.001
invasive ductal carcinoma -1.900 0.002

Synonym

Accession P25103 A8K150 SPR
Symbols SPR
NK1R
NKIR
TAC1R

Gene

PANTHER Protein Class (2)

PDB

2KS9   2KSA   2KSB  

  TechDev Info (1)

MLP Assay (12)

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
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)
743250 screening 1 / 0 / 0 Discovery and characterization of a small molecule allosteric agonists of mas-related G-Protein coupled receptor X1 ( MrgX1)
743251 screening 1 / 0 / 0 Development of a novel orthosteric Muscarinic 5 (M5) antagonist possessing a hig degree of muscarinic subtype selectivity
743252 screening 1 / 0 / 0 Development of the first CNS penetrant Muscarinic 5 (M5) Positive Allosteric Modulator based on a novel non-isatin core
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Gene RIF (126)

PMID Text
26516161 These findings reveal important insight into the molecular mechanisms of the NK1R complex as a critical component in a model of pediatric liver cancer and may support the development of novel therapeutic interventions for hepatoblastoma
26371842 Neuropeptide signaling through neurokinin-1 and neurokinin-2 receptors augments antigen presentation by human dendritic cells
26012530 The single nucleotide polymorphisms in the TACR1 gene are associated with sex differences in postoperative nausea and vomiting.
25841180 Results show the existence of a relevant alteration in NK-1R expression in bipolar disorder patients and further suggest Substance P involvement in BD.
25817575 NK-1 activation could enhance EGFR expression and phosphorylation, and then activate EGFR related Erk/MAPK and Akt pathway.
25786041 Findings indicate a role of the TACR1 gene in the development of sicca syndrome in subjects affected with fibromyalgia.
25783846 Report absence of full-length neurokinin-1 receptor protein expression by cutaneous T cells in mycosis fungoides.
25684939 Immunohistochemical NK-1R and pEGFR positivity with VDR negativity can be used to identify areas of sporadic colorectal neoplasia.
25659767 NK-1R activation by substance P stimulation promotes growth and migration of esophageal squamous cell carcinoma cells.
25204428 Inhibition of CaV2.3 channels by NK1 receptors is sensitive to membrane cholesterol but insensitive to caveolin-1.
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AA Sequence

MDNVLPVDSDLSPNISTNTSEPNQFVQPAWQIVLWAAAYTVIVVTSVVGNVVVMWIILAHKRMRTVTNYF      1 - 70
LVNLAFAEASMAAFNTVVNFTYAVHNEWYYGLFYCKFHNFFPIAAVFASIYSMTAVAFDRYMAIIHPLQP     71 - 140
RLSATATKVVICVIWVLALLLAFPQGYYSTTETMPSRVVCMIEWPEHPNKIYEKVYHICVTVLIYFLPLL    141 - 210
VIGYAYTVVGITLWASEIPGDSSDRYHEQVSAKRKVVKMMIVVVCTFAICWLPFHIFFLLPYINPDLYLK    211 - 280
KFIQQVYLAIMWLAMSSTMYNPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQGSVYK    281 - 350
VSRLETTISTVVGAHEEEPEDGPKATPSSLDLTSNCSSRSDSKTMTESFSFSSNVLS                 351 - 407
//

Text Mined References (158)

PMID Year Title
26516161 2015 Targeting the Neurokinin-1 Receptor Compromises Canonical Wnt Signaling in Hepatoblastoma.
26371842 2015 Neuropeptide signaling through neurokinin-1 and neurokinin-2 receptors augments antigen presentation by human dendritic cells.
26012530 2015 TACR1 gene polymorphism and sex differences in postoperative nausea and vomiting.
25841180 2015 Neurokinin (NK)-1 receptor expression in monocytes from bipolar disorder patients: a pilot study.
25817575 2015 Neurokinin-1 activation affects EGFR related signal transduction in triple negative breast cancer.
25786041 The rs3771863 single nucleotide polymorphism of the TACR1 gene is associated to a lower risk of sicca syndrome in fibromyalgia patients.
25783846 2015 Absence of full-length neurokinin-1 receptor protein expression by cutaneous T cells: implications for substance P-mediated signaling in mycosis fungoides.
25684939 2015 Immunohistochemical expression of SP-NK-1R-EGFR pathway and VDR in colonic inflammation and neoplasia.
25659767 2015 Elevated SP/NK-1R in esophageal carcinoma promotes esophageal carcinoma cell proliferation and migration.
25204428 2015 Inhibition of CaV2.3 channels by NK1 receptors is sensitive to membrane cholesterol but insensitive to caveolin-1.
More...