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GRIN2A (Glutamate receptor ionotropic, NMDA 2A) is a gene that drives cell growth when it is altered. The public catalogues list it as a drug target, an oncogene driver and a fusion partner, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Colorectal cancer, Lung cancer, Skin cancer and 5 more.
Component of N-methyl-D-aspartate (NMDA) receptors (NMDARs) that function as heterotetrameric, ligand-gated cation channels with high calcium permeability and voltage-dependent block by Mg(2+). NMDARs participate in synaptic plasticity for learning and memory formation by contributing to the slow phase of excitatory postsynaptic current, long-term synaptic potentiation, and learning. Channel activation requires binding of the neurotransmitter L-glutamate to the GluN2 subunit, glycine or D-serine binding to the GluN1 subunit, plus membrane depolarisation to eliminate channel inhibition by Mg(2+).
Open Targets scores its association with cancer at 0.75 (direct and indirect evidence; datatypes clinical 0.59, literature 0.41, genetic association 0.49, somatic mutation 0.87, animal model 0.32). IntOGen calls it a driver in 6 cohorts (4 activating, 0 loss-of-function), covering Bladder Urothelial Carcinoma, Cholangiocarcinoma, Colorectal Adenocarcinoma, Malignant Tumour, Pancreas.
In plain words · GRIN2A (Glutamate receptor ionotropic, NMDA 2A) is a gene that drives cell growth when it is altered. The public catalogues list it as a drug target, an oncogene driver and a fusion partner, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Colorectal cancer, Lung cancer, Skin cancer and 5 more.
GRIN2A (Glutamate receptor ionotropic, NMDA 2A) is a gene that drives cell growth when it is altered. The public catalogues list it as a drug target, an oncogene driver and a fusion partner, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Colorectal cancer, Lung cancer, Skin cancer and 5 more.
Component of N-methyl-D-aspartate (NMDA) receptors (NMDARs) that function as heterotetrameric, ligand-gated cation channels with high calcium permeability and voltage-dependent block by Mg(2+).
No product in this corpus aims at GRIN2A yet. Drugs fit a pocket that exists only in one shape of the mutant protein and hold it there, off.
Tumour-specific alteration: the catalogues call it an oncogene driver (IntOGen cohort analysis finds it activated more often than chance) and a fusion partner (UniProt records a translocation); what a medicine would aim at or exploit is the altered form or its loss, absent from normal cells; no corpus medicine is aimed at it yet. HPA GRIN2A: RNA tissue enriched (brain 15 nTPM); high antibody staining in 1 normal tissue. Distribution: 8 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Colorectal cancer, Lung cancer (all types), Skin cancer (all types), Bladder & urothelial cancer, Pancreatic ductal adenocarcinoma, Breast cancer (all types), Prostate cancer and more); Open Targets associates it with 0 specific cancer types at or above 0.5. (Rule 6 of scripts/fetch-target-specificity.ts.)
Sources: UniProt Q12879; IntOGen GRIN2A; Human Protein Atlas GRIN2A tissue; Open Targets ENSG00000183454 associations
First described 1994. Earliest sequence paper UniProt cites for the protein: Foldes R.L. et al, Biochim. Biophys. Acta, 1994, "Human N-methyl-D-aspartate receptor modulatory subunit hNR2A: cloning and sequencing of the cDNA and primary structure of the protein". Source.
Sources: HGNC HGNC:4585 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q12879 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000183454 (association with cancer (MONDO_0004992) 0.75; per-cancer scores at or above 0.5: prostate cancer 0.51, melanoma 0.59, skin cancer 0.57, breast cancer 0.57, lung cancer 0.58, biliary tract cancer 0.50 (GraphQL API, CC0)); IntOGen GRIN2A (driver in 6 cohorts (Act 4, LoF 0); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Component of N-methyl-D-aspartate (NMDA) receptors (NMDARs) that function as heterotetrameric, ligand-gated cation channels with high calcium permeability and voltage-dependent block by Mg(2+). NMDARs participate in synaptic plasticity for learning and memory formation by contributing to the slow phase of excitatory postsynaptic current, long-term synaptic potentiation, and learning. Channel activation requires binding of the neurotransmitter L-glutamate to the GluN2 subunit, glycine or D-serine binding to the GluN1 subunit, plus membrane depolarisation to eliminate channel inhibition by Mg(2+). NMDARs mediate simultaneously the potassium efflux and the influx of calcium and sodium. Each GluN2 subunit confers differential attributes to channel properties, including activation, deactivation and desensitisation kinetics, pH sensitivity, Ca2(+) permeability, and binding to allosteric modulators. Participates in the synaptic plasticity regulation through activation by the L-glutamate releaseed by BEST1, into the synaptic cleft, upon F2R/PAR-1 activation in astrocyte. Location: Cell projection, dendritic spine; Cell membrane; Synapse; Postsynaptic cell membrane (UniProt). Locus 16p13.2 (HGNC).
RNA: tissue enriched (brain 15 nTPM), detected in some normal tissues.
Medium: Caudate, Cerebral cortex.
RNA cancer enhanced: Kidney Renal Clear Cell Carcinoma 2 pTPM, Ovary Serous Cystadenocarcinoma 2 pTPM.
No cancer stained high; medium in cervical cancer, pancreatic cancer, stomach cancer.
HPA GRIN2A tissue · HPA GRIN2A pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
Query for this target: (TITLE:"GRIN2A" OR ABSTRACT:"GRIN2A" OR TITLE:"glutamate ionotropic receptor NMDA type subunit 2A" OR ABSTRACT:"glutamate ionotropic receptor NMDA type subunit 2A" OR TITLE:"Glutamate receptor ionotropic, NMDA 2A" OR ABSTRACT:"Glutamate receptor ionotropic, NMDA 2A" OR TITLE:"GluN2A" OR ABSTRACT:"GluN2A" OR TITLE:"NR2A" OR ABSTRACT:"NR2A" OR TITLE:"NMDAR2A" OR ABSTRACT:"NMDAR2A") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about GRIN2A, not a curated reading list.
Shares Biliary tract cancer (all types), Bladder & urothelial cancer, IntOGen, Lung cancer (all types).
Shares Biliary tract cancer (all types), Skin cancer (all types), IntOGen, Breast cancer (all types).
Shares Biliary tract cancer (all types), Skin cancer (all types), IntOGen, Breast cancer (all types).
Shares Biliary tract cancer (all types), Skin cancer (all types), IntOGen, Breast cancer (all types).
Shares Biliary tract cancer (all types), IntOGen, Lung cancer (all types), Breast cancer (all types).
Shares Biliary tract cancer (all types), Skin cancer (all types), IntOGen, Open Targets Platform.
Shares Biliary tract cancer (all types), IntOGen, Breast cancer (all types), Open Targets Platform.
Shares Biliary tract cancer (all types), Skin cancer (all types), IntOGen, Open Targets Platform.