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MAP3K1 is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, an oncogene driver, a tumour suppressor and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response.
Component of a protein kinase signal transduction cascade. Activates the ERK and JNK kinase pathways by phosphorylation of MAP2K1 and MAP2K4. May phosphorylate the MAPK8/JNK1 kinase.
CIViC holds 1 clinical evidence item and 0 assertions across 2 variants, naming Selumetinib. Open Targets scores its association with cancer at 0.83 (direct and indirect evidence; datatypes genetic literature 0.38, clinical 0.06, literature 0.97, genetic association 0.61, somatic mutation 0.96, animal model 0.86). IntOGen calls it a driver in 19 cohorts (3 activating, 16 loss-of-function), covering Invasive Breast Carcinoma, Renal Clear Cell Carcinoma, Cervical Adenocarcinoma, Colon Adenocarcinoma, Colorectal Adenocarcinoma, Glioblastoma Multiforme and others.
In plain words · MAP3K1 is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, an oncogene driver, a tumour suppressor and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response.
MAP3K1 is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, an oncogene driver, a tumour suppressor and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response.
Component of a protein kinase signal transduction cascade. Activates the ERK and JNK kinase pathways by phosphorylation of MAP2K1 and MAP2K4.
No product in this corpus aims at MAP3K1 yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Tumour-specific alteration: the catalogues call it an oncogene driver (IntOGen cohort analysis finds it activated more often than chance) and a tumour suppressor (IntOGen finds it knocked out more often than chance), so the direction differs between cohorts but the alteration is somatic either way; 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 MAP3K1: RNA low tissue specificity; high antibody staining in 15 normal tissues; highest cancer staining thyroid cancer (3 of 3 high). Distribution: 8 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Breast cancer (all types), Ovarian cancer, Endometrial cancer, Renal cell carcinoma, Colorectal cancer, Skin cancer (all types), Cervical cancer and more); Open Targets associates it with 3 specific cancer types at or above 0.5 (breast adenocarcinoma, breast carcinoma, ovarian cancer). (Rule 6 of scripts/fetch-target-specificity.ts.)
Sources: UniProt Q13233; CIViC gene MAP3K1; IntOGen MAP3K1; Human Protein Atlas MAP3K1 tissue; Open Targets ENSG00000095015 associations
First described 1995. Earliest sequence paper UniProt cites for the protein: Vinik B.S. et al, Mamm. Genome, 1995, "Mapping of the MEK kinase gene (Mekk) to mouse chromosome 13 and human chromosome 5". Source.
Sources: HGNC HGNC:6848 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q13233 (protein name, function text, keywords and locations (REST API)); CIViC gene MAP3K1 (1 evidence items, 0 assertions, 2 variants; diseases: Cancer (GraphQL API, CC0)); Open Targets ENSG00000095015 (association with cancer (MONDO_0004992) 0.83; per-cancer scores at or above 0.5: prostate cancer 0.55, ovarian cancer 0.64, endometrial cancer 0.56, skin cancer 0.58, breast cancer 0.77 (GraphQL API, CC0)); IntOGen MAP3K1 (driver in 19 cohorts (Act 3, LoF 16); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Component of a protein kinase signal transduction cascade. Activates the ERK and JNK kinase pathways by phosphorylation of MAP2K1 and MAP2K4. May phosphorylate the MAPK8/JNK1 kinase. Activates CHUK and IKBKB, the central protein kinases of the NF-kappa-B pathway. Locus 5q11.2 (HGNC).
RNA: low tissue specificity, detected in all normal tissues.
Medium: Appendix, Bone marrow, Breast, Caudate, Cerebellum, Cerebral cortex, Endometrium, Epididymis.
Medium only: renal cancer, skin cancer.
HPA MAP3K1 tissue · HPA MAP3K1 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:"MAP3K1" OR ABSTRACT:"MAP3K1" OR TITLE:"mitogen-activated protein kinase kinase kinase 1" OR ABSTRACT:"mitogen-activated protein kinase kinase kinase 1" OR TITLE:"Mitogen-activated protein kinase kinase kinase 1" OR ABSTRACT:"Mitogen-activated protein kinase kinase kinase 1" OR TITLE:"MAPKKK1" OR ABSTRACT:"MAPKKK1" OR TITLE:"MEKK1" OR ABSTRACT:"MEKK1") 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 MAP3K1, not a curated reading list.