MAP3K1
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
Component of a protein kinase signal transduction cascade. Activates the ERK and JNK kinase pathways by phosphorylation of MAP2K1 and MAP2K4.
- 3 · How drugs use it
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.
External identifiers
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)
Biology
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).
- Breast cancer: Open Targets association 0.77 with breast cancer (MONDO_0007254); IntOGen driver in 8 cohorts (BRCA)
- Ovarian cancer: Open Targets association 0.64 with ovarian cancer (MONDO_0008170)
- Endometrial cancer: Open Targets association 0.56 with endometrial cancer (MONDO_0011962); IntOGen driver in 2 cohorts (UCEC)
- Renal cell carcinoma: IntOGen driver in 2 cohorts (CCRCC)
- Colorectal cancer: IntOGen driver in 2 cohorts (COAD, COADREAD)
- Skin cancer: Open Targets association 0.58 with skin cancer (MONDO_0002898)
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: Open Targets known-drug datatype score 0.06; IntOGen calls it an activating (Act) driver in 3 cohorts; IntOGen calls it a loss-of-function (LoF) driver in 16 cohorts; CIViC holds 1 clinical evidence items on its variants. Evidence tier "clinical-evidence" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery 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.