MAPK1
MAPK1 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
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signalling cascade initiated by activated KIT and KITLG/SCF.
CIViC holds 5 clinical evidence items and 1 assertion across 3 variants, naming Erlotinib and WZ4002. Open Targets scores its association with cancer at 0.82 (direct and indirect evidence; datatypes clinical 0.19, affected pathway 0.86, literature 0.99, genetic association 0.08, somatic mutation 0.95). IntOGen calls it a driver in 5 cohorts (4 activating, 1 loss-of-function), covering Cervical Squamous Cell Carcinoma, Chronic Lymphocytic Leukaemia/Small Lymphocytic Lymphoma, Hepatocellular Carcinoma, Head and Neck Squamous Cell Carcinoma.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · MAPK1 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
MAPK1 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
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade.
- 3 · How drugs use it
No product in this corpus aims at MAPK1 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:6871 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P28482 (protein name, function text, keywords and locations (REST API)); CIViC gene MAPK1 (5 evidence items, 1 assertions, 3 variants; diseases: Head And Neck Squamous Cell Carcinoma, Lung Non-small Cell Carcinoma, Cancer (GraphQL API, CC0)); Open Targets ENSG00000100030 (association with cancer (MONDO_0004992) 0.82; per-cancer scores at or above 0.5: cervical cancer 0.52, skin cancer 0.52, breast cancer 0.54, lung cancer 0.51 (GraphQL API, CC0)); IntOGen MAPK1 (driver in 5 cohorts (Act 4, LoF 1); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Biology
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signalling cascade initiated by activated KIT and KITLG/SCF. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell growth, adhesion, survival and differentiation through the regulation of transcription, translation, cytoskeletal rearrangements. The MAPK/ERK cascade also plays a role in initiation and regulation of meiosis, mitosis, and postmitotic functions in differentiated cells by phosphorylating a number of transcription factors. About 160 substrates have already been discovered for ERKs. Location: Cytoplasm, cytoskeleton, spindle; Nucleus; Cytoplasm, cytoskeleton, microtubule organizing center, centrosome; Cytoplasm (UniProt). Locus 22q11.22 (HGNC).
- Head and neck squamous cell carcinoma: CIViC evidence names this disease; IntOGen driver in 1 cohort (HNSC)
- Cervical cancer: Open Targets association 0.52 with cervical cancer (MONDO_0002974); IntOGen driver in 2 cohorts (CESC)
- Hepatocellular carcinoma: IntOGen driver in 1 cohort (HCC)
- Breast cancer: Open Targets association 0.54 with breast cancer (MONDO_0007254)
- Skin cancer: Open Targets association 0.52 with skin cancer (MONDO_0002898)
- Lung cancer: Open Targets association 0.51 with lung cancer (MONDO_0008903)
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 0.19; IntOGen calls it an activating (Act) driver in 4 cohorts; IntOGen calls it a loss-of-function (LoF) driver in 1 cohort; CIViC holds 5 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:"MAPK1" OR ABSTRACT:"MAPK1" OR TITLE:"mitogen-activated protein kinase 1" OR ABSTRACT:"mitogen-activated protein kinase 1" OR TITLE:"Mitogen-activated protein kinase 1" OR ABSTRACT:"Mitogen-activated protein kinase 1" OR TITLE:"ERK2" OR ABSTRACT:"ERK2" OR TITLE:"p41mapk" OR ABSTRACT:"p41mapk" OR TITLE:"MAPK2" OR ABSTRACT:"MAPK2") 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 MAPK1, not a curated reading list.
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