ACVR2A
ACVR2A (Activin receptor type-2A) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as an oncogene driver and a tumour suppressor, and it is called a cancer driver by mutation analysis of patient cohorts. Tied to Colorectal cancer, Hepatocellular carcinoma, Pancreatic ductal adenocarcinoma and 4 more.
Overview
On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Receptor for activin A, activin B and inhibin A.
Open Targets scores its association with cancer at 0.76 (direct and indirect evidence; datatypes literature 0.92, animal model 0.27, genetic association 0.41, somatic mutation 0.94). IntOGen calls it a driver in 13 cohorts (1 activating, 12 loss-of-function), covering Colorectal Adenocarcinoma, Cutaneous Squamous Cell Carcinoma, Hepatocellular Carcinoma, Pancreatic Adenocarcinoma, Prostate Adenocarcinoma, Stomach Adenocarcinoma 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 · ACVR2A (Activin receptor type-2A) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as an oncogene driver and a tumour suppressor, and it is called a cancer driver by mutation analysis of patient cohorts. Tied to Colorectal cancer, Hepatocellular carcinoma, Pancreatic ductal adenocarcinoma and 4 more.
- 1 · What it is
ACVR2A (Activin receptor type-2A) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as an oncogene driver and a tumour suppressor, and it is called a cancer driver by mutation analysis of patient cohorts. Tied to Colorectal cancer, Hepatocellular carcinoma, Pancreatic ductal adenocarcinoma and 4 more.
- 2 · What goes wrong in cancer
On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases.
- 3 · How drugs use it
No product in this corpus aims at ACVR2A 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:173 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P27037 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000121989 (association with cancer (MONDO_0004992) 0.76; per-cancer scores at or above 0.5: colorectal cancer 0.64, gastric cancer 0.56 (GraphQL API, CC0)); IntOGen ACVR2A (driver in 13 cohorts (Act 1, LoF 12); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Biology
On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Receptor for activin A, activin B and inhibin A. Mediates induction of adipogenesis by GDF6. Location: Cell membrane (UniProt). Locus 2q22.3-q23.1 (HGNC).
- Colorectal cancer: Open Targets association 0.64 with colorectal cancer (MONDO_0005575); IntOGen driver in 3 cohorts (COADREAD)
- Hepatocellular carcinoma: IntOGen driver in 3 cohorts (HCC)
- Pancreatic ductal adenocarcinoma: IntOGen driver in 3 cohorts (PAAD)
- Gastric & gastro-oesophageal junction cancer: Open Targets association 0.56 with gastric cancer (MONDO_0001056); IntOGen driver in 1 cohort (STAD)
- Prostate cancer: IntOGen driver in 1 cohort (PRAD)
- Endometrial cancer: IntOGen driver in 1 cohort (UCEC)
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: IntOGen calls it an activating (Act) driver in 1 cohort; IntOGen calls it a loss-of-function (LoF) driver in 12 cohorts. Evidence tier "cohort-driver" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery for this target: (TITLE:"ACVR2A" OR ABSTRACT:"ACVR2A" OR TITLE:"activin A receptor type 2A" OR ABSTRACT:"activin A receptor type 2A" OR TITLE:"Activin receptor type-2A" OR ABSTRACT:"Activin receptor type-2A" OR TITLE:"ACTRII" OR ABSTRACT:"ACTRII" OR TITLE:"ACVR2" OR ABSTRACT:"ACVR2") 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 ACVR2A, not a curated reading list.
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