EP300
EP300 (Histone acetyltransferase p300) is a protein that switches other genes on and off. The public catalogues list it as an oncogene driver, a tumour suppressor, a biomarker and a fusion partner, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Colorectal cancer, Bladder & urothelial cancer, Head and neck squamous cell carcinoma and 5 more.
Overview
Functions as a histone acetyltransferase and regulates transcription via chromatin remodeling. Acetylates all four core histones in nucleosomes. Histone acetylation gives an epigenetic tag for transcriptional activation.
CIViC holds 2 clinical evidence items and 0 assertions across 2 variants. Open Targets scores its association with cancer at 0.87 (direct and indirect evidence; datatypes affected pathway 0.82, literature 0.99, genetic association 0.69, somatic mutation 0.95, animal model 0.59). IntOGen calls it a driver in 30 cohorts (10 activating, 20 loss-of-function), covering Angiosarcoma, Bladder Urothelial Carcinoma, Invasive Breast Carcinoma, Cervical Squamous Cell Carcinoma, Cholangiocarcinoma, Colorectal 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 · EP300 (Histone acetyltransferase p300) is a protein that switches other genes on and off. The public catalogues list it as an oncogene driver, a tumour suppressor, a biomarker and a fusion partner, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Colorectal cancer, Bladder & urothelial cancer, Head and neck squamous cell carcinoma and 5 more.
- 1 · What it is
EP300 (Histone acetyltransferase p300) is a protein that switches other genes on and off. The public catalogues list it as an oncogene driver, a tumour suppressor, a biomarker and a fusion partner, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Colorectal cancer, Bladder & urothelial cancer, Head and neck squamous cell carcinoma and 5 more.
- 2 · What goes wrong in cancer
Functions as a histone acetyltransferase and regulates transcription via chromatin remodeling. Acetylates all four core histones in nucleosomes.
- 3 · How drugs use it
No product in this corpus aims at EP300 yet. Transcription factors have no pocket to plug, so drugs either degrade them or block the partner protein they need to dock on DNA.
External identifiers
Sources: HGNC HGNC:3373 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q09472 (protein name, function text, keywords and locations (REST API)); CIViC gene EP300 (2 evidence items, 0 assertions, 2 variants; diseases: Diffuse Large B-cell Lymphoma, Oesophagus Squamous Cell Carcinoma (GraphQL API, CC0)); Open Targets ENSG00000100393 (association with cancer (MONDO_0004992) 0.87; per-cancer scores at or above 0.5: colorectal cancer 0.74, oesophageal cancer 0.54, urinary bladder cancer 0.65, cervical cancer 0.60, melanoma 0.60, head and neck squamous cell carcinoma 0.62 (GraphQL API, CC0)); IntOGen EP300 (driver in 30 cohorts (Act 10, LoF 20); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Biology
Functions as a histone acetyltransferase and regulates transcription via chromatin remodeling. Acetylates all four core histones in nucleosomes. Histone acetylation gives an epigenetic tag for transcriptional activation. Mediates acetylation of histone H3 at 'Lys-122' (H3K122ac), a modification that localises at the surface of the histone octamer and stimulates transcription, possibly by promoting nucleosome instability. Mediates acetylation of histone H3 at 'Lys-18' and 'Lys-27' (H3K18ac and H3K27ac, respectively). Also able to acetylate histone lysine residues that are already monomethylated on the same side chain to form N6-acetyl-N6-methyllysine (Kacme), an epigenetic mark of active chromatin associated with increased transcriptional initiation. Location: Cytoplasm; Nucleus; Chromosome (UniProt). Locus 22q13.2 (HGNC).
- Colorectal cancer: Open Targets association 0.74 with colorectal cancer (MONDO_0005575); IntOGen driver in 1 cohort (COADREAD)
- Bladder & urothelial cancer: Open Targets association 0.65 with urinary bladder cancer (MONDO_0001187); IntOGen driver in 7 cohorts (BLCA, UTUC)
- Head and neck squamous cell carcinoma: Open Targets association 0.62 with head and neck squamous cell carcinoma (MONDO_0010150); IntOGen driver in 3 cohorts (HNSC)
- Non-Hodgkin lymphoma: Open Targets association 0.62 with non-Hodgkin lymphoma (MONDO_0018908); IntOGen driver in 2 cohorts (MLYM, NHL)
- Lung cancer: Open Targets association 0.62 with lung cancer (MONDO_0008903)
- Cervical cancer: Open Targets association 0.60 with cervical cancer (MONDO_0002974); IntOGen driver in 3 cohorts (CESC)
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 10 cohorts; IntOGen calls it a loss-of-function (LoF) driver in 20 cohorts; CIViC holds 2 clinical evidence items on its variants; UniProt disease notes describe a translocation or gene fusion involving the gene. 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:"EP300" OR ABSTRACT:"EP300" OR TITLE:"EP300 lysine acetyltransferase" OR ABSTRACT:"EP300 lysine acetyltransferase" OR TITLE:"Histone acetyltransferase p300" OR ABSTRACT:"Histone acetyltransferase p300" OR TITLE:"p300" OR ABSTRACT:"p300" OR TITLE:"KAT3B" OR ABSTRACT:"KAT3B") 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 EP300, not a curated reading list.
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