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SETDB1 (Histone-lysine N-methyltransferase SETDB1) is a protein that switches other genes on and off. 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 Breast cancer, Colorectal cancer, Hepatocellular carcinoma and 5 more.
Histone methyltransferase that specifically trimethylates 'Lys-9' of histone H3 (H3K9me3). H3 'Lys-9' trimethylation represents a specific tag for epigenetic transcriptional repression by recruiting HP1 (CBX1, CBX3 and/or CBX5) proteins to methylated histones. Mainly functions in euchromatin regions, thereby playing a central role in the silencing of euchromatic genes.
IntOGen calls it a driver in 8 cohorts (5 activating, 3 loss-of-function), covering Invasive Breast Carcinoma, Chronic Lymphocytic Leukaemia/Small Lymphocytic Lymphoma, Colon Adenocarcinoma, Hepatocellular Carcinoma, Head and Neck Squamous Cell Carcinoma, Pancreatic Adenocarcinoma and others.
In plain words · SETDB1 (Histone-lysine N-methyltransferase SETDB1) is a protein that switches other genes on and off. 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 Breast cancer, Colorectal cancer, Hepatocellular carcinoma and 5 more.
SETDB1 (Histone-lysine N-methyltransferase SETDB1) is a protein that switches other genes on and off. 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 Breast cancer, Colorectal cancer, Hepatocellular carcinoma and 5 more.
Histone methyltransferase that specifically trimethylates 'Lys-9' of histone H3 (H3K9me3).
No product in this corpus aims at SETDB1 yet. Transcription factors have no pocket to plug, so drugs either degrade them or block the partner protein they need to dock on DNA.
First described 1994. Earliest sequence paper UniProt cites for the protein: Nomura et al, DNA Res, 1994, "Prediction of the coding sequences of unidentified human genes. II. The coding sequences of 40 new genes (KIAA0041-KIAA0080) deduced by analysis of cDNA clones from human cell line KG-1". Source.
Sources: HGNC HGNC:10761 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q15047 (protein name, function text, keywords and locations (REST API)); IntOGen SETDB1 (driver in 8 cohorts (Act 5, LoF 3); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Histone methyltransferase that specifically trimethylates 'Lys-9' of histone H3 (H3K9me3). H3 'Lys-9' trimethylation represents a specific tag for epigenetic transcriptional repression by recruiting HP1 (CBX1, CBX3 and/or CBX5) proteins to methylated histones. Mainly functions in euchromatin regions, thereby playing a central role in the silencing of euchromatic genes. H3 'Lys-9' trimethylation is coordinated with DNA methylation. Forms a complex with MBD1 and ATF7IP that represses transcription and couples DNA methylation and histone 'Lys-9' trimethylation. Its activity is dependent on MBD1 and is heritably maintained through DNA replication by being recruited by CAF-1. Location: Nucleus; Cytoplasm; Chromosome (UniProt). Locus 1q21.3 (HGNC).
Query for this target: (TITLE:"SETDB1" OR ABSTRACT:"SETDB1" OR TITLE:"SET domain bifurcated histone lysine methyltransferase 1" OR ABSTRACT:"SET domain bifurcated histone lysine methyltransferase 1" OR TITLE:"Histone-lysine N-methyltransferase SETDB1" OR ABSTRACT:"Histone-lysine N-methyltransferase SETDB1" OR TITLE:"KG1T" OR ABSTRACT:"KG1T" OR TITLE:"KIAA0067" OR ABSTRACT:"KIAA0067" OR TITLE:"KMT1E" OR ABSTRACT:"KMT1E") 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 SETDB1, not a curated reading list.
Shares Mesothelioma, Hepatocellular carcinoma, IntOGen, Breast cancer (all types).
Shares Mesothelioma, IntOGen, Head and neck squamous cell carcinoma, Breast cancer (all types).
Shares Mesothelioma, Hepatocellular carcinoma, IntOGen, Breast cancer (all types).
Shares Mesothelioma, IntOGen, Colorectal cancer.
Shares Mesothelioma, Hepatocellular carcinoma, IntOGen, Breast cancer (all types).
Shares Mesothelioma, IntOGen, Head and neck squamous cell carcinoma, Breast cancer (all types).
Shares Mesothelioma, IntOGen, Breast cancer (all types), Colorectal cancer.
Shares Mesothelioma, Hepatocellular carcinoma, IntOGen.