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Tbio
SETDB1
Histone-lysine N-methyltransferase SETDB1

Protein Summary
Description
Histone methyltransferase that specifically trimethylates 'Lys-9' of histone H3. 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. Probably 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. SETDB1 is targeted to histone H3 by TRIM28/TIF1B, a factor recruited by KRAB zinc-finger proteins. Probably forms a corepressor complex required for activated KRAS-mediated promoter hypermethylation and transcriptional silencing of tumor suppressor genes (TSGs) or other tumor-related genes in colorectal cancer (CRC) cel ...more
Uniprot Accession IDs
Gene Name
Ensembl ID
  • ENST00000271640
  • ENSP00000271640
  • ENSG00000143379
  • ENST00000368962
  • ENSP00000357958
  • ENST00000368969
  • ENSP00000357965

Symbol
  • KIAA0067
  • KMT1E
  • ESET
  • KG1T
  • KMT1E
  • TDRD21
  • H3-K9-HMTase4
Illumination Graph
Knowledge Table
Most Knowledge About
Knowledge Value (0 to 1 scale)
protein domain
0.97
ligand (protein) perturbation
0.96
histone modification site profile
0.87
hub protein
0.85
molecular function
0.79


Protein Classes
No PANTHER Classes or DTO Classes found
IDG Development Level Summary
Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 214.57   (req: < 5)
Gene RIFs: 49   (req: <= 3)
Antibodies: 356   (req: <= 50)
Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 214.57   (req: >= 5)
Gene RIFs: 49   (req: > 3)
Antibodies: 356   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 9
Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligand: 0
Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0