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Tchem
SETD2
Histone-lysine N-methyltransferase SETD2

Protein Summary
Description
Histone methyltransferase that specifically trimethylates 'Lys-36' of histone H3 (H3K36me3) using dimethylated 'Lys-36' (H3K36me2) as substrate (PubMed:16118227, PubMed:19141475, PubMed:21526191, PubMed:21792193, PubMed:23043551, PubMed:27474439). Represents the main enzyme generating H3K36me3, a specific tag for epigenetic transcriptional activation (By similarity). Plays a role in chromatin structure modulation during elongation by coordinating recruitment of the FACT complex and by interacting with hyperphosphorylated POLR2A (PubMed:23325844). Acts as a key regulator of DNA mismatch repair in G1 and early S phase by generating H3K36me3, a mark required to recruit MSH6 subunit of the MutS alpha complex: early recruitment of the MutS alpha complex to chromatin to be replicated allows a quick identification of mismatch DNA to initiate the mismatch repair reaction (PubMed:23622243). Required for DNA double-strand break repair in response to DNA damage: acts by mediating formation of H3K ...more
Uniprot Accession IDs
Gene Name
Ensembl ID
  • ENST00000409792
  • ENSP00000386759
  • ENSG00000181555

Symbol
  • HIF1
  • HYPB
  • KIAA1732
  • KMT3A
  • SET2
  • LLS
  • HYPB
  • SET2
  • HIF-1
  • HIP-1
  • KMT3A
  • HBP231
  • HSPC069
  • p231HBP
Illumination Graph
Knowledge Table
Most Knowledge About
Knowledge Value (0 to 1 scale)
hub protein
0.97
biological process
0.86
histone modification site profile
0.74
protein domain
0.73
drug perturbation
0.71


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: 731.97   (req: < 5)
Gene RIFs: 66   (req: <= 3)
Antibodies: 303   (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: 731.97   (req: >= 5)
Gene RIFs: 66   (req: > 3)
Antibodies: 303   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 34
Tchem

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

Active Ligand: 1
Tclin

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

Active Drug: 0