Tchem EHMT1 Histone-lysine N-methyltransferase EHMT1

Protein Summary

Description

Histone methyltransferase that specifically mono- and dimethylates 'Lys-9' of histone H3 (H3K9me1 and H3K9me2, respectively) in euchromatin. H3K9me represents a specific tag for epigenetic transcriptional repression by recruiting HP1 proteins to methylated histones. Also weakly methylates 'Lys-27' of histone H3 (H3K27me). Also required for DNA methylation, the histone methyltransferase activity is not required for DNA methylation, suggesting that these 2 activities function independently. Probably targeted to histone H3 by different DNA-binding proteins like E2F6, MGA, MAX and/or DP1. During G0 phase, it probably contributes to silencing of MYC- and E2F-responsive genes, suggesting a role in G0/G1 transition in cell cycle. In addition to the histone methyltransferase activity, also methylates non-histone proteins: mediates dimethylation of 'Lys-373' of p53/TP53. The protein encoded by this gene is a histone methyltransferase that methylates the lysine-9 position of histone H3. This action marks the genomic region packaged with these methylated histones for transcriptional repression. This protein may be involved in the silencing of MYC- and E2F-responsive genes and therefore could play a role in the G0/G1 cell cycle transition. Defects in this gene are a cause of chromosome 9q subtelomeric deletion syndrome (9q-syndrome, also known as Kleefstra syndrome). Alternative splicing results in multiple transcript variants. [provided by RefSeq, Aug 2017]

Uniprot Accession IDs

• Q9H9B1
• B1AQ58
• B1AQ59
• Q86X08
• Q8TCN7
• Q96F53
• Q96JF1
• Q96KH4

Gene Name

• EHMT1

Ensembl ID

• ENST00000371394
• ENSP00000485945
• ENSG00000181090
• ENST00000460843
• ENSP00000417980
• ENST00000462484
• ENSP00000417328

Symbol

• EUHMTASE1
• GLP
• KIAA1876
• KMT1D
• GLP
• GLP1
• KMT1D
• KLEFS1
• FP13812
• EHMT1-IT1
• EUHMTASE1
• Eu-HMTase1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
transcription factor binding site profile	0.82
molecular function	0.81
protein domain	0.73
histone modification site profile	0.72
biological process	0.68

Protein Classes

DTO Classes

Protein / Epigenetic Regulator / Writer / Protein Methyltransferase / Histone-lysine N-methyltransferase Ehmt1

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: 152.25   (req: < 5)

Gene RIFs: 56   (req: <= 3)

Antibodies: 483   (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: 152.25   (req: >= 5)

Gene RIFs: 56   (req: > 3)

Antibodies: 483   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 19

Tchem

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

Active Ligands: 106

Tclin

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

Active Drug: 0