Tchem EZH1 Histone-lysine N-methyltransferase EZH1

Protein Summary

Description

Polycomb group (PcG) protein. Catalytic subunit of the PRC2/EED-EZH1 complex, which methylates 'Lys-27' of histone H3, leading to transcriptional repression of the affected target gene. Able to mono-, di- and trimethylate 'Lys-27' of histone H3 to form H3K27me1, H3K27me2 and H3K27me3, respectively. Required for embryonic stem cell derivation and self-renewal, suggesting that it is involved in safeguarding embryonic stem cell identity. Compared to EZH2-containing complexes, it is less abundant in embryonic stem cells, has weak methyltransferase activity and plays a less critical role in forming H3K27me3, which is required for embryonic stem cell identity and proper differentiation. EZH1 is a component of a noncanonical Polycomb repressive complex-2 (PRC2) that mediates methylation of histone H3 (see MIM 602812) lys27 (H3K27) and functions in the maintenance of embryonic stem cell pluripotency and plasticity (Shen et al., 2008 [PubMed 19026780]).[supplied by OMIM, Mar 2009]

Uniprot Accession IDs

• Q92800
• A6NCH6
• B4DIJ1
• B4DIZ7
• B4DSS2
• B4E3R7
• O43287
• Q14459
• Q53XP3

Gene Name

• EZH1

Ensembl ID

• ENST00000428826
• ENSP00000404658
• ENSG00000108799
• ENST00000585893
• ENSP00000467871
• ENST00000590078
• ENSP00000465220
• ENST00000592743
• ENSP00000466924

Symbol

• KIAA0388
• KMT6B

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
disease perturbation	0.99
kinase perturbation	0.97
transcription factor binding site profile	0.84
cell type or tissue	0.78
microRNA	0.75

Protein Classes

DTO Classes

Protein / Epigenetic Regulator / Writer / Protein Methyltransferase / Histone-lysine N-methyltransferase Ezh1

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: 48.38   (req: < 5)

Gene RIFs: 22   (req: <= 3)

Antibodies: 378   (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: 48.38   (req: >= 5)

Gene RIFs: 22   (req: > 3)

Antibodies: 378   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 7

Tchem

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

Active Ligands: 21

Tclin

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

Active Drug: 1