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Target intelligence / Profile preview
Histone-lysine N-methyltransferase EZH2 (EZH2)
- Target
- EZH2
- Molecular classification
- Enzyme, Histone modification, Methyltransferase, Transcription factor
01
Overview
EZH2 is a histone-lysine N-methyltransferase and the catalytic subunit of the Polycomb Repressive Complex 2 (PRC2). It methylates lysine 27 on histone H3 (H3K27me), leading to transcriptional repression. It is involved in various cancers and plays a role in stem cell identity. EZH2 activity is regulated by post-translational modifications and antagonistic epigenetic marks. It primarily localizes to the nucleus. It can also methylate non-histone proteins.
- Other names
- Enhancer of zeste homolog 2Lysine N-methyltransferase 6KMT6ENX1ENX-1
02
Mechanism of action
EZH2 inhibition disrupts PRC2 complex function, leading to altered gene expression and cell death in susceptible cancers.
03
Biological functions
Transcriptional repressionChromatin modificationCell cycle regulationDevelopmentStem cell maintenanceRegulation of circadian clock
04
Disease associations
CancerLymphoma
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