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Target intelligence / Profile preview
Enhancer of zeste homolog 2 protein (EZH2)
- Target
- EZH2
- Molecular classification
- Enzyme, Histone modification, Histone-lysine N-methyltransferase
01
Overview
Enhancer of zeste homolog 2 (EZH2) is the catalytic subunit of Polycomb Repressive Complex 2 (PRC2), an epigenetic regulator that represses gene transcription by catalyzing the trimethylation of histone H3 at lysine 27 (H3K27me3). It plays crucial roles in embryonic development, cell proliferation, and differentiation, and is implicated in various diseases, particularly cancer, where its overexpression or mutation leads to aberrant gene silencing and tumorigenesis. EZH2 is a target for drug development, with small molecule inhibitors being investigated for cancer therapy.
02
Mechanism of action
Inhibition of EZH2 enzymatic activity, leading to decreased H3K27 trimethylation and altered gene expression.
03
Biological functions
Cell proliferationApoptosisDNA repairCell lineage determinationStem cell fateEpigenetic gene silencingTranscription regulation
04
Disease associations
CancerWeaver syndromeObesity/adipogenesisSkin diseasesImmune disorders
05
Interacting drugs
EZH2 inhibitors (multiple small molecule inhibitors)
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