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Target intelligence / Profile preview
Mutant Histone H3 Protein Containing Lysine-to-Methionine Substitution at Position 27 (H3K27M)
- Target
- H3K27M
- Molecular classification
- Histone modification, Histone protein, Epigenetic regulator
01
Overview
The mutant histone H3 protein containing a lysine-to-methionine substitution at position 27 ("H3K27M") acts dominantly to inhibit PRC2-mediated trimethylation across chromatin. This results in widespread epigenetic deregulation implicated primarily in aggressive pediatric brain cancers such as diffuse midline gliomas. Its unique mechanism—competitive inhibition via direct interaction with EZH2—makes it both clinically significant and valuable for research into chromatin biology.
- Other names
- H3.3 K27MH3K27M mutantLys27Met H3Histone H3 K27M
02
Mechanism of action
Dominant-negative inhibition of PRC2; competitive inhibition of EZH2
03
Biological functions
Chromatin remodelingGene repressionEpigenetic regulationRegulation of transcription
04
Disease associations
CancerDiffuse midline glioma (DMG)Diffuse intrinsic pontine glioma (DIPG)Pediatric brain tumors
05
Safety considerations
Global epigenetic dysregulationPotential for off-target effects in epigenetic therapiesComplexity of chromatin interactions
06
Biomarkers
H3K27me3 levelsH3K27M expression
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