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Histone H3.3 Lysine 27 to Methionine Mutant (H3.3 K27M)

Target: H3.3 K27M
Molecular classification: Histone modification, Histone variant

Overview

The Histone H3.3 K27M mutation is a point mutation where lysine at position 27 is replaced with methionine. It primarily occurs in histone H3.3 (H3F3A) and less frequently in H3.1. This mutation acts as a dominant negative inhibitor of PRC2, leading to global loss of H3K27 trimethylation and widespread dysregulation of gene expression, driving oncogenesis particularly in diffuse midline gliomas (DMGs) and diffuse intrinsic pontine gliomas (DIPGs).

Other names: H3 K27MH3F3A K27MHistone H3.1 K27MK27M-mutated Histone H3

Mechanism of action

Dominant-negative inhibition of Polycomb Repressive Complex 2 (PRC2)

Biological functions

Chromatin regulationGene expression regulationEpigenetic modificationCell differentiation

Disease associations

CancerDiffuse Midline Glioma (DMG)Diffuse Intrinsic Pontine Glioma (DIPG)

Safety considerations

Targeting chromatin regulators can have broad effects on gene expression, potentially leading to off-target effects.Resistance to therapies targeting K27M or its downstream effects may develop.

Biomarkers

Diagnosis of DMG/DIPGPrognosis in DMG/DIPGResponse to therapy (potential)

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