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Target intelligence / Profile preview
Disrupter of telomeric silencing 1-like protein (DOT1L)
- Target
- DOT1L
- Molecular classification
- Enzyme, Histone methyltransferase
01
Overview
DOT1L is an essential non‐SET domain histone methyltransferase responsible for H3K79 methylation on nucleosomes marked by ubiquitinated H2B. It plays central roles in transcriptional activation/repression depending on context—most notably implicated as an oncogenic cofactor when recruited by mixed lineage leukemia fusions—and represents an important drug target under active clinical investigation.
02
Mechanism of action
Inhibition of DOT1L catalytic activity, reducing H3K79 methylation
03
Biological functions
Transcription regulationCell cycle controlDNA damage responseDevelopmentSomatic reprogrammingSpermatogenesisHeterochromatin formationImmune function
04
Disease associations
CancerLeukemiaGliomaAtherosclerosis
05
Interacting drugs
EPZ004777
1 more in the full profile.
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