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Target intelligence / Profile preview
Disruptor of Telomeric Silencing 1-Like Protein (DOT1L)
- Target
- DOT1L
- Molecular classification
- Enzyme, Histone modification, Methyltransferase
01
Overview
DOT1L (Disruptor of telomeric silencing 1-like) is a histone methyltransferase that catalyzes the mono-, di-, and tri-methylation of lysine-79 on histone H3 (H3K79me1/2/3). It plays roles in transcriptional activation and repression, DNA damage response, cell cycle progression and is implicated in diseases such as mixed-lineage leukemia. Small molecule inhibitors targeting its catalytic activity are under clinical investigation.
02
Mechanism of action
Inhibition of DOT1L catalytic activity
03
Biological functions
Transcriptional regulationDNA repairCell cycleCell proliferationHeterochromatin formationSpermatogenesis
04
Disease associations
CancerHematologic cancerMixed-lineage leukemiaGliomaCardiovascular disease
05
Interacting drugs
EPZ004777
1 more in the full profile.
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