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Target intelligence / Profile preview
Histone-lysine N-methyltransferase SETD2 (SETD2)
- Target
- SETD2
- Molecular classification
- Enzyme, Histone modification, Methyltransferase, Transcription factor
01
Overview
Histone lysine N-methyltransferase SETD2 is a critical epigenetic regulator responsible for trimethylating histone H3 at lysine 36. It maintains genome integrity through roles in transcription regulation, mRNA processing, and homologous recombination-based DNA repair. Loss or mutation leads to developmental defects and contributes significantly to cancer pathogenesis as a tumor suppressor gene.
- Other names
- SET domain containing 2KMT3A
02
Mechanism of action
Inhibition of histone methyltransferase activity (H3K36me3)
03
Biological functions
Transcription regulationDNA repairmRNA splicing regulationChromatin organizationEpigenetic regulationGenome stability
04
Disease associations
CancerIntellectual Developmental DisorderLuscan-Lumish Syndrome
05
Safety considerations
Potential for off-target effects due to epigenetic modificationsDevelopmental toxicityGenomic instability
06
Biomarkers
SETD2 mutations in cancerH3K36me3 levels
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