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Target intelligence / Profile preview
Mixed-lineage leukemia protein 1 (KMT2A)
- Target
- KMT2A
- Molecular classification
- Enzyme, Histone modification, Transcription factor, Lysine methyltransferase
01
Overview
KMT2A encodes a lysine methyltransferase enzyme that is a key regulator of gene expression during early development and hematopoiesis. It primarily functions by catalyzing the methylation of histone H3 at lysine 4 (H3K4), an epigenetic mark associated with transcriptional activation. Chromosomal translocations involving KMT2A are causative events in aggressive forms of acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).
- Other names
- MLLMLL1ALL-1HRX (zinc finger protein HRX)mixed-lineage leukemia 1 protein
02
Mechanism of action
Inhibition of KMT2A methyltransferase activity; disruption of KMT2A fusion protein interactions
03
Biological functions
Epigenetic regulationTranscriptional regulationChromatin modificationRegulation of HOX gene expressionStem cell maintenanceDifferentiation
04
Disease associations
CancerAcute lymphoblastic leukemia (ALL)Acute myeloid leukemia (AML)Myeloid malignancies
05
Safety considerations
Off-target effects due to widespread role in gene regulationPotential for drug resistanceDevelopmental toxicity
06
Biomarkers
KMT2A translocations/mutationsH3K4 methylation levels
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