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Target intelligence / Profile preview
Menin–Histone-Lysine N-Methyltransferase 2A Protein–Protein Interaction
- Molecular classification
- Protein-Protein Interaction, Transcription factor, Histone modification
01
Overview
The interaction between menin and histone-lysine N-methyltransferase 2A (KMT2A, also known as MLL1) is a critical protein-protein interaction that plays a central role in epigenetic regulation, gene transcription, and the pathogenesis of certain leukemias. KMT2A is a histone methyltransferase responsible for methylating lysine 4 on histone H3 (H3K4), which is associated with active transcription. Menin acts as a scaffolding protein that binds to KMT2A within multi-protein chromatin complexes. Disruption of this interaction has emerged as an effective therapeutic strategy for leukemias with KMT2A rearrangements or NPM1 mutations.
02
Mechanism of action
Inhibition of menin-KMT2A protein-protein interaction
03
Biological functions
Epigenetic regulationTranscriptional regulationHematopoiesisEmbryonic development
04
Disease associations
Acute myeloid leukemia (AML)Acute lymphoblastic leukemia (ALL)
05
Safety considerations
QT interval prolongation
06
Interacting drugs
Revumenib
1 more in the full profile.
07
Biomarkers
KMT2A rearrangementsNPM1 mutationsMolecular clearance of disease markers
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