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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