Target intelligence / Profile preview

Menin–MLL binding interaction

Molecular classification
Protein–protein interaction, Epigenetic regulator complex, Other (scaffold protein and histone methyltransferase complex)
01

Overview

The **menin–MLL binding interaction** refers to the direct physical association between menin, a scaffold protein encoded by the MEN1 gene, and mixed lineage leukemia proteins (most notably MLL1/KMT2A), which are histone methyltransferases. This protein-protein interface is critical for regulating epigenetic modifications and controlling gene expression programs involved in cell fate determination. Disruption of this interaction—such as by small-molecule inhibitors—has emerged as a promising therapeutic strategy in cancers driven by aberrant activity of the menin–MLL axis, particularly acute leukemias with chromosomal translocations involving MLL genes. High-affinity small molecules have been developed that bind specifically to menin at its MLL-binding site and block this pathogenic partnership.

Other names
Menin–mixed lineage leukemia protein interactionMenin–MLL1 interactionMEN1–MLL binding interface
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Mechanism of action

Inhibition of the menin–MLL protein–protein interaction to disrupt oncogenic gene expression programs

03

Biological functions

Regulation of gene expressionEpigenetic modificationCell proliferationHematopoietic differentiation
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Disease associations

Cancer (especially acute leukemias with MLL rearrangements)
05

Safety considerations

no specific safety concerns or therapeutic challenges are detailed in the provided source; further research may be needed for clinical data
06

Interacting drugs

MIV series inhibitors (e.g., MIV‑3, MIV‑6, MIV‑7)

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