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Target intelligence / Profile preview
Histone-lysine N-methyltransferase 2A (MLL1)
- Target
- MLL1
- Molecular classification
- Enzyme, Histone modification, Transcription factor
01
Overview
Histone-lysine N-methyltransferase 2A (KMT2A), also known as MLL1, is a histone methyltransferase that acts as a positive global regulator of gene transcription. It plays an essential role in regulating gene expression during early development and hematopoiesis. KMT2A catalyzes the transfer of methyl groups to histone H3 lysine 4 (H3K4), resulting in mono-, di-, and trimethylation marks associated with active chromatin. Chromosomal translocations involving KMT2A are implicated in various leukemias, disrupting normal epigenetic regulation and leading to oncogenic transformation.
- Other names
- ALL-1HRXMyeloid/lymphoid or mixed-lineage leukemia 1
02
Mechanism of action
Inhibition of KMT2A methyltransferase activity.
03
Biological functions
Epigenetic maintenance of transcriptional memoryTranscriptional activationHOX gene regulationHistone H3 lysine 4 methylationGene transcription regulationHematopoiesisEarly development
04
Disease associations
LeukemiaCancer
05
Safety considerations
Oncogenic transformation due to chromosomal translocations/fusion proteins
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