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Target intelligence / Profile preview
Lysine-specific histone demethylase 1 (LSD1)
- Target
- LSD1
- Molecular classification
- Enzyme, Histone modification, Flavin-dependent amine oxidase
01
Overview
Lysine-specific histone demethylase 1 (LSD1), also known as KDM1A, is a flavin-dependent amine oxidase that plays a central role in the regulation of gene expression through epigenetic modification. It specifically demethylates mono- and dimethylated lysines on histones, primarily histone H3 at lysine 4 (H3K4me1/2) and H3K9me1/2. LSD1 acts both as a transcriptional repressor or activator depending on its context within different protein complexes. Overexpression or dysregulation of LSD1 has been linked to various cancers, and LSD1 inhibitors are being developed as antitumor agents.
- Other names
- KDM1A
02
Mechanism of action
Inhibition of LSD1 enzymatic activity, leading to altered histone methylation patterns and gene expression.
03
Biological functions
Epigenetic regulationGene expression regulationChromatin structure regulationTranscriptional repressionTranscriptional activationCell proliferationAdipogenesisSpermatogenesisChromosome segregationOocyte growthEmbryogenesisHematopoiesisTissue-specific differentiation
04
Disease associations
Cancer
05
Safety considerations
Global deletion leads to perinatal lethality due to developmental defectsCardiac remodeling and fibrosis response after injury
06
Interacting drugs
LSD1 inhibitors
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