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Target intelligence / Profile preview
Lysine-specific histone demethylase 1A (LSD1)
- Target
- LSD1
- Molecular classification
- Enzyme, Histone modification, FAD-dependent amine oxidase
01
Overview
Lysine-specific histone demethylase 1A (LSD1), also known as KDM1A, is a nuclear enzyme that removes methyl groups from histone H3 at lysine 4 (H3K4me1/2). This epigenetic modification plays a crucial role in regulating gene expression and is involved in various biological processes, including development, differentiation, and DNA damage response. LSD1 is often found in complex with other proteins, such as CoREST and NuRD, which influence its activity and substrate specificity. Dysregulation of LSD1 has been implicated in various diseases, particularly cancer, making it an attractive therapeutic target. Inhibitors of LSD1 are currently under clinical investigation for the treatment of cancer and other conditions.
- Other names
- KDM1A
02
Mechanism of action
Inhibition of LSD1 enzymatic activity, leading to increased histone methylation and altered gene expression.
03
Biological functions
Epigenetic regulationTranscriptional regulationDevelopmentCell differentiationDNA damage responseAntitumor immunity regulation
04
Disease associations
CancerCardiac remodelingCardiac hypertrophyCardiac fibrosis
05
Safety considerations
Potential for off-target effects due to the broad role of LSD1 in development and cellular processes.Development of resistance mechanisms in cancer.
06
Interacting drugs
LSD1 inhibitors (in clinical trials)
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