NCIt definition : An orally available, reversible, noncompetitive inhibitor of lysine-specific demethylase
1 (LSD1, or KDM1A), with potential antineoplastic activity. Upon oral administration,
seclidemstat reversibly inhibits LSD1, a demethylase that suppresses the expression
of target genes by converting the di- and mono-methylated forms of lysine at position
4 of histone 3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition
enhances H3K4 methylation and increases the expression of tumor suppressor genes.
This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells.
In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression
of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases
transcription of these genes.;
Semantic type(s)