NCIt definition : An orally available inhibitor of lysine-specific demethylase 1 (LSD1), with potential
antineoplastic activity. Upon administration, INCB059872 binds to and 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 H3 (H3K4) to mono- and
unmethylated H3K4, respectively, through amine oxidation. LSD1 inhibition enhances
H3K4 methylation and increases the expression of tumor-suppressor genes. 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. Altogether, this may lead to an inhibition of cell growth in LSD1-overexpressing
tumor cells. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent
amine oxidase family, is overexpressed in certain tumor cells and plays a key role
in the regulation of gene expression and in tumor cell growth and survival.;
Semantic type(s)