NCIt definition : An orally available inhibitor of lysine specific demethylase 1 (LSD1), with potential
antineoplastic activity. Upon administration, pulrodemstat 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. LSD1 inhibition enhances H3K4 methylation and increases
the expression of tumor (remove hyphen) 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. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent
amine oxidase family that is overexpressed in certain tumor cells, plays a key role
in tumor cell growth and survival.;