Preferred Label : LSD1 Inhibitor TAS1440;
NCIt synonyms : Lysine-specific Demethylase 1 Inhibitor TAS1440;
NCIt definition : An orally available inhibitor of lysine-specific demethylase 1 (LSD1; KDM1A), with
potential antineoplastic activity. Upon oral administration, LSD1 inhibitor TAS1440
specifically targets, 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 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. LSD1 is overexpressed in a number of tumor
cell types. LSD1 acts on histone H3 as a transcription co-repressor through demethylation
of lysine 4 (H3K4) or as a transcription co-activator through demethylation of lysine
9 (H3K9).;
Molecule name : TAS 1440; TAS-1440;
NCI Metathesaurus CUI : CL1413420;
Origin ID : C175973;
UMLS CUI : C5446898;
Semantic type(s)
- concept_is_in_subset
- has_target
