Preferred Label : Lysine-specific Demethylase 1 Inhibitor INCB059872;
NCIt synonyms : LSD1 Inhibitor INCB059872;
NCIt related terms : INCB-059872;
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.;
UNII : 12XU6D9FLM;
CAS number : 1802909-49-4; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1802909-49-4
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G-SRS /a ;
Molecule name : INCB059872;
NCI Metathesaurus CUI : CL504960;
Origin ID : C126421;
UMLS CUI : C4287752;
Semantic type(s)
- concept_is_in_subset
- has_target
