Preferred Label : Bomedemstat Tosylate;
NCIt definition : The tosylate form of bomedemstat, an orally available, irreversible inhibitor of lysine-specific
demethylase 1 (LSD1), with potential antineoplastic activity. Upon administration,
bomedemstat 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. 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; thus, inhibition of LSD1 also 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, tumor cell growth
and survival.;
UNII : 2PYF2U9JNF;
CAS number : 1990504-72-7;
NCI Metathesaurus CUI : CL1778568;
Origin ID : C186383;
UMLS CUI : C5670495;
Semantic type(s)
concept_is_in_subset
has_free_acid_or_base_form
has_target
is_salt_form_of