Preferred Label : LSD1 Inhibitor SYHA1807;
NCIt synonyms : Lysine-specific Demethylase 1 Inhibitor SYHA1807;
NCIt definition : An orally available inhibitor of lysine-specific demethylase 1 (LSD1; KDM1A), with
potential antineoplastic activity. Upon oral administration, LSD1 inhibitor SYHA1807
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 : SYHA-1807; SYHA 1807;
NCI Metathesaurus CUI : CL1407574;
Origin ID : C173722;
UMLS CUI : C5418023;
Semantic type(s)
- concept_is_in_subset
- has_target
