Preferred Label : EZH1/2 Inhibitor HH2853;
NCIt synonyms : EZH1 and EZH2 Inhibitor HH2853;
NCIt definition : An orally bioavailable inhibitor of the histone lysine methyltransferases enhancer
of zeste homolog 1 (EZH1) and 2 (EZH2), with potential antineoplastic activity. Upon
oral administration, EZH1/2 inhibitor HH2853 inhibits the activity of both wild-type
and mutated forms of EZH1 and EZH2. Inhibition of EZH1/2 specifically prevents the
methylation of lysine 27 on histone H3 (H3K27). This decrease in histone methylation
alters gene expression patterns associated with cancer pathways, enhances transcription
of certain target genes, and results in decreased proliferation of EZH1/2-expressing
cancer cells. EZH1/2, histone lysine methyltransferase (HMT) class enzymes and catalytic
subunits of the polycomb repressive complex 2 (PRC2), are overexpressed or mutated
in a variety of cancer cells and play key roles in tumor cell proliferation, progression,
stem cell self-renewal and migration.;
Molecule name : HH 2853; HH-2853;
NCI Metathesaurus CUI : CL1407522;
Origin ID : C173698;
UMLS CUI : C5418014;
Semantic type(s)
- concept_is_in_subset
- has_target
