Preferred Label : EZH2 Inhibitor SHR2554;
NCIt synonyms : Enhancer of Zeste Homolog 2 Inhibitor SHR2554;
NCIt definition : An orally available selective inhibitor of the histone lysine methyltransferase (HMT)
enhancer of zeste homolog 2 (EZH2), with potential antineoplastic activity. Upon oral
administration, EZH2 inhibitor SHR2554 selectively targets, binds to and inhibits
the activity of EZH2. Inhibition of EZH2 specifically prevents the methylation of
histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene
expression patterns associated with cancer pathways and results in decreased proliferation
of EZH2-expressing cancer cells. EZH2, an HMT class enzyme and the catalytic subunit
of the polycomb repressive complex 2 (PRC2), is overexpressed or mutated in a variety
of cancer cells and plays a key role in tumor cell proliferation; its expression is
correlated with tumor initiation, progression, stem cell self-renewal, migration and
angiogenesis.;
Molecule name : SHR 2554; SHR-2554;
NCI Metathesaurus CUI : CL950708;
Origin ID : C158742;
UMLS CUI : C5203926;
Semantic type(s)
- concept_is_in_subset
- has_target
