Preferred Label : Lirametostat;
NCIt synonyms : EZH2 Inhibitor CPI-1205;
NCIt definition : An orally available selective inhibitor of the histone lysine methyltransferase EZH2,
with potential antineoplastic activity. Upon oral administration, lirametostat selectively
inhibits the activity of both wild-type and mutated forms 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, a histone
lysine methyltransferase (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.;
UNII : 455J2479FY;
InChIKey : HPODOLXTMDHLLC-QGZVFWFLSA-N;
CAS number : 1621862-70-1;
Molecule name : CPI-1205;
Origin ID : C121639;
UMLS CUI : C5446292;
Semantic type(s)
- concept_is_in_subset
- has_target
