Preferred Label : EED Inhibitor APG-5918;
NCIt synonyms : Ectodermal Embryonic Development Inhibitor APG-5918;
NCIt definition : An orally bioavailable, small molecule, allosteric inhibitor of the polycomb repressive
complex 2 (PRC2) component embryonic ectoderm development (EED) protein, with potential
antineoplastic activity. Upon oral administration, EED inhibitor APG-5918 targets
and binds to EED. This inhibits the binding of EED with trimethylated histone H3 on
lysine 27 (H3K27me3), prevents the interaction of EED with the histone methyltransferase
(HMT) and the catalytic subunit of the PRC2 enhancer zeste homolog 2 (EZH2), and prevents
H3K27 methylation. The decrease in histone methylation alters gene expression patterns
associated with cancer pathways and results in decreased tumor cell proliferation
in EZH2-mutated and PRC2-dependent cancer cells. EZH2 is overexpressed or mutated
in a variety of cancer cells. EED is essential for the histone methyltransferase activity
of PRC2.;
Molecule name : APG 5918; EEDi 5273; EEDi-5273; APG-5918;
NCI Metathesaurus CUI : CL1793609;
Origin ID : C188355;
UMLS CUI : C5706488;
Semantic type(s)
- concept_is_in_subset
- has_target
