Preferred Label : EED Inhibitor BR1733;
NCIt definition : An orally bioavailable inhibitor of the polycomb repressive complex 2 (PRC2) component
embryonic ectoderm development (EED) protein, with potential antineoplastic activity.
Upon oral administration, EED inhibitor BR1733 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 : BR-1733; BR 1733;
NCI Metathesaurus CUI : CL1907085;
Origin ID : C200261;
concept_is_in_subset
- has_target
