Preferred Label : BRD4 Inhibitor PLX2853;
NCIt definition : An orally bioavailable inhibitor of the bromodomain-containing protein 4 (BRD4), with
potential antineoplastic activity. Upon oral administration, the BRD4 inhibitor PLX2853
binds to the acetylated lysine recognition motifs in the bromodomains of the BRD4
protein, thereby preventing the binding of BRD4 to acetylated lysines on histones.
This disrupts chromatin remodeling and dyregulates gene expression. This may lead
to the downregulation of the expression of certain growth-promoting genes, which may
induce apoptosis and inhibit the proliferation of BRD4-overexpressing tumor cells.
BRD4, a member of the human bromodomain and extra-terminal (BET) family of proteins,
is a transcriptional regulator that is overexpressed in certain tumor cells and plays
an important role in cellular proliferation.;
Molecule name : PLX 2853; PLX-2853;
NCI Metathesaurus CUI : CL544855;
Origin ID : C146825;
UMLS CUI : C4687482;
Semantic type(s)
- concept_is_in_subset
- has_target
