Preferred Label : BET/CBP/p300 Inhibitor EP31670;
NCIt synonyms : BET/CBP/p300 Bromodomain Inhibitor EP31670; BET/CBP/p300 BRD Inhibitor EP31670; BET/CBP/p300 Inhibitor NEO2734; BET and CBP/p300 Inhibitor EP31670;
NCIt definition : An orally bioavailable inhibitor of the bromodomains (BRDs) of the bromodomain and
extra-terminal (BET) family of proteins and the histone acetyltransferase (HAT) paralogs
CREB binding protein (CBP) and p300 (E1A-associated protein p300; p300 HAT), with
potential antineoplastic activity. Upon oral administration, BET/CBP/p300 inhibitor
EP31670 targets and binds to the BET proteins bromodomain-containing proteins 2, 3,
and 4 (BRD2, BRD3, and BRD4) and bromodomain testis-specific protein (BRDT), as well
as the BRD of CBP and p300. This prevents the interaction between BET proteins and
acetylated histones, disrupts chromatin remodeling and suppresses the expression of
certain oncogenes, resulting in the inhibition of tumor cell growth. BET proteins
are transcriptional regulators that play an important role in the modulation of gene
expression during cellular growth and development. In addition, this prevents the
co-activation of the androgen receptor (AR) including AR-v7 by CBP and p300, which
may inhibit tumor cell proliferation in AR-positive tumor cells. The HAT paralogs
CBP and p300 are key transcriptional co-activators that are essential for a multitude
of cellular processes and are implicated in the progression and therapeutic resistance
of certain cancers.;
Molecule name : EP 31670; NEO 2734; EP-31670; NEO-2734;
NCI Metathesaurus CUI : CL1798786;
Origin ID : C190126;
UMLS CUI : C5783512;
Semantic type(s)
- concept_is_in_subset
- has_target
