Preferred Label : CBP/p300 Bromodomain Inhibitor OPN-6602;
NCIt synonyms : EP300/CBP Bromodomain Inhibitor OPN-6602;
NCIt definition : An orally bioavailable small molecule inhibitor of the bromodomain of the histone
acetyltransferase (HAT) paralogs, CREB binding protein (CBP) and p300 (E1A-associated
protein p300; EP300; p300 HAT), with potential antineoplastic activity. Upon oral
administration, CBP/p300 bromodomain inhibitor OPN-6602 targets and binds to the bromodomains
of p300 and CBP. This disrupts the acetylation of histones and other proteins, prevents
the co-activation of key transcription factors that contribute to tumor progression
including the androgen receptor (AR), interferon regulatory factor 4 (IRF4) and Myc
proto-oncogene protein (c-Myc), and downregulates AR and IRF4/MYC signaling, thereby
inhibiting tumor cell proliferation. The HAT paralogs p300 and CBP 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 : OPN-6602; OPN 6602;
Origin ID : C207752;
concept_is_in_subset
- has_target
