Preferred Label : Inobrodib;
NCIt synonyms : p300 HAT/CREB Binding Protein Inhibitor CCS1477; p300/CBP Bromodomain Inhibitor CCS1477;
NCIt definition : An orally bioavailable, small molecule inhibitor of the highly conserved bromodomains
of the histone acetyltransferase (HAT) paralogs, p300 (E1A-associated protein p300;
p300 HAT) and CREB binding protein (CBP), with potential antineoplastic activity.
Upon oral administration, inobrodib selectively and reversibly binds to the bromodomains
of p300 and CBP. This disrupts the acetylation of histones and other proteins and
prevents the co-activation of key transcription factors that contribute to tumor progression
including the androgen receptor (AR), androgen receptor splice variants (AR-SV), hypoxia-inducible
factor 1-alpha (HIF-1-alpha) and Myc proto-oncogene protein (c-Myc). 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.;
UNII : BW5QA5GEW7;
CAS number : 2222941-37-7;
Molecule name : CCS-1477; CCS 1477;
NCI Metathesaurus CUI : CL969329;
Origin ID : C160195;
UMLS CUI : C5667189;
Semantic type(s)
- concept_is_in_subset
