Tag: CBP

NEO2734 is an Orally Active Dual p300/CBP and BET Bromodomain Selective Inhibitor

NUT midline carcinoma (NMC) is a rare, aggressive subtype of squamous carcinoma. This kind of cancer is usually driven by BRD4-NUT fusion oncoprotein. BRD4, a BET protein, binds to chromatin through its two bromodomains. At the same time, NUT recruits the p300 HAT to activate oncogenic target genes transcription....

GNE-207 is an Orally Active Inhibitor for the Bromodomain of CBP

Both CBP (Cyclic AMP response element binding protein, binding protein) and P300 (paralog E1A-associated protein of 300 kDa) possess several structured regions. As such, the histone acetyltransferase (HAT) domain is a common region. It acetylates both histone and non-histone proteins, and bromodomain (BRD) that binds acetylated lysine (KAc). In...