UMB298 is a Selective CBP (P300) Bromodomain Inhibitor
CBP (cyclic AMP response element-binding protein) and P300 (E1A binding protein) are two non-BET bromodomain oncology targets. Additionally, P300 is a paralogue of CBP, and they conduct similar activity. Specifically, CBP and P300 are multidomain proteins containing bromodomain and other domains, such as lysine acetyl transferase (KAT). CBP/P300 bromodomains...
L-Moses Disrupts PCAF-Brd Histone H3.3 Interaction
Bromodomains proteins (Brds) bind to acetylated lysines (KAc) through the Brd acetyllysine-binding site. Misregulation of these proteins is linked to the onset and progression of multiple disease states. They include cancer, HIV infection, and neuroinflammation. The p300/CBP-associated factor, PCAF (KAT2B), is a multi-domain protein. It contains a single Brd,...
NHWD-870 is an Orally Active and Selective BET Bromodomain Inhibitor
Brominedomain can recognize acetylated lysine residues. As the “reader” of lysine acetylation, the bromine domain is responsible for the transduction of signals carried by acetylated lysine residues and transforming them into various normal or abnormal phenotypes. Specifically, the bromine domain-containing proteins have a variety of functions. Besides, it ranges...
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....
BY27 is a Selective and Orally Active BET BD2 Inhibitor
BET (Bromodomain and extra terminal domain) is a well-known member of the bromodomain family. It contains BRD2, BRD3, BRD4, and BRDT, which have two tandem bromodomains (BD1 and BD2). BD1 and BD2 are recognition motifs for the acetyl-lysine residues of N terminuses of histones as well as other proteins....