Tag: BRD

MS645, a Bivalent BET BrD Inhibitor, Inhibits BRD4 Transcriptional Activity

Bromodomains (BrDs) in transcription proteins bind acetyl-lysine in histones and transcription factors to direct gene transcription in biology and disease conditions.  BRD4 contains two characteristic tandem BrDs. Meanwhile, BRD4 is a major drug target owing to its implicated functions in oncogenesis and inflammation. BET protein BRD4 in gene transcription...

dBET57 is a Selective PROTAC Degrader of BRD4

PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that bring a target protein into spatial proximity with an E3 ubiquitin ligase to trigger target ubiquitination and subsequent proteasomal degradation. PROTAC recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4. As we all know,...

ARV-825 is a PROTAC Degrader of BRD4 with Profound Anti-Leukemic Effect

BRD4 (Bromodomain-containing protein 4) belongs to the BET family, which also contains BRD2, BRD3, and BRDT. BRD4 has two bromodomains to recognize acetylated lysine residues. They are BD1 and BD2. It also contains an extended C-terminal domain. The latter interacts with P-TEFb and RNA polymerase II to promote gene...

MZP-55 is a Selective PROTAC Degrader of BRD3/4

MZP-55 is a selective PROTAC degrader of BRD3/4, shows no obvious effect on BRD2. MZP-55 exhibits excellent activity in cancer research. PROTAC (proteolysis targeting chimera) is a chimera, functions to degrade certain proteins. It is composed of two headed molecules as well as a linker. One is able to...