GNE-987, a BET PROTAC Degrader, is a Part of PROTAC-Antibody (CLL1) Conjugate for ADC
BRD4 is a member of the BET family of proteins (BRD2, 3, 4, and T). It functions as an epigenetic “reader” of acetylated histone lysine residues via its two bromodomain motifs (BD1 and BD2). Disruption of BRD4-histone interactions is an attractive strategy for the development of novel anti-cancer agents....
BETd-260 is a Potent PROTAC BET Degrader
The bromodomain and extra-terminal (BET) family proteins consist of BRD2, BRD3, BRD4, and testis-specific BRDT members. They are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are attractive therapeutic targets for cancer and other human diseases. In this study, BETd-260 is capable...
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....
GSK778 is a Potent and Selective Inhibitor of BET BD1
The bromodomain is a protein domain of about 110 amino acids, which can recognize acetylated lysine residues. Specifically, the bet (Bromo- and terminal domain) family consists of germ cell-specific (BRDT) and ubiquitously expressed (BRD2, BRD3, Brd4) epigenetic reader proteins. As a “reader” of lysine acetylation, bromodomain is responsible for...
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...
CD161 is an Orally Active BET Bromodomain Inhibitor
Bromodomain and extra-terminal (BET) family proteins include BRD2, BRD3, BRD4, and a testis-specific protein BRDT. In this study, researchers identify CD161. CD161 is a potent, orally bioavailable and selective BET bromodomain inhibitor. Especially, CD161 binds to BET proteins with low nanomolar affinities and demonstrates high selectivity over 24 non-BET...
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....