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....
Alobresib is an Orally Active BET Bromodomain Inhibitor for Uterine Serous Carcinoma Treatment
Uterine serous carcinoma is a rare and highly aggressive variant of endometrial cancer. Uterine serous carcinoma accounts for 10% of all endometrial cancer; however, it carries the poorest prognosis, with 5-year survival rates as low as 55%. Whole-exome sequencing studies have recently reported c-Myc gene amplification in a large...
dBET6, an Orally Active PROTAC Degrader of BET, Has Potential to Treat ALL
Development of drugs based on PROTAC is not new to us. We have mentioned the technology many times in our blogs. PROTAC is used to move the unwanted proteins to treat terrible diseases, especially various kinds of cancer. Today, we will talk about another PROTAC agent used in the...
BAY1238097 is a Selective Inhibitor of BET Binding to Histones
Several BET inhibitors with strong anti-tumor efficacy have been described in recent years. Most of them are derived from diazepine and azepine scaffolds, besides, more recently quinazolinones and isoxazoles chemotypes have been identified. Additionally, a study from Pascale Lejeune identified and verified a novel BET inhibitor BAY1238097, which shows...