PR-619 is a Broad-Range DUB Inhibitor
Ubiquitination is a post-translational modification where the polypeptide ubiquitin is attached to lysine residues of substrate proteins. This process is reversible, and ubiquitin removal is orchestrated by a large family of deubiquitinating enzymes (DUBs). DUBs fall into six subfamilies based on sequence and domain similarity. Ubiquitination and deubiquitination together...
RA-9 is a Selective Proteasome-Associated DUBs Inhibitor
The ubiquitin-proteasome-system (UPS) is responsible for most of the intracellular protein degradation in eukaryotes. UPS consists of three components: the proteasomes, the ubiquitin conjugating system, and the deubiquitinating enzymes (DUBs). DUBs deconjugate ubiquitin from targeted proteins and this step is essential for protein degradation. The de-ubiquitination is required for...
GSK2643943A is a Novel DUB Inhibitor
The ubiquitin proteasome system participates in a variety of biological functions including cell cycle progression, intracellular signaling and protein degradation. Therefore, it is not surprising to find many misregulation of this system in cancer. Fortunately, the first-generation deubiquitylating enzyme (DUB) inhibitors are now approaching clinical trials. For instance, the...