Tag: Proteasome

Epoxomicin is a Selective and Irreversible Inhibitor of Proteasome

Epoxomicin (BU-4061T) is a potent, selective and irreversible proteasome inhibitor. Epoxomicin can cross the blood-brain barrier and has strongly antitumor and anti-inflammatory activity. Proteasome is a 700 kDa, cylindrical-shaped multicatalytic protease complex. It has 28 subunits and organizes into four rings. Besides, Eukaryote 20S proteasome has three major proteolytic...

Oprozomib (PR-047) is an Orally Active Peptide Epoxyketone Proteasome Inhibitor

Proteasome inhibition has been validated as a modality in the research of multiple myeloma and Non-Hodgkin’s lymphoma. The proteasome is a multicatalytic protease complex that is responsible for the ubiquitin-dependent turnover of cellular proteins. Proteasome substrates include misfolded or misassembled proteins as well as short-lived components of signaling cascades...

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...

UT-34 is an Orally Active pan-Androgen Receptor Degrader (SARD)

Prostate cancer drugs targeting the androgen receptor (AR) are mainly competitive ligand-binding domain (LBD) binding antagonists. A common mechanism of drug resistance can inactivate it. Specifically, AR is a nuclear receptor that is activated by binding to any androgen. In addition, radical prostatectomy combined with gonadotropin and androgen synthetase...

ARCC-4 is a Highly Potent PROTAC Androgen Receptor Degrader

Androgen receptor (AR) signaling is crucial for normal prostate development. It also drives the growth and survival of prostate cancer cells. AR signaling suppression is a common strategy for treating prostate cancer. Like other occupancy-based inhibitors, the antiandrogen enzalutamide requires high saturating drug concentrations to achieve its clinical benefit....