Proteasomes contribute to maintaining protein homeostasis and their inhibition is beneficial
in certain types of cancer and in autoimmune diseases. However, the inhibition of the …

Inhibitors of the immunoproteasome (i-20S) have shown promise in mouse models of
autoimmune diseases and allograft rejection. In this study, we used a novel inhibitor of the …

The ubiquitin‐proteasome pathway (UPP) represents the principal proteolytic apparatus in
the cytosol and nucleus of all eukaryotic cells. Nowadays, proteasome inhibitors (PIs) are …

Proteasomes of pathogenic microbes have become attractive targets for anti-infectives.
Coevolving with its human host, Mycobacterium tuberculosis (Mtb) has developed …

Large-scale virtual screening of boronic acid derivatives was performed to identify
nonpeptidic covalent inhibitors of the β5i subunit of the immunoproteasome. A hierarchical …

A structure-based virtual screening of over 400,000 small molecules against the constitutive
proteasome activity followed by in vitro assays led to the discovery of a family of proteasome …

The ubiquitin–proteasome system is responsible for the degradation of proteins and plays a
critical role in key cellular processes. While the constitutive proteasome (cPS) is expressed …

Inhibitors of the proteasome have found broad therapeutic applications; however, they show
severe toxicity due to the abundance of proteasomes in healthy cells. In contrast, inhibitors …

Remarkable successes with the FDA-approved proteasome inhibitors bortezomib
(Velcade®) and carfilzomib (Kyprolis®) have proved that the proteasome is an effective …

Carfilzomib, a second-generation proteasome inhibitor, has significantly improved the
survival rate of multiple myeloma (MM) patients, but its clinical application is still restricted by …