Advances in Proteasome Inhibition

Dear Colleagues,

The ubiquitin–proteasome pathway (UPP) is the major proteolytic system in the cytosol and nucleus of all eukaryotic cells, and it is crucial for intracellular protein homeostasis in physiological conditions and adaptive stress responses. The 26S proteasome is a large multifunctional particle composed of a barrel-shaped 20S core particle, which contains the protease subunits, capped by two 19S regulatory particles that control the proteolytic function of the protease core. UPP is responsible for the inappropriate or accelerated cell cycle regulatory proteins degradation that occurs because of pathological conditions in which the normal cellular pathways become dysregulated, such as cancer, resulting in accelerated and uncontrolled mitosis and promoting cancer growth and spread. For this reason, proteasome inhibitors are employed to treat cancer (e.g., multiple myeloma and mantle cell lymphoma). To date, three proteasome inhibitors (bortezomib, carfilzomib, and ixazomib) have been approved by the Food and Drug Administration and European Medicines Agency for the treatment of these pathologies. However, further research is needed due to the lack of selectivity and resistance development of the compounds and drugs discovered so far. Papers related to any aspect of proteasome inhibition will be considered for this Special Issue. Experimental and bioinformatics papers, up-to-date review articles, and commentaries are also welcome.

This Special Issue aims to provide a platform for molecular mechanistic research on proteasome inhibitors, with a special focus on drug targets and their roles in diseases. We warmly welcome your submissions of original papers and reviews based on results from molecular viewpoints.

This Special Issue is supervised by Dr. Laura Ielo and assisted by our Topical Advisory Panel Member, Dr. Andrea Citarella <[email protected]> (Department of Chemistry, University of Milan, Via Golgi 19, 20133 Milano, Italy).

Dr. Laura Ielo
Guest Editor

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• proteasome inhibitors
• anti-proliferative activity
• in vivo studies
• in vitro studies
• multiple myeloma
• natural products
• cancer
• crystal structures