Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

The ubiquitin–proteasome system (UPS) plays an important role in the cellular processes for
protein quality control and homeostasis. Dysregulation of the UPS has been implicated in …

The ubiquitin system is complex, multifaceted, and is crucial for the modulation of a vast
number of cellular processes. Ubiquitination is tightly regulated at different levels by a range …

Background Ixazomib is an oral proteasome inhibitor that is currently being studied for the
treatment of multiple myeloma. Methods In this double-blind, placebo-controlled, phase 3 …

Drug resistance is a major obstacle in the field of pre-clinical and clinical therapeutics. The
development of novel technologies and targeted therapies have yielded new modalities to …

Proteasome inhibitors are one of the most important classes of agents to have emerged for
the treatment of multiple myeloma in the past two decades, and now form one of the …

Dynamic modulation of protein levels is tightly controlled in response to physiological cues.
In mammalian cells, much of the protein degradation is carried out by the ubiquitin …

Control of protein levels by nucleic-acid-based technologies has proven to be a useful
research tool but lacks the advantages of small molecules with respect to cell permeability …

Proteasomes are large, multisubunit proteolytic complexes presenting multiple targets for
therapeutic intervention. The 26S proteasome consists of a 20S proteolytic core and one or …

Newly synthesized transmembrane proteins undergo a series of steps to ensure that only
the required amount of correctly folded protein is localized to the membrane. The regulation …