An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry
between 2018 and 2021 was conducted to identify lead generation strategies most …

Cancer cells are characterized by a higher rate of protein turnover and greater demand for
protein homeostasis compared to normal cells. In this scenario, the ubiquitin–proteasome …

The ubiquitin-proteasome system (UPS) is critical for protein quality control and regulating
protein lifespans. Following ubiquitination, UPS substrates bind multidomain receptors that …

The ubiquitin–proteasome system (UPS) is involved in multiple cellular functions including
the regulation of protein homeostasis, major histocompatibility (MHC) class I antigen …

Proteasome is a multi-subunit protein degradation machine, which plays a key role in the
maintenance of protein homeostasis and, through degradation of regulatory proteins, in the …

The proteasome is the central component of the main cellular protein degradation pathway.
During the past four decades, the critical function of the proteasome in numerous …

The proteasome is responsible for mediating intracellular protein degradation and
regulating cellular function with impact on tumor and immune effector cell biology. The …

Numerous cellular processes are controlled by the proteasome, a multicatalytic protease in
the cytosol and nucleus of all eukaryotic cells, through regulated protein degradation. The …

The recent ascent of targeted covalent inhibitors (TCI) in drug discovery brings new
opportunities and challenges to quantum chemical reactivity calculations supporting …

Proteasomes are broadly expressed key components of the ubiquitin-dependent protein
degradation pathway containing catalytically active subunits (β1, β2, and β5). LMP7 (β5i) is …