Article
Inhibition of the ubiquitin-proteasome system by an NQO1-activatable compound.
Cell death & disease - 6 Oct 2021
Giovannucci Tatiana A, Salomons Florian A, Haraldsson Martin, Elfman Lotta H M, Wickström Malin, Young Patrick, Lundbäck Thomas, Eirich Jürgen, Altun Mikael, Jafari Rozbeh, Gustavsson Anna-Lena, Johnsen John Inge, Dantuma Nico P
Abstract excerpt
Malignant cells display an increased sensitivity towards drugs that reduce the function of the ubiquitin-proteasome system (UPS), which is the primary proteolytic system for destruction of aberrant proteins. Here, we report on the discovery of the bioactivatable compound CBK77, which causes an irreversible collapse of the UPS, accompanied by a general accumulation of ubiquitylated proteins and caspase-dependent...
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