Bioactivatable inhibitor of ubiquitin-dependent proteasomal degradation

The hyperactive state of malignant cells results in the production of an excess of aberrant proteins that challenge the clearing capacity of the ubiquitin-proteasome system (UPS), resulting in an increased sensitivity towards drugs that reduce the efficacy of this critical proteolytic system. In this project we report the identification of an inhibitor that subsequent to cellular metabolism inhibits the UPS.