Abstract

Introduction: Targeting ubiquitin-proteasome system (UPS) has emerged as a rational approach in the treatment of human cancer. The therapeutic potential of this pathway has been validated by the clinical successes of bortezomib – the first proteasome inhibitor drug implemented in the therapy of multiple myeloma and mantle cell lymphoma. However, the treatment of solid tumors remains challenging, mostly due to poor tumor-selective drug delivery and low therapeutic efficacy. Previously, we reported on the development of novel potential therapeutic – CPL-410-005 – a non-selective, cell permeable, inhibitor of ubiquitin-activating enzyme (E1).

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