Proteasome Inhibitors

Abstract

Abstract The proteasome has emerged as a major player in regulating essential cellular activities such as cell proliferation and inflammation. The FDA approval of bortezomib, the first‐in‐class proteasome inhibitor drug, for treatment of recurring multiple myeloma, has validated the proteasome as a target for treatment of cancer. This has catalyzed intense medicinal chemistry and library screening efforts to develop novel or improved proteasome inhibitors. Currently, a number of proteasome inhibitors are being investigated in clinical trials for cancer therapy. In this section, particular attention is focused on these inhibitors under clinical trials as well as traditional medicine recently identified as proteasome inhibitors. In addition, we discuss some of the medicinal chemistry efforts in the course of development of proteasome inhibitors with better efficacy. Finally, we describe novel proteasome inhibitors that target specific subunits of proteasomes.