Abstract: | The proteasome is a multicatalytic protease complex with an unusual enzyme mechanism. It plays a central role in intracellular protein degradation and its important function in the regulation of the cell cycle makes it an interesting target for cancer therapy. First developed as reagents to elucidate the catalytic functions of the proteasome, several proteasome inhibitors are presently being tested in clinical trials. It appears that proteasome inhibitors of the classes peptidyl boronic acids, peptide epoxyketones, and β‐lactone‐γ‐lactams are particularly effective as anticancer agents. |