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Most known proteasome inhibitors4,5 are peptidomimetics containing an electrophilic functional group, and can therefore be classified as site-directed enzyme inhibitors. This group is normally placed at one end of the molecule and reacts with the threonine hydroxyl after its activation. Many of these compounds bear a close relationship with inhibitors of serine proteases (e.g., HIV protease). Some representative examples are given below. Among these compounds, borte-zomib was approved in 2003 for the treatment of multiple myeloma, the second most common hematological cancer, and is currently being clinically evaluated for various other malignancies.6 Bortezomib (PS-341, LDP-341, MLN-341) affects multiple signaling cascades (e.g., NF-kB) within the cell because of proteasome inhibition and induces G2/M phase arrest followed by apoptosis in cancer cells.7

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