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Chem Biol. 2001 Aug;8(8):739-58.

Proteasome inhibitors: from research tools to drug candidates.

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Department of Cell Biology, Harvard Medical School, 240 Longwood Ave., Boston, MA 02115, USA.


The 26S proteasome is a 2.4 MDa multifunctional ATP-dependent proteolytic complex, which degrades the majority of cellular polypeptides by an unusual enzyme mechanism. Several groups of proteasome inhibitors have been developed and are now widely used as research tools to study the role of the ubiquitin-proteasome pathway in various cellular processes, and two inhibitors are now in clinical trials for treatment of multiple cancers and stroke.

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