Proteasome inhibitors: from research tools to drug candidates.

By A. Kisselev, A. Goldberg. Chemistry and Biology, 2001

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Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome. (2007, background): “Although both PR-171 and bortezomib form covalent adducts with the proteasome (25, 30), the hydrolytic stability of the two inhibitor-enzyme complexes differ: the dual covalent morpholino adduct formed with PR-171 is irreversible, whereas the tetrahedral intermediate formed with bortezomib is slowly”
Protein degradation and protection against misfolded or damaged proteins (2003, background): “When unfolded proteins build up and exceed the cell's degradative capacity (for example, in the presence of proteasome inhibitors), cells activate the heat-shock respons”
Protein degradation by the ubiquitin-proteasome pathway in normal and disease states. (2006, background): “Because the proteolytic mechanism is novel, highly specific inhibitors of the active sites have been synthesized (or microorganisms have produced them) (40).”
The ubiquitin ligase activity in the DDB2 and CSA complexes is differentially regulated by the COP9 signalosome in response to DNA damage. (2003, background): “Conversely, DDB2 in the complexes purified from cells (Kisselev and Goldberg, 2001).”