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Proteasome inhibitors: from in vitro uses to clinical trials
Author(s) -
Rivett A. Jennifer,
Gardner Robert C.
Publication year - 2000
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/1099-1387(200009)6:9<478::aid-psc285>3.0.co;2-f
Subject(s) - proteasome , intracellular , proteolysis , transcription factor , in vitro , microbiology and biotechnology , protein degradation , chemistry , biochemistry , biology , cancer research , enzyme , gene
Proteasomes are multicatalytic proteinase complexes which play a central role in intracellular protein degradation. They catalyse key events in cell cycle regulation and in the activation of the transcription factor NFκB. Proteasome inhibitors have been useful for the characterization of proteasome catalytic components and in the elucidation of proteasome functions in animal cells. Potent small peptide inhibitors of proteasomes also represent a novel approach to the treatment of inflammatory diseases (which involve activation of NFκB) and cancer. Such compounds have recently been shown to be effective in a variety of animal models, and at least one is currently in use in clinical trials. Copyright © 2000 European Peptide Society and John Wiley & Sons, Ltd.