Proteasome inhibitors: from in vitro uses to clinical trials

J Pept Sci. 2000 Sep;6(9):478-88. doi: 10.1002/1099-1387(200009)6:9<478::AID-PSC285>3.0.CO;2-F.


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 NFkappaB. 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 NFkappaB) 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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Autoimmune Diseases / drug therapy*
  • Clinical Trials as Topic
  • Cysteine Endopeptidases
  • Data Interpretation, Statistical
  • Disease Models, Animal
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / pathology
  • Molecular Structure
  • Multienzyme Complexes / antagonists & inhibitors*
  • Peptide Hydrolases / metabolism
  • Probability
  • Protease Inhibitors / pharmacology
  • Protease Inhibitors / therapeutic use*
  • Proteasome Endopeptidase Complex


  • Multienzyme Complexes
  • Protease Inhibitors
  • Peptide Hydrolases
  • Cysteine Endopeptidases
  • Proteasome Endopeptidase Complex