Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids

Bioorg Med Chem Lett. 1998 Feb 17;8(4):333-8. doi: 10.1016/s0960-894x(98)00029-8.


Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases.

MeSH terms

  • Boronic Acids / chemistry
  • Boronic Acids / pharmacology*
  • Cysteine Endopeptidases / drug effects*
  • Molecular Structure
  • Multienzyme Complexes / drug effects*
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology*
  • Proteasome Endopeptidase Complex


  • Boronic Acids
  • Multienzyme Complexes
  • Protease Inhibitors
  • Cysteine Endopeptidases
  • Proteasome Endopeptidase Complex