Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids

J Adams; M Behnke; S Chen; A A Cruickshank; L R Dick; L Grenier; J M Klunder; Y T Ma; L Plamondon; R L Stein

doi:10.1016/s0960-894x(98)00029-8

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.

Authors

J Adams¹, M Behnke, S Chen, A A Cruickshank, L R Dick, L Grenier, J M Klunder, Y T Ma, L Plamondon, R L Stein

Affiliation

¹ ProScript, Inc., Cambridge, MA 02139, USA.

PMID: 9871680
DOI: 10.1016/s0960-894x(98)00029-8

Abstract

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

Substances

Boronic Acids
Multienzyme Complexes
Protease Inhibitors
Cysteine Endopeptidases
Proteasome Endopeptidase Complex