Mixing of peptides and electrophilic traps gives rise to potent, broad-spectrum proteasome inhibitors

Org Biomol Chem. 2007 May 7;5(9):1416-26. doi: 10.1039/b702268a. Epub 2007 Mar 23.

Abstract

The synthesis and evaluation of hybrid proteasome inhibitors that contain structural elements of the known inhibitors bortezomib, epoxomicin and peptide vinyl sulfones is described. From the panel of 15 inhibitors some structure activity relationships can be deduced with regard to inhibitory activity in relation to peptide recognition element, inhibitor size and nature of the electrophilic trap. Further, the panel contains one of the most potent peptide-based pan-proteasome inhibitors reported to date.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Peptides / chemistry*
  • Peptides / pharmacology*
  • Proteasome Endopeptidase Complex / metabolism
  • Proteasome Inhibitors*
  • Static Electricity
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Peptides
  • Proteasome Inhibitors
  • Proteasome Endopeptidase Complex