Glutamine vinyl ester proteasome inhibitors selective for trypsin-like (beta2) subunit

Eur J Med Chem. 2007 May;42(5):586-92. doi: 10.1016/j.ejmech.2006.12.008. Epub 2007 Jan 9.

Abstract

Here we report the study of a new series of peptide-based proteasome inhibitors with a vinyl ester moiety at C-terminal. The presence of Tic, a rigid analogue of phenylalanine, in the central portion of some derivatives is not favourable for the activity. The best analogue of the series shows a potent and selective inhibition for the beta2 subunit and good enzymatic stability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cysteine Proteinase Inhibitors / pharmacology*
  • Esters
  • Glutamine / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Proteasome Inhibitors*
  • Trypsin / chemistry
  • Trypsin / drug effects*

Substances

  • Cysteine Proteinase Inhibitors
  • Esters
  • Proteasome Inhibitors
  • Glutamine
  • Trypsin