Development of pseudopeptides and peptidomimetics as eukaryote proteasome inhibitors

Date publication

octobre 2009

Auteurs

Membres identifiés du Cancéropôle Est :
Dr VANDERESSE Régis

Tous les auteurs :
Basse N, Felten AS, Papapostolou D, Bernard E, Jamart-Gregoire B, Reboud-Ravaux M, Vanderesse R

Résumé

Deregulation of the ubiquitin-proteasome system has been implicated in the pathogenesis of many diseases. The regulation of the proteasome activity by specific inhibitors makes this enzyme a promising target for cancer treatment. We present here the design, synthesis and biological evaluation of novel pseudopeptides acting as inhibitors of eukaryote 20S proteasome. D-Amino acids were also introduced into the peptides of interest to reduce proteolysis. To cite this article: N. Basse et al., C R. Chimie 12 2009. (C) 2009 Academie des sciences. Published by Elsevier Masson SAS. All rights reserved.

Référence

C R Chim. 2009 Oct-nov;12(10-11):1163-72