Novel fluorinated pseudopeptides as proteasome inhibitors

Lucia Formicola; Xavier Maréchal; Nicolas Basse; Michelle Bouvier-Durand; Danièle Bonnet-Delpon; Thierry Milcent; Michèle Reboud-Ravaux; Sandrine Ongeri

doi:10.1016/j.bmcl.2008.11.012

Novel fluorinated pseudopeptides as proteasome inhibitors

Bioorg Med Chem Lett. 2009 Jan 1;19(1):83-6. doi: 10.1016/j.bmcl.2008.11.012. Epub 2008 Nov 7.

Authors

Lucia Formicola¹, Xavier Maréchal, Nicolas Basse, Michelle Bouvier-Durand, Danièle Bonnet-Delpon, Thierry Milcent, Michèle Reboud-Ravaux, Sandrine Ongeri

Affiliation

¹ Faculté de Pharmacie, Université Paris-Sud 11, UMR-CNRS 8076, Molécules Fluorées et Chimie Médicinale, IFR 141, Châtenay-Malabry cedex, France.

PMID: 19041239
DOI: 10.1016/j.bmcl.2008.11.012

Abstract

We have designed novel small inhibitors of rabbit 20S proteasome using a trifluoromethyl-beta-hydrazino acid scaffold. Structural variations influenced their inhibition of the three types of active sites. Proteasome inhibition at the micromolar level was selective, calpain I and cathepsin B were not inhibited.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Catalytic Domain
Fluorine
Glycine / analogs & derivatives
Molecular Mimicry*
Peptides / chemistry*
Protease Inhibitors / chemical synthesis*
Protease Inhibitors / pharmacology
Proteasome Inhibitors*
Rabbits
Structure-Activity Relationship

Substances

Peptides
Protease Inhibitors
Proteasome Inhibitors
Fluorine
Glycine