title: Novel fluorinated pseudopeptides as proteasome inhibitors.
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.
authors.affiliation: Faculté de Pharmacie, Université Paris-Sud 11, UMR-CNRS 8076, Molécules Fluorées et Chimie Médicinale, IFR 141, Châtenay-Malabry cedex, France.
authors.forename: Lucia
authors.initials: L
authors.lastname: Formicola
authors.forename: Xavier
authors.initials: X
authors.lastname: Maréchal
authors.forename: Nicolas
authors.initials: N
authors.lastname: Basse
authors.forename: Michelle
authors.initials: M
authors.lastname: Bouvier-Durand
authors.forename: Danièle
authors.initials: D
authors.lastname: Bonnet-Delpon
authors.forename: Thierry
authors.initials: T
authors.lastname: Milcent
authors.forename: Michèle
authors.initials: M
authors.lastname: Reboud-Ravaux
authors.forename: Sandrine
authors.initials: S
authors.lastname: Ongeri
mesh_terms: D000818:Animals; D020134:Catalytic Domain; D005461:Fluorine; D005998:Glycine / Q000031:analogs & derivatives; D018716:Molecular Mimicry; D010455:Peptides / Q000737:chemistry*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D061988:Proteasome Inhibitors; D011817:Rabbits; D013329:Structure-Activity Relationship
chemical_list: D010455:Peptides; D011480:Protease Inhibitors; D061988:Proteasome Inhibitors; D005461:Fluorine; D005998:Glycine