Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors.
Several groups of proteasome inhibitors are widely used to study the role of the ubiquin proteasome pathway in various cellular processes or as anticancer drugs. Peptidomimetics have been developed to circumvent problems inherent in peptides such as poor bioavailability and protease-mediated degradation, while retaining biological activity. In this study, we introduce new pseudopeptides, the retro hydrazino-azapeptoids, designed as proteasome inhibitor peptidomimetics. Their proteasome inhibitory activity and antiproliferative properties are reported here.
Aubin
Sandrine
S
Laboratoire de Synthèse et Electrosynthèse Organiques, UMR CNRS 6510, Université Rennes 1, Av. du Général Leclerc, F-35042 Rennes Cédex, France.
Martin
Bénédicte
B
Delcros
Jean-Guy
JG
Arlot-Bonnemains
Yannick
Y
Baudy-Floc'h
Michèle
M
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D001671:Biochemistry / Q000379:methods; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006834:Hydrazines / Q000737:chemistry; D020128:Inhibitory Concentration 50; D007939:Leukemia L1210; D051379:Mice; D018716:Molecular Mimicry; D034444:Peptoids / Q000737:chemistry* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D061988:Proteasome Inhibitors; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D006834:Hydrazines; D034444:Peptoids; D011480:Protease Inhibitors; D061988:Proteasome Inhibitors