2. Academic Validation
  3. Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors

Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors

  • J Med Chem. 2005 Jan 13;48(1):330-4. doi: 10.1021/jm049455f.
Sandrine Aubin 1,  Bénédicte Martin,  Jean-Guy Delcros,  Yannick Arlot-Bonnemains,  Michèle Baudy-Floc'h
Affiliations

Affiliation

  • 1 Laboratoire de Synthèse et Electrosynthèse Organiques, UMR CNRS 6510, Université Rennes 1, Av. du Général Leclerc, F-35042 Rennes Cédex, France.
PMID: 15634028 DOI: 10.1021/jm049455f
Abstract

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.

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