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Cell culture studies identified peptide-based, noncovalent inhibitors of the 20S proteasome that could be useful for treating cancer. Marketed proteasome inhibitors bind the target covalently, and noncovalent inhibitors could potentially hit the target with more specificity and fewer side effects. A series of dimerized linear mimics of a noncovalent cyclopeptide proteasome inhibitor were generated, and the most potent members of the series inhibited the 20S proteasome's catalytic activity with micromolar and submicromolar IC50 values in a human cell line. Next steps include evaluating the in vivo biological activity, toxicity and stability of the lead peptides.
Takeda Pharmaceutical Co. Ltd. and Johnson & Johnson market Velcade bortezomib, a covalent small molecule dipeptide boronic acid proteasome inhibitor, to treat multiple myeloma (MM) and mantle cell lymphoma (MCL).
Onyx Pharmaceuticals Inc. and Ono Pharmaceutical Co. Ltd. market Kyprolis carfilzomib, a covalent proteasome inhibitor, to treat MM.
At least five other companies have proteasome inhibitors in Phase II testing or earlier to treat various types of cancer.

SciBX 6(15); doi:10.1038/scibx.2013.359
Published online April 18, 2013

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Desvergne, A. et al. J. Med. Chem.; published online March 29, 2013;
Contact: Michèle Reboud-Ravaux, Pierre and Marie Curie University, Paris, France
Contact: Joelle Vidal, University of Rennes 1, Rennes, France