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Cell culture studies suggest a noncompetitive, imidazoline-based proteasome inhibitor could help treat cancer. In in vitro assays, the lead compound inhibited the proteasome with an IC50 value of
130 nM without targeting the proteasome catalytic site. In cultured human myeloma cell lines sensitive or insensitive to Velcade bortezomib, the lead imidazoline-based inhibitor caused greater cell death than the parent inhibitor. Next steps include evaluating the in vivo toxicity of the lead inhibitor.
Takeda Pharmaceutical Co. Ltd. and Johnson & Johnson market the competitive proteasome inhibitor Velcade to treat multiple myeloma (MM) and mantle cell lymphoma.
Onyx Pharmaceuticals Inc. and Ono Pharmaceutical Co. Ltd. market the selective proteasome inhibitor Kyprolis carfilzomib to treat MM.
At least 10 companies have proteasome inhibitors in Phase III testing or earlier development to treat cancer.

SciBX 6(28); doi:10.1038/scibx.2013.715
Published online July 25, 2013

Patented; available for licensing from Michigan State University Technologies

Azevedo, L.M. et al. J. Med. Chem.; published online June 22, 2013;
Contact: Jetze J. Tepe, Michigan State University, East Lansing, Mich.