Thursday, July 25, 2013
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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
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.
Pharmaceutical Co. Ltd. and Johnson
& Johnson market the competitive proteasome inhibitor
Velcade to treat multiple myeloma (MM) and mantle cell lymphoma.
Pharmaceuticals Inc. and Ono
Pharmaceutical Co. Ltd. market the selective proteasome
to treat MM.
At least 10 companies have proteasome inhibitors in Phase III testing or
earlier development to treat cancer.
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
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