Article
Bortezomib-resistant mutant proteasomes: structural and biochemical evaluation with carfilzomib and ONX 0914.
Structure (London, England : 1993) - 3 Feb 2015
Huber Eva M, Heinemeyer Wolfgang, Groll Michael
Abstract excerpt
Inhibition of the 20S proteasome by bortezomib (Velcade) constitutes a successfully applied therapy for blood cancer. However, emerging resistance restricts its medicinal use. For example, mutations in the proteolytically active β5-subunit of the proteasome, the main target of inhibitors, were reported to impair drug binding and thus to reduce therapeutic efficacy. Using yeast as a model system, we describe here...
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