Article
Impaired bortezomib binding to mutant β5 subunit of the proteasome is the underlying basis for bortezomib resistance in leukemia cells.
Leukemia - 1 Apr 2012
Franke N E, Niewerth D, Assaraf Y G, van Meerloo J, Vojtekova K, van Zantwijk C H, Zweegman S, Chan E T, Kirk C J, Geerke D P, Schimmer A D, Kaspers G J L, Jansen G, Cloos J
Abstract excerpt
Proteasome inhibition is a novel treatment for several hematological malignancies. However, resistance to the proteasome inhibitor bortezomib (BTZ, Velcade) is an emerging clinical impediment. Mutations in the β5 subunit of the proteasome, the primary target of BTZ, have been associated with drug resistance. However, the exact mechanism by which these mutations contribute to BTZ resistance, is still largely...
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