Article
Mutations that increase both Hsp90 ATPase activity in vitro and Hsp90 drug resistance in vivo.
Biochimica et biophysica acta - 1 May 2010
Zurawska Anna, Urbanski Jakub, Matuliene Jurgita, Baraniak Janina, Klejman Marcin P, Filipek Slawomir, Matulis Daumantas, Bieganowski Pawel
Abstract excerpt
Hsp90 inhibitors are currently tested in clinical trials as anticancer agents. We investigated whether inhibitor resistance may arise as a result of a point mutation in Hsp90. We used yeast cells that expressed human Hsp90beta to select inhibitor-resistant mutants from the randomly mutagenized library. Single amino acid substitution, I123T, in a selected mutant was sufficient to confer inhibitor resistance....
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