Article
Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I.
Blood - 15 Apr 2008
Gontarewicz Artur, Balabanov Stefan, Keller Gunhild, Colombo Riccardo, Graziano Alessio, Pesenti Enrico, Benten Daniel, Bokemeyer Carsten, Fiedler Walter, Moll Jürgen, Brümmendorf Tim H
Abstract excerpt
The emergence of resistance to imatinib (IM) mediated by mutations in the BCR-ABL domain has become a major challenge in the treatment of chronic myeloid leukemia (CML). Here, we report on studies performed with a novel small molecule inhibitor, PHA-739358, which selectively targets Bcr-Abl and Aurora kinases A to C. PHA-739358 exhibits strong antiproliferative and proapoptotic activity against a broad panel of...
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