Targeting the SH2-Kinase Interface in Bcr-Abl Inhibits Leukemogenesis

  title={Targeting the SH2-Kinase Interface in Bcr-Abl Inhibits Leukemogenesis},
  author={Florian Grebien and Oliver Hantschel and John Wojcik and Ines Kaupe and Boris Kovacic and Arkadiusz M. Wyrzucki and Gerald D. Gish and Sabine Cerny-Reiterer and Akiko Koide and Hartmut Beug and Tony J. Pawson and Peter Valent and Shohei Koide and Giulio Superti-Furga},
Chronic myelogenous leukemia (CML) is caused by the constitutively active tyrosine kinase Bcr-Abl and treated with the tyrosine kinase inhibitor (TKI) imatinib. However, emerging TKI resistance prevents complete cure. Therefore, alternative strategies targeting regulatory modules of Bcr-Abl in addition to the kinase active site are strongly desirable. Here, we show that an intramolecular interaction between the SH2 and kinase domains in Bcr-Abl is both necessary and sufficient for high… CONTINUE READING
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