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Nilotinib and MEK inhibitors induce synthetic lethality through paradoxical activation of RAF in drug-resistant chronic myeloid leukemia

SUMMARY: We show that imatinib, nilotinib and dasatinib possess weak off-target activity against RAF and therefore drive paradoxical activation of BRAF and CRAF in a RAS-dependent manner. Critically, since RAS is activated by BCR-ABL, in drug-resistant chronic myeloid leukemia (CML) cells RAS activi...

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Detalhes bibliográficos
Main Authors: Packer, Leisl M., Rana, Sareena, Hayward, Robert, O'Hare, Thomas, Eide, Christopher A., Rebocho, Ana, Heidorn, Sonja, Zabriskie, Matthew S., Niculescu-Duvaz, Ion, Druker, Brian J., Springer, Caroline, Marais, Richard
Formato: Artigo
Idioma:Inglês
Publicado em: 2011
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Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3951999/
https://ncbi.nlm.nih.gov/pubmed/22169110
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.ccr.2011.11.004
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