MAGA G.

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Protein kinases, either membrane-embedded receptorial or cytosolic non-receptorial ones, are important transducers of cell proliferation signals. In almost all tumor cells, the activity of some kinases is deregulated, either because of the presence of cancer-specific aberrant forms, or as a consequence of alterations in regulatory pathways, at...

The tyrosine kinase Src and its close homolog Abl, both play important roles in chronic myelogenous leukemia (CML) progression and Imatinib resistance. No clin. approved inhibitors of the drug-resistant AblT315I exist to date. Here, we present a thorough kinetic anal. of two potent dual Src-Abl inhibitors towards wild type Src and Abl, and...