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Activity of the ABL kinase inhibitor dasatinib in imatinib-resistant Philadelphia chromosome–positive leukemias
The three-dimensional structure of ABL kinase (green) bound to dasatinib (on left) and imatinib (on right). Dasatinib and imatinib are rendered in stick (carbon atoms in aqua and magenta, respectively). The P loop of ABL is colored yellow, and the activation loop is colored red. Note the diverging direction of the activation loop in the two structures. Imatinib would not be able to bind to the active conformation of ABL because of a clash with the activation loop when it is positioned in the dasatinib-bound ABL conformation. Dasatinib, on the other hand, would be able to bind to the activation loop in either conformation.
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