Target spectrum of the BCR-ABL inhibitors imatinib, nilotinib and dasatinib
O Hantschel, U Rix, G Superti-Furga - Leukemia & lymphoma, 2008 - Taylor & Francis
O Hantschel, U Rix, G Superti-Furga
Leukemia & lymphoma, 2008•Taylor & FrancisFollowing the initial success of imatinib as frontline therapy for chronic myeloid leukemia
(CML), several second-generation therapeutics have been developed with increased
potency and the ability to inhibit the majority of imatinib-resistant mutations. Here, we review
the current knowledge about the target specificity of the two new inhibitors nilotinib and
dasatinib in comparison to imatinib, including the recent large-scale chemical proteomics
screens.
(CML), several second-generation therapeutics have been developed with increased
potency and the ability to inhibit the majority of imatinib-resistant mutations. Here, we review
the current knowledge about the target specificity of the two new inhibitors nilotinib and
dasatinib in comparison to imatinib, including the recent large-scale chemical proteomics
screens.
Following the initial success of imatinib as frontline therapy for chronic myeloid leukemia (CML), several second-generation therapeutics have been developed with increased potency and the ability to inhibit the majority of imatinib-resistant mutations. Here, we review the current knowledge about the target specificity of the two new inhibitors nilotinib and dasatinib in comparison to imatinib, including the recent large-scale chemical proteomics screens.
Taylor & Francis Online