Target spectrum of the BCR-ABL inhibitors imatinib, nilotinib and dasatinib

被引:198
作者
Hantschel, Oliver [1 ]
Rix, Uwe [1 ]
Superti-Furga, Giulio [1 ]
机构
[1] Austrian Acad Sci, Ctr Mol Med, A-1090 Vienna, Austria
关键词
BCR-ABL; imatinib; drug targets; chemical proteomics;
D O I
10.1080/10428190801896103
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
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.
引用
收藏
页码:615 / 619
页数:5
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