Kinases inhibited by imatinib

Nilotinib and dasatinib both emerged into clinical use after the experience of imatinib resistant clinical mutations had been identified and characterized. 

This second generation of Abl kinase inhibitors therefore exemplifies two strategies to overcome clinical resistance. 

In the following sections, the cancers relevant to kinases inhibited by imatinib will be reviewed. Clinical resistance mutations will be described, most of which were identified based on the clinical experience with imatinib. The development of the two second-generation inhibitors will be described, and subsequent clinical experience will be reviewed. Finally, additional kinase inhibitors to this group of kinases will be reviewed. 

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Chu S, Holtz M, Gupta M et al. (2004) BCR/ABL kinase inhibition by imatinib mesylate enhances MAP kinase activity in chronic myelogenous leukemia CD34+ cells. Blood 103 3167-3174... 

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