Mechanisms of resistance to BCR-ABL and other kinase inhibitors.
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics(2013)
摘要
In this article, we are reviewing the molecular mechanisms that lead to kinase inhibitor resistance. As the oncogenic BCR-ABL kinase is the target of the first approved small-molecule kinase inhibitor imatinib, we will first focus on the structural and mechanistic basis for imatinib resistance. We will then show ways how next generations of BCR-ABL inhibitors and alternative targeting strategies have helped to offer effective treatment options for imatinib-resistant patients. Based on these insights, we discuss commonalities and further mechanisms that lead to resistance to other kinase inhibitors in solid tumors. This article is part of a Special Issue entitled: Inhibitors of Protein Kinases (2012).
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关键词
Kinase inhibitor,BCR-ABL,Imatinib,Resistance
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