Journal
BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS
Volume 1834, Issue 7, Pages 1449-1459Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.bbapap.2012.12.009
Keywords
Kinase inhibitor; BCR-ABL; Imatinib; Resistance
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Funding
- ISREC Foundation
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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). (C) 2012 Elsevier B.V. All rights reserved.
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