Article
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.
Proceedings of the National Academy of Sciences of the United States of America - 2 Aug 2005
Carter Todd A, Wodicka Lisa M, Shah Neil P, Velasco Anne Marie, Fabian Miles A, Treiber Daniel K, Milanov Zdravko V, Atteridge Corey E, Biggs William H, Edeen Philip T, Floyd Mark, Ford Julia M, Grotzfeld Robert M, Herrgard Sanna, Insko Darren E, Mehta Shamal A, Patel Hitesh K, Pao William, Sawyers Charles L, Varmus Harold, Zarrinkar Patrick P, Lockhart David J
Abstract excerpt
To realize the full potential of targeted protein kinase inhibitors for the treatment of cancer, it is important to address the emergence of drug resistance in treated patients. Mutant forms of BCR-ABL, KIT, and the EGF receptor (EGFR) have been found that confer resistance to the drugs imatinib, gefitinib, and erlotinib. The mutations weaken or prevent drug binding, and interestingly, one of the most common...
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