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Molecular Cancer Therapeutics
Molecular Cancer Therapeutics
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Therapeutic Discovery

Combined Treatment with Silibinin and Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors Overcomes Drug Resistance Caused by T790M Mutation

Jin Kyung Rho, Yun Jung Choi, Byung-Suk Jeon, Su Jin Choi, Gi Jeong Cheon, Sang-Keun Woo, Hye-Ryoun Kim, Cheol Hyeon Kim, Chang-Min Choi and Jae Cheol Lee
Jin Kyung Rho
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Yun Jung Choi
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Byung-Suk Jeon
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Su Jin Choi
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Gi Jeong Cheon
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Sang-Keun Woo
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Hye-Ryoun Kim
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Cheol Hyeon Kim
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Chang-Min Choi
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Jae Cheol Lee
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DOI: 10.1158/1535-7163.MCT-10-0625 Published December 2010
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Abstract

Although epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKI) produce an initially dramatic response in lung cancer patients harboring a mutation in the EGFR gene, development of acquired resistance is almost inevitable. A secondary mutation of threonine 790 (T790M) is associated with approximately half of the cases of acquired resistance. This study investigated whether the addition of silibinin to therapy with gefitinib or erlotinib could overcome T790M-mediated drug resistance considering that silibinin has various antitumor effects, including EGFR modulation. Silibinin selectively reduced the activity of the EGFR family (EGFR, ErbB2, and ErbB3) through the inhibition of receptor dimerization in lung cancer cells with EGFR mutations, but not in those harboring the wild type. In primary and acquired resistant cells with T790M, addition of silibinin enhanced the ability of EGFR-TKIs to downregulate EGFR signals and to inhibit cell growth. Similarly, the combination of silibinin and erlotinib effectively suppressed tumor growth in erlotinib resistance-bearing PC-9 xenografts. The results indicate that the addition of silibinin to EGFR-TKIs is a promising strategy to overcome T790M-mediated drug resistance. Mol Cancer Ther; 9(12); 3233–43. ©2010 AACR.

Footnotes

  • Note: Supplementary material for this article is available at Molecular Cancer Therapeutics Online (http://mct.aacrjournals.org/).

  • Received July 6, 2010.
  • Revision received September 7, 2010.
  • Accepted September 28, 2010.
  • ©2010 American Association for Cancer Research.
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Molecular Cancer Therapeutics: 9 (12)
December 2010
Volume 9, Issue 12
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Combined Treatment with Silibinin and Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors Overcomes Drug Resistance Caused by T790M Mutation
Jin Kyung Rho, Yun Jung Choi, Byung-Suk Jeon, Su Jin Choi, Gi Jeong Cheon, Sang-Keun Woo, Hye-Ryoun Kim, Cheol Hyeon Kim, Chang-Min Choi and Jae Cheol Lee
Mol Cancer Ther December 1 2010 (9) (12) 3233-3243; DOI: 10.1158/1535-7163.MCT-10-0625

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Combined Treatment with Silibinin and Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors Overcomes Drug Resistance Caused by T790M Mutation
Jin Kyung Rho, Yun Jung Choi, Byung-Suk Jeon, Su Jin Choi, Gi Jeong Cheon, Sang-Keun Woo, Hye-Ryoun Kim, Cheol Hyeon Kim, Chang-Min Choi and Jae Cheol Lee
Mol Cancer Ther December 1 2010 (9) (12) 3233-3243; DOI: 10.1158/1535-7163.MCT-10-0625
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Molecular Cancer Therapeutics
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