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Cancer Discov. 2013 Feb;3(2):138-40. doi: 10.1158/2159-8290.CD-12-0581.

Maximizing the benefits of off-target kinase inhibitor activity.

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1
Department of Medicine, Vanderbilt-Ingram Cancer Center, Nashville, Tennessee 37232, USA.

Abstract

Investigators report the identification of novel mutant-specific inhibition of EGF receptor (EGFR) T790M by bis-indole-based inhibitors of protein kinase C using a small-molecule cancer cell line-based screening platform. This study shows the power of high-throughput drug screening in cancer cell lines and provides new lead scaffolds for optimization against resistant EGFR mutants in lung cancer.

PMID:
23400472
DOI:
10.1158/2159-8290.CD-12-0581
[Indexed for MEDLINE]
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