Maximizing the benefi of off-target kinase inhibitor activity

Abstract

Investigators report the identifi cation of novel mutant-specifi c 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. © 2012 American Association for Cancer Research.