A potent and selective quinoxalinone-based STK33 inhibitor does not show synthetic lethality in KRAS-dependent cells

…, W Silkworth, S Dandapani, M Palmer…

Index: Weiwer, Michel; Spoonamore, James; Wei, Jingqiang; Guichard, Boris; Ross, Nathan T.; Masson, Kristina; Silkworth, Whitney; Dandapani, Sivaraman; Palmer, Michelle; Scherer, Christina A.; Stern, Andrew M.; Schreiber, Stuart L.; Munoz, Benito ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 12 p. 1034 - 1038

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Citation Number: 20

Abstract

The KRAS oncogene is found in up to 30% of all human tumors. In 2009, RNAi experiments revealed that lowering mRNA levels of a transcript encoding the serine/threonine kinase STK33 was selectively toxic to KRAS-dependent cancer cell lines, suggesting that small- molecule inhibitors of STK33 might selectively target KRAS-dependent cancers. To test this hypothesis, we initiated a high-throughput screen using compounds in the Molecular ...