Article
Selective cytotoxicity of a bicyclic Ras inhibitor in cancer cells expressing K-Ras(G13D).
Biochemical and biophysical research communications - 4 Sept 2009
Palmioli Alessandro, Sacco Elena, Airoldi Cristina, Di Nicolantonio Federica, D'Urzo Annalisa, Shirasawa Senji, Sasazuki Takehiko, Di Domizio Alessandro, De Gioia Luca, Martegani Enzo, Bardelli Alberto, Peri Francesco, Vanoni Marco
Abstract excerpt
Mutation of RAS genes is a critical event in the pathogenesis of different human tumors and in some developmental disorders. Here we present an arabinose-derived bicyclic compound displaying selective cytotoxicity in human colorectal cancer cells expressing K-Ras(G13D), that shows high intrinsic nucleotide exchange rate. We characterize binding of bicyclic compounds by docking and NMR experiments and their...
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