Article
Inhibition of KRAS codon 12 mutants using a novel DNA-alkylating pyrrole-imidazole polyamide conjugate.
Nature communications - 27 Apr 2015
Hiraoka Kiriko, Inoue Takahiro, Taylor Rhys Dylan, Watanabe Takayoshi, Koshikawa Nobuko, Yoda Hiroyuki, Shinohara Ken-ichi, Takatori Atsushi, Sugimoto Hirokazu, Maru Yoshiaki, Denda Tadamichi, Fujiwara Kyoko, Balmain Allan, Ozaki Toshinori, Bando Toshikazu, Sugiyama Hiroshi, Nagase Hiroki
Abstract excerpt
Despite extensive efforts to target mutated RAS proteins, anticancer agents capable of selectively killing tumour cells harbouring KRAS mutations have remained unavailable. Here we demonstrate the direct targeting of KRAS mutant DNA using a synthetic alkylating agent (pyrrole-imidazole polyamide indole-seco-CBI conjugate; KR12) that selectively recognizes oncogenic codon 12 KRAS mutations. KR12 alkylates adenine...
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