The biological impact of sequence-specific DNA alkylation by pyrrole-imidazole polyamides

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The biological impact of sequence-specific DNA alkylation by pyrrole-imidazole polyamides
2006
Shunta Sasaki, Masafumi Minoshima, Tatsuhiko Shimizu, Jun Fujimoto, Ken-ichi Shinohara, Toshikazu Bando and Hiroshi Sugiyama
Department of Chemistry, Graduate School of Science, Kyoto University, Kitashirakawa Oiwake, Sakyo-ku, Kyoto 606-8502, Japan
Nucleic Acids Symposium Series 2006
We have developed a series of novel DNA alkylating polyamides possessing indole linkers. Investigations using high-resolution gel electrophoresis revealed that the indole linked Py?Im polyamide alkylated at A of a targeted nine base pair matching sequence. Evaluation in human cancer cell lines revealed that the indole linked Py?Im polyamides have strong cytotoxicities. Furthermore, we showed that alkylation of the template strand of the coding region by these polyamides causes effective gene silencing.
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