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

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 revea...

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Bibliographic Details
Published in:Nucleic Acids Symposium Series 2006-11, Vol.50 (1), p.111-112
Main Authors: Sasaki, Shunta, Minoshima, Masafumi, Shimizu, Tatsuhiko, Fujimoto, Jun, Shinohara, Ken-ichi, Bando, Toshikazu, Sugiyama, Hiroshi
Format: Article
Language:English
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Summary: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.
ISSN:0261-3166
1746-8272
DOI:10.1093/nass/nrl055