Recently, we have demonstrated that 2-amino-6-vinypurine derivative (1) achieves triplex-forming cross-linking with high selectivity toward the cytosine of the G-C target site. In this study, we have investigated the cross-linking as well as induction of point mutations with the TFO incorporating 1 to a target site in a shuttle vector plasmid that replicates in mammalian cells. It was revealed that the TFO bearing 1 introduced mutations at the site of cross-linking. These results have suggested that the selective cross-linking with 1 might be useful for development of new biotechnology for targeted-mutagenesis.
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