Article
Sequence-specific DNA alkylation targeting for Kras codon 13 mutation by pyrrole-imidazole polyamide seco-CBI conjugates.
Chemistry (Weinheim an der Bergstrasse, Germany) - 27 Jan 2014
Taylor Rhys Dylan, Asamitsu Sefan, Takenaka Tomohiro, Yamamoto Makoto, Hashiya Kaori, Kawamoto Yusuke, Bando Toshikazu, Nagase Hiroki, Sugiyama Hiroshi
Abstract excerpt
Hairpin N-methylpyrrole-N-methylimidazole polyamide seco-CBI conjugates 2-6 were designed for synthesis by Fmoc solid-phase synthesis, and their DNA-alkylating activities against the Kras codon 13 mutation were compared by high-resolution denaturing gel electrophoresis with 225 base pair (bp) DNA fragments. Conjugate 5 had high reactivity towards the Kras codon 13 mutation site, with alkylation occurring at the A...
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