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  • Title: Synthesis and biological properties of pyrrole-imidazole polyamide conjugates.
    Author: Minoshima M, Sasaki S, Fujimoto J, Shinohara K, Bando T, Sugiyama H.
    Journal: Nucleic Acids Symp Ser (Oxf); 2007; (51):35-6. PubMed ID: 18029573.
    Abstract:
    We have developed a series of conjugates between pyrrole (Py)-imidazole (Im) polyamides and 1-(chloromethyl)-5-hydroxy-1,2-dihydro-3H benz[e]indole (seco-CBI) with an indole linker. High resolution polyacrylamide gel electrophoresis revealed that these conjugates alkylated DNA at predetermined sequences. Then, we demonstrated that conjugates 1 and 2 have DNA alkylation activities at double stranded human telomere sequence and potent cytotoxicities in cancer cell lines. In addition, we showed that conjugate 3 alkylates DNA with ten-base-pair recognition sequence in the presence of partner polyamide 4, which suggested alkylation through 3-4 heterodimer formation.
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