Intracellular Inducible Alkylation System That Exhibits Antisense Effects with Greater Potency and Selectivity than the Natural Oligonucleotide

Abstract

One mismatch is discriminated in a target mRNA sequence by an inducible alkylation system based on sulfide precursors to the nucleoside 2-amino-6-vinylpurine (see scheme). The reactive oligonucleotides were delivered into the cell as poly(ethylene glycol) (PEG) conjugates in polyion-complex (PIC) micelles and showed antisense activity of high selectivity and greater potency than that of the natural antisense oligonucleotide.