修飾型センスと天然型アンチセンスからなる二本鎖オリゴデオキシヌクレオチドの安定性と生体内動態

概要

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Novel stabilizing method for unmodified oligodeoxynucleotides (ODNs) has been investigated. Chemically modified ODNs, which carry complementary sequences of unmodified antisense ODN, can form a double-stranded complex with the ability to stabilize the unmodified oligomer. The modifications were made on phosphodiester back-bone (phosphorothioate, SO), thymine base (5-phenylethyl substitution), 5'-terminal(introduction of poly(ethylene glycol)). To determine the potential of this method, the in vitro stability in human plasma and in vivo retention in mouse after iv injection of the hemi-modified double-stranded ODNs were evaluated. Dissociation of unmodified antisensc ODN from the hemi modified double-strand and reconstitution of the double-strand with an unmodified sense ODN were also recognized.
日本DDS学会の論文