Novel DNA/polymer conjugate for intelligent antisense reagent with improved nuclease resistance

Masaharu Murata, Wataru Kaku, Takahisa Anada, Yoshikuni Sato, Takeshi Kano, Mizuo Maeda, Yoshiki Katayama

Research output: Contribution to journalArticlepeer-review

22 Citations (Scopus)


Antisense technology provides an effective strategy to inhibit synthesis of the gene product. We prepared a novel antisense reagent comprised of oligodeoxynucleotides (ODN) and a thermo responsive polymer, poly(N-isopropylacrylamide) (PNIPAAm). The conjugate inhibited gene expression in a dose-dependent manner. The ODN-PNIPAAm conjugate demonstrated excellent resistance to S1 nuclease. In particular, PNIPAAm-modified antisense ODN at the 3′,5′-ends of the ODN provided complete resistance against nuclease at 37°C, which is above the phase transition temperature of the PNIPAAm side chain. These characteristics of the conjugate suggest it may have potential for use in a new gene delivery system as part of an antisense strategy.

Original languageEnglish
Pages (from-to)3967-3970
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number22
Publication statusPublished - Nov 17 2003

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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