Disulfide-unit conjugation enables ultrafast cytosolic internalization of antisense DNA and siRNA

Papers published
Z. Shu, I. Tanaka, A. Ota, D. Fushihara, N. Abe, S. Kawaguchi, K. Nakamoto, F. Tomoike, S. Tada, Y. Ito, Y. Kimura, and H. Abe, Angewandte Chemie International Edition, (2019). DOI: 10.1002/anie.201900993
  • Antisense and siRNA-mediated gene expression suppression have attracted great promise as innovative treatments for diseases that are difficult to treat with small molecule drugs. However, one of the major problems is that oligonucleotides have difficulty in getting into cells. Intracellular delivery methods based on liposomes are generally used for this, but the problem has been that oligonucleotides remain in endosomes for more than 4 hours and their transition into the cytoplasm is very slow. In this study, we successfully delivered oligonucleotides into the cytoplasm highly efficiently in a short time of about 10 minutes by tandemly introducing disulfide units at the end of oligonucleotides. This method is an excellent method for intracytoplasmic delivery of oligonucleotides, and its application to oligonucleotide medicines is highly expected.

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