| 摘要 |
<p>The invention relates to antisense oligonucleotides. More particularly, the invention relates to the stabilization of antisense oligonucleotides by modification of internucleoside linkages. The invention provides antisense oligonucleotides which have the benefit of stability provided by phosphorothioate linkages without the side effects. The invention achieves this by providing antisense oligonucleotides having phosphorothiate linkages only at the most 3' positions. This is made possible by incorporating only stereospecific S-enantiomers of phosphorothioate linkages at those positions. Surprisingly, such antisense oligonucleotides retain the stability of antisense oligonucleotides in which all of the internucleoside linkages are phosphorothioates.</p> |
