LNA GAPMER OLIGONUCLEOTIDES COMPRISING CHIRAL PHOSPHOROTHIOATE LINKAGES

摘要

The present relates to LNA gapmer antisense oligonucleotides which comprise stereodefined phosphoramidite linkages. The use of stereodefined phosphoramidite linkages in LNA gapmers has been found to provide enhanced RNaseH activity, and modifying stereospecificity enables the reduced toxicity, altered biodistribution, and enhanced mismatch discrimination.