2'-carbohydrate modifications in antisense oligonucleotide therapy: importance of conformation, configuration and conjugation.

@article{Manoharan19992carbohydrateMI,
  title={2'-carbohydrate modifications in antisense oligonucleotide therapy: importance of conformation, configuration and conjugation.},
  author={Muthiah Manoharan},
  journal={Biochimica et biophysica acta},
  year={1999},
  volume={1489 1},
  pages={
          117-30
        }
}
The 2'-position of the carbohydrate moiety has proven to be a fertile position for oligonucleotide modifications for antisense technology. The 2'-modifications exhibit high binding affinity to target RNA, enhanced chemical stability and nuclease resistance and increased lipophilicity. All high binding affinity 2'-modifications have C3'-endo sugar pucker. In addition to gauche effects, charge effects are also important in determining the level of their nuclease resistance. Pharmacokinetic… CONTINUE READING
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