Antisense oligonucleotides containing conformationally constrained 2',4'-(N-methoxy)aminomethylene and 2',4'-aminooxymethylene and 2'-O,4'-C-aminomethylene bridged nucleoside analogues show improved potency in animal models.

@article{Prakash2010AntisenseOC,
  title={Antisense oligonucleotides containing conformationally constrained 2',4'-(N-methoxy)aminomethylene and 2',4'-aminooxymethylene and 2'-O,4'-C-aminomethylene bridged nucleoside analogues show improved potency in animal models.},
  author={Thazah P Prakash and Andrew M. Siwkowski and Charles R. Allerson and Michael Todd Migawa and Sam Poong Lee and Hans J. Gaus and Christopher A. Black and Punit P Seth and Eric E Swayze and B. Shyamasundara Bhat},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 4},
  pages={
          1636-50
        }
}
To identify chemistries and strategies to improve the potency of MOE second generation ASOs, we have evaluated gapmer antisense oligonucleotides containing BNAs having N-O bonds. These modifications include N-MeO-amino BNA, N-Me-aminooxy BNA, 2',4'-BNA(NC)[NMe], and 2',4'-BNA(NC) bridged nucleoside analogues. These modifications provided increased thermal stability and improved in vitro activity compared to the corresponding ASO containing the MOE modification. Additionally, ASOs containing N… CONTINUE READING
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