Synthesis and Evaluation of Neutral Phosphate Triester Backbone-Modified siRNAs
Two unsymmetrical dinucleotide phosphate triesters were synthesized via transesterification from tris(2,2,2-trifluoroethyl) phosphate. The protected triesters were phosphytilated to generate phosphoramidites for solid-phase oligonucleotide synthesis. Neutral phenylethyl phosphate-modified short-interfering RNAs (siRNAs) were synthesized and evaluated for their gene-silencing ability, siRNA strand selection, and resistance to nucleases. These backbone-modified phosphate triester siRNAs offer many improvements compared to natural unmodified siRNAs.
Desaulniers, Jean-Paul,Hammill, Matthew L.,Kitamura, Mitsuru,Okauchi, Tatsuo,Tsubaki, Kouta,Varley, Andrew J.
p. 1457 - 1462
(2020/11/02)
O-Allyl Protection of Guanine and Thymine Residues in Oligodeoxyribonucleotides
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Hayakawa, Yoshihiro,Hirose, Masaaki,Noyori, Ryoji
p. 5551 - 5555
(2007/10/02)
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