Synthesis and Evaluation of Neutral Phosphate Triester Backbone-Modified siRNAs.

ABSTRACT: 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.

SUBMITTER: Tsubaki K 

PROVIDER: S-EPMC7357222 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature