Synthesis and Evaluation of Neutral Phosphate Triester Backbone-Modified siRNAs.
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DOI: 10.1021/acsmedchemlett.0c00232
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… read more here.
Keywords: phosphate triester; synthesis evaluation; backbone modified; phosphate ... See more keywords
SiRNAs with Neutral Phosphate Triester Hydrocarbon Tails Exhibit Carrier-Free Gene-Silencing Activity.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00027
Abstract: Short interfering RNAs (siRNAs) show promise as gene-silencing therapeutics, but their cellular uptake remains a challenge. We have recently shown the synthesis of siRNAs bearing a single neutral phenylethyl phosphotriester linkage within the sense strand.… read more here.
Keywords: gene; gene silencing; phosphate triester; carrier ... See more keywords