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Syntheses of prodrug-type phosphotriester oligonucleotides responsive to intracellular reducing environment for improvement of cell membrane permeability and nuclease resistance.

Abstract：

:We synthesized prodrug-type phosphotriester (PTE) oligonucleotides containing the six-membered cyclic disulfide moiety by using phosphoramidite chemistry. Prodrug-type oligonucleotides named "Reducing-Environment-Dependent Uncatalyzed Chemical Transforming (REDUCT) PTE oligonucleotides" were converted into natural oligonucleotides under cytosol-mimetic reductive condition. Furthermore, the REDUCT PTE oligonucleotides were robust to nuclease digestion and exhibited good cell membrane permeability.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Hayashi J,Samezawa Y,Ochi Y,Wada SI,Urata H

doi

10.1016/j.bmcl.2017.05.031

subject

Has Abstract

pub_date

2017-07-15 00:00:00

pages

3135-3138

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(17)30512-7

journal_volume

27

pub_type

杂志文章

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