Literature DB >> 26648391

Reductively Cleavable Nanocaplets for siRNA Delivery by Template-Assisted Oxidative Polymerization.

P K Hashim1, Kou Okuro1, Shigekazu Sasaki2, Yasutaka Hoashi2, Takuzo Aida1,3.   

Abstract

A series of water-soluble telechelic dithiol monomers bearing multiple guanidinium ion (Gu(+)) units in their main chains were synthesized for packaging siRNA by template-assisted oxidative polymerization at their thiol termini. In the presence of siRNA, oxidative polymerization of (TEG)Gu4 affords a uniform-sized (7 ± 2 nm) nanocaplet containing siRNA (P(TEG)Gu4⊃siRNA; P(TEG)Gu4 = polymerized (TEG)Gu4). When this small conjugate is incubated with live cells, cellular uptake occurs, and the nanocaplet undergoes depolymerization in the reductive cytosolic environment to liberate the packaged siRNA. Consequently, gene expression in the live cells is suppressed.

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Year:  2015        PMID: 26648391     DOI: 10.1021/jacs.5b08948

Source DB:  PubMed          Journal:  J Am Chem Soc        ISSN: 0002-7863            Impact factor:   15.419


  11 in total

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