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Grafting multi-maleimides on antisense oligonucleotide to enhance its cellular uptake and gene silencing capability

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Abstract

A multitude of maleimides are grafted onto the backbone of a phosphorothioate antisense oligonucleotide (ASO) to generate the construct of maleimide-grafted ASO (Mal-g-ASO). Through click conjugation with cell membrane thiols that triggers endocytosis-independent cellular internalization, Mal-g-ASO exhibited enhanced cellular uptake efficiency, resulting in a remarkable improvement of ASO-based gene silencing.

Graphical abstract: Grafting multi-maleimides on antisense oligonucleotide to enhance its cellular uptake and gene silencing capability

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Article information


Submitted
08 Apr 2020
Accepted
14 May 2020
First published
14 May 2020

Chem. Commun., 2020, Advance Article
Article type
Communication

Grafting multi-maleimides on antisense oligonucleotide to enhance its cellular uptake and gene silencing capability

Y. Guo, J. Zhang, G. Pan, C. H. J. Choi, P. Wang, Y. Li, X. Zhu and C. Zhang, Chem. Commun., 2020, Advance Article , DOI: 10.1039/D0CC02548H

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