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    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.


    Yuanyuan Guo, Jiao Zhang, Gaifang Pan, Chung Hang Jonathan Choi, Ping Wang, Yuehua Li, Xinyuan Zhu, Chuan Zhang. Grafting multi-maleimides on antisense oligonucleotide to enhance its cellular uptake and gene silencing capability. Chemical communications (Cambridge, England). 2020 Jul 11;56(54):7439-7442

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    PMID: 32494799

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