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Bridged Nucleic Acids for Therapeutic Oligonucleotides

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Handbook of Chemical Biology of Nucleic Acids

Abstract

Recent developments in genetic technologies for genomic analysis, diagnostics, and therapeutics have revolutionary effects on medical science. Oligonucleotide (ON) molecules play an essential role in managing cellular genetic disorders because of their sequence-specific inhibitory effect on complementary RNAs. ONs with modified nucleosides exhibit higher enzymatic stability, duplex-forming ability, sequence selectivity, and in vivo pharmacokinetic profiles, which are extremely anticipated for ON therapeutics. We previously reported 2′-O,4′-C-methylene bridged nucleic acid/locked nucleic acid (2′,4′-BNA/LNA) with exceptionally high duplex-forming capability toward complementary sequences. In recent years, we have focused on developing further intensified bridged nucleic acids with high enzymatic resistance, sequence specificity, high in vivo efficacy, and low toxicity. Herein, we report numerous promising bridged nucleic acids that have been developed in our laboratory since the introduction of 2′,4′-BNA/LNA.

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Authors and Affiliations

  1. Graduate School of Pharmaceutical Sciences, Osaka University, Osaka, Japan

    Md Ariful Islam & Satoshi Obika

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  1. Md Ariful Islam
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  2. Satoshi Obika
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Correspondence to Satoshi Obika .

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  1. Frontier Institute for Biomolecular Engineering Research (FIBER), Konan University, Kobe, Japan

    Naoki Sugimoto

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  1. Rega Institute, KU Leuven University, Leuven, Belgium

    Piet Herdewijn

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Islam, M.A., Obika, S. (2023). Bridged Nucleic Acids for Therapeutic Oligonucleotides. In: Sugimoto, N. (eds) Handbook of Chemical Biology of Nucleic Acids. Springer, Singapore. https://doi.org/10.1007/978-981-19-9776-1_18

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