The crystal structure of a 2′,4′-BNANC[N–Me]-modified antisense gapmer in complex with the target RNA

Jiro Kondo; Yusuke Nomura; Yukiko Kitahara; Satoshi Obika; Hidetaka Torigoe

doi:10.1039/C5CC08300A

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The crystal structure of a 2′,4′-BNA^NC[N–Me]-modified antisense gapmer in complex with the target RNA†

Jiro Kondo,*^a Yusuke Nomura,^bc Yukiko Kitahara,^a Satoshi Obika*^d and Hidetaka Torigoe*^b

Author affiliations

* Corresponding authors

^a Department of Materials and Life Sciences, Sophia University, 7-1 Kioi-cho, Chiyoda-ku, 102-8554 Tokyo, Japan
E-mail: j.kondo@sophia.ac.jp

^b Department of Applied Chemistry, Faculty of Science, Tokyo University of Science, 1-3 Kagurazaka, Shinjuku-ku, 162-8601 Tokyo, Japan
E-mail: htorigoe@rs.kagu.tus.ac.jp

^c Division of Medical Devices, National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, 158-8501 Tokyo, Japan

^d Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamadaoka, Suita, 565-0871 Osaka, Japan
E-mail: obika@phs.osaka-u.ac.jp

Abstract

It has been confirmed by our previous studies that a 2′,4′-BNA^NC[N–Me]-modified antisense gapmer displays high affinity and selectivity to the target RNA strand, promising mRNA inhibitory activity and excellent nuclease resistance. Herein, we have obtained a crystal structure that provides insights into these excellent antisense properties.

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Article information

DOI: https://doi.org/10.1039/C5CC08300A
Article type: Communication
Submitted: 06 Oct 2015
Accepted: 21 Dec 2015
First published: 21 Dec 2015

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Chem. Commun., 2016,52, 2354-2357

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The crystal structure of a 2′,4′-BNA^NC[N–Me]-modified antisense gapmer in complex with the target RNA

J. Kondo, Y. Nomura, Y. Kitahara, S. Obika and H. Torigoe, Chem. Commun., 2016, 52, 2354 DOI: 10.1039/C5CC08300A

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