2021年9月
Synthesis of crosslinked 2 '-OMe RNA duplexes and their application for effective inhibition of miRNA function
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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- 巻
- 48
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- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.bmcl.2021.128257
- 出版者・発行元
- PERGAMON-ELSEVIER SCIENCE LTD
The interstrand crosslinking of nucleic acids is one of the strategies to create the stable complex between an oligonucleotide and RNA by covalent bond formation. We previously reported that fully 2'-O-methylated (2'-OMe) RNAs having the 2-amino-6-vinylpurine (AVP) exhibited an efficient crosslinking to uracil in the target RNA. In this study, we established a chemical method to efficiently synthesize the crosslinked 2'-OMe RNA duplexes using AVP and prepared the anti-miRNA oligonucleotides (AMOs) containing the antisense targeting miR-21 and crosslinked duplex at the terminal sequences. These AMOs showed a markedly higher anti miRNA activity than that of the commercially-available miR-21 inhibitor which has locked nucleic acid (LNA) residues.
- リンク情報
- ID情報
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- DOI : 10.1016/j.bmcl.2021.128257
- ISSN : 0960-894X
- eISSN : 1464-3405
- Web of Science ID : WOS:000684377000004