Synthesis of peptide nucleic acids (PNA) with a crosslinking agent to RNA and effective inhibition of dicer

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• 作者：Takuya Akisawa ; Ken Yamada ; Fumi Nagatsugi ; ^{nagatugi@tagen.tohoku.ac.jp}
• 关键词：Crosslink ; Peptide nucleic acid ; miRNA ; Dicer ; Invasion
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 December 2016
• 年：2016
• 卷：26
• 期：24
• 页码：5902-5906
• 全文大小：1053 K
• 卷排序：26

文摘

Peptide nucleic acids (PNAs) are structural mimics of nucleic acids that form stable hybrids with DNA and RNA. Due to these characteristics, PNAs are widely used as biochemical tools, for example, in antisense/antigene therapy. In this study, we have synthesized PNAs incorporating 2-amino-6-vinylpurine (AVP) for the covalent targeting of single-stranded DNA and RNA, and evaluated their reactivities for these targets. PNA containing AVP at the N-terminal position showed a high reactivity to uracil in RNA and thymine in DNA at the complementary site with AVP. In addition, the crosslinking reactions to pre-miR122 with PNA containing AVP increased the inhibition effect for the Dicer processing of pre-miR122 in vitro.