Alteration of cross-linking selectivity with the 2′-OMe analogue of 2-amino-6-vinylpurine and evaluation of antisense effects

被引：24
|
作者：
Imoto, Shuhei [1 ]
Hori, Tsuneaki [1 ]
Hagihara, Shinya [1 ]
Taniguchi, Yosuke [2 ]
Sasaki, Shigeki [2 ,3 ]
Nagatsugi, Fumi [1 ,3 ]
机构：
[1] Tohoku Univ, Inst Multidisciplinary Res Adv Mat, Aoba Ku, Sendai, Miyagi 9808577, Japan
[2] Kyushu Univ, Grad Sch Pharmaceut Sci, Higashi Ku, Fukuoka 8128582, Japan
[3] Japan Sci & Technol Agcy, CREST, Kawaguchi, Saitama 3320012, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 20期
基金：
日本学术振兴会; 日本科学技术振兴机构;
关键词：
Oligonucleotide; Cross-linking; Antisense; DNA; Nucleic acids chemistry; MODIFIED OLIGONUCLEOTIDES; INHIBITION; DNA; ACTIVATION; EFFICIENT; MICRORNA; STRATEGY;
D O I：
10.1016/j.bmcl.2010.08.027
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We previously reported that oligodeoxynucleotides containing 2-amino-6-vinylpurine (2-AVP: 1) exhibit efficient selective cross-linking to cytosine. In this study, the 2'-OMe nucleoside analogue (2) of 2-AVP was designed in order to increase its affinity to RNA and enhance metabolic stability. It has been demonstrated that 2'-OMe oligonucleotides bearing 2 achieve highly selective cross-linking to the thymine base in DNA and show higher antisense effect on luciferase production in cell lysate. (C) 2010 Elsevier Ltd. All rights reserved.
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页码：6121 / 6124
页数：4
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