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

Alteration of cross-linking selectivity with the 2′-OMe analogue of 2-amino-6-vinylpurine and evaluation of antisense effects
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DOI:
10.1016/j.bmcl.2010.08.027
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发表时间:
2010-10-15
影响因子:
2.7
通讯作者:
Nagatsugi, Fumi
Nagatsugi, Fumi
中科院分区:
医学4区
文献类型:
--
作者:
Imoto, Shuhei;Hori, Tsuneaki;Nagatsugi, Fumi

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我们以前报道过,含有2-氨基-6-乙烯基嘌呤(2-AVP:1)的寡脱氧核苷酸表现出有效的选择性交联胞嘧啶。在本研究中,设计了2-AVP的2 '-OMe核苷类似物(2),以增加其与RNA的亲和力并增强代谢稳定性。已经证明,带有2的2 '-OMe寡核苷酸实现了与DNA中的胸腺嘧啶碱基的高度选择性交联,并且对细胞裂解物中的荧光素酶产生显示出更高的反义作用。(C)2010爱思唯尔有限公司版权所有。
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.