以吡啶作为非天然核碱基的2',4'-双环核酸（BNA）衍生物的合成及三链体形成特性

Synthesis and triplex-forming properties of 2',4'-BNA derivatives bearing pyridines as an unnatural nucleobase.

作者信息

Matsugu Sachiko, Inohara Hiroyasu, Obika Satoshi, Imanishi Takeshi

机构信息

Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamadaoka, Suita, Osaka 565-0871, Japan.

出版信息

Nucleic Acids Symp Ser (Oxf). 2005(49):159-60. doi: 10.1093/nass/49.1.159.

DOI:10.1093/nass/49.1.159

PMID:17150682

Abstract

Triplex-forming oligonucleotide (TFO) could serve as a potential tool to regulate gene expression. However, stability of the triplex is relatively low, and the sequence of the target dsDNA is severely regulated. In an attempt to overcome these problems, we have designed and synthesized 2',4'-BNA monomers bearing a 6-aminopyridin-3-yl (aPy(B)) and pyridin-2-yl group (Py(B)) as a nucleobase. These monomers were successfully incorporated into natural TFOs, and the triplex-forming property of the modified TFOs was evaluated by UV melting experiments.

摘要

三链形成寡核苷酸（TFO）可作为调控基因表达的潜在工具。然而，三链体的稳定性相对较低，且靶双链DNA的序列受到严格限制。为了克服这些问题，我们设计并合成了带有6-氨基吡啶-3-基（aPy(B)）和吡啶-2-基（Py(B)）作为核碱基的2',4'-双环核酸单体。这些单体成功地掺入到天然TFO中，并通过紫外熔解实验评估了修饰后TFO的三链形成特性。