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甲基膦酸酯锁核酸:一种具有甲基膦酸酯连接的锁核酸。

Methylphosphonate LNA: a locked nucleic acid with a methylphosphonate linkage.

作者信息

Lauritsen Anne, Dahl Britta M, Dahl Otto, Vester Birte, Wengel Jesper

机构信息

Department of Chemistry, University of Copenhagen, Universitetsparken 5, DK-2100 Copenhagen, Denmark.

出版信息

Bioorg Med Chem Lett. 2003 Jan 20;13(2):253-6. doi: 10.1016/s0960-894x(02)00882-x.

Abstract

Synthesis of an oligonucleotide containing one methylphosphonate locked nucleic acid (LNA) thymine monomer using the phosphoramidite approach is described. The binding affinity of this 9-mer methylphosphonate LNA towards complementary DNA and RNA oligonucleotides was increased compared to the reference DNA, but decreased compared to the reference LNA. In the 9-mer sequence context studied, introduction of a single methylphosphonate LNA monomer, contrary to a single LNA monomer, efficiently inhibits 3'-exonucleolytic degradation.

摘要

描述了使用亚磷酰胺方法合成包含一个甲基膦酸酯锁定核酸(LNA)胸腺嘧啶单体的寡核苷酸。与参考DNA相比,这种9聚体甲基膦酸酯LNA对互补DNA和RNA寡核苷酸的结合亲和力有所增加,但与参考LNA相比则有所降低。在所研究的9聚体序列背景下,与单个LNA单体相反,引入单个甲基膦酸酯LNA单体可有效抑制3'-核酸外切酶降解。

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