Synthesis and Properties of 2’-O,4’-C-Spirocyclopropylene Bridged Nucleic Acid (scpBNA), an Analogue of 2’,4’-BNA/LNA Bearing a Cyclopropane Ring.
Synthesis and Properties of 2’-O,4’-C-Spirocyclopropylene Bridged Nucleic Acid (scpBNA), an Analogue of 2’,4’-BNA/LNA Bearing a Cyclopropane Ring.
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2-O,4-C-螺环丙烯桥核酸 (scpBNA) 的合成和性质，它是带有环丙烷环的 2,4-BNA/LNA 的类似物。
DOI：
10.1039/c5cc02024g
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发表时间：
2015
期刊：
影响因子：
--
通讯作者：
Obika S.
中科院分区：
文献类型：
--
作者：
Yamaguchi T.;Horiba M.;Obika S.
合成了2‘-O，4’-C-螺环丙烯桥联核酸(ScpBNA)，它是一种类似于2‘-O，4’-C-亚甲基桥联核酸(2‘，4’-BNA/LNA)，在6‘-位带有环丙烷环，并成功地掺入到寡核苷酸中。与相应的天然寡核苷酸和2‘，4’-BNA/LNA修饰的寡核苷酸相比，scpBNA修饰的寡核苷酸具有良好的与互补单链RNA形成双链的能力，并表现出更高的酶稳定性。我们的结果证明了scpBNA在反义技术等基因治疗方面的潜力。
2′-O,4′-C-Spirocyclopropylene bridged nucleic acid (scpBNA), an analogue of 2′-O,4′-C-methylene bridged nucleic acid (2′,4′-BNA/LNA) bearing a cyclopropane ring at the 6′-position, was synthesized and successfully incorporated into oligonucleotides. The scpBNA-modified oligonucleotides showed excellent duplex-forming ability with complementary single-stranded RNA and exhibited increased enzymatic stability as compared to the corresponding natural and 2′,4′-BNA/LNA-modified oligonucleotides. Our results demonstrate the potential of scpBNA for gene therapeutics, such as antisense technology.