化学
寡核苷酸
核酸
碱基
胍
核糖核酸
嘌呤
DNA
立体化学
组合化学
取代基
核酸结构
生物化学
酶
基因
作者
Naohiro Horie,Shinji Kumagai,Yutaro Kotobuki,Takao Yamaguchi,Satoshi Obika
摘要
An N-methylguanidine-bridged nucleic acid (GuNA[NMe]), a guanidine-bridged nucleic acid (GuNA) bearing a methyl substituent at the bridge, was successfully synthesised and incorporated into oligonucleotides. By employing an acetyl protecting group, GuNA[NMe]-modified oligonucleotides bearing acid-sensitive purine nucleobases were successfully prepared. The obtained GuNA[NMe]-modified oligonucleotides exhibit excellent binding affinity towards the complementary single-stranded RNA and DNA. Furthermore, even a single GuNA[NMe] modification provides robust enzymatic stability, similar to that achieved by the well-established phosphorothioate backbone modification. These data indicate that such a GuNA[NMe] represents a valuable modification for the development of therapeutic oligonucleotides.
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