Synthesis, biophysical properties, and stability studies of mixed backbone oligonucleotides containing segments of methylphosphotriester internucleotidic linkages

被引:12
作者
Iyer, RP
Yu, D
Jiang, ZW
Agrawal, S
机构
[1] Hybridon Inc., Worcester, MA 01605, One Innovation Drive
关键词
D O I
10.1016/0040-4020(96)00875-7
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The synthesis of mixed-backbone-oligonucleotides (MBOs) (15 to 25-mers) which contain phosphoric diester (PO) or phosphorothioate (PS) backbones along with segments of internucleotidic O-methylphosphate (POOMe) or O-methylphosphorothioate (PSOMe) linkages have been accomplished using N-pent-4-enoyl (PNT) nucleoside phosphoramidite synthons. The T(m)s of the MBOs reveal that they form stable duplexes with complementary DNA and RNA. The MBOs also showed increased resistance to degradation by nucleases. Consequently, the MBOs with methylphosphotriester segments represent a novel class of antisense oligonucleotides with potential for therapeutic and diagnostic applications. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:14419 / 14436
页数:18
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