Oligonucleosides: synthesis of a novel methylhydroxylamine-linked nucleoside dimer and its incorporation into antisense sequences

Oligonucleosides: synthesis of a novel methylhydroxylamine-linked nucleoside dimer and its incorporation into antisense sequences
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寡核苷:新型甲基羟胺连接的核苷二聚体的合成及其并入反义序列

DOI:
10.1021/ja00036a076
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发表时间:
1992
影响因子:
15
通讯作者:
P. Cook
P. Cook
中科院分区:
化学1区
文献类型:
--
作者:
J. Vasseur;F. Debart;Y. Sanghvi;P. Cook

文献摘要

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Modulation of gene expressionby antisense technologies requires the development of modified oligonucleotides possessing enhanced cellular uptake, resistance toward degradation by nucleases, and appropriate hybridization to target RNAs. 1 These oligonucleotide pharmacokinetic design features are amenable tostructure-activity relationship (SAR) studies and lead toantisense oligonucleotides modified in the heterocycle, sugar, phosphodiester linkage, and phosphorus atom. 1 Our research in this area has focused on the development of neutral or positively charged, achiral linkages between the 3'-carbon and the 4'-carbon of the sugars of an oligonucleoside. 2 Linkages of this type would circumvent the