High-Throughput Chemical Modification of Oligonucleotides for Systematic Structure-Activity Relationship Evaluation

被引：2

作者：

Zewge, Daniel ^{[1
]}

Gosselin, Francis ^{[1
]}

Kenski, Denise M. ^{[1
]}

Li, Jenny ^{[1
]}

Jadhav, Vasant ^{[1
]}

Yuan, Yu ^{[1
]}

Nerurkar, Sandhya S. ^{[1
]}

Tellers, David M. ^{[1
]}

Flanagan, W. Michael ^{[1
]}

Davies, Ian W. ^{[1
]}

机构：

[1] Merck Res Labs, Dept Proc Chem, Rahway, NJ 07065 USA

来源：

BIOCONJUGATE CHEMISTRY | 2014年 / 25卷 / 12期

关键词：

SMALL-INTERFERING RNA; IN-VITRO POTENCY; CLICK CHEMISTRY; BIOLOGICAL-ACTIVITY; SIRNA DELIVERY; SOLID-PHASE; ACID; STABILITY; IMMUNOSTIMULATION; CONJUGATION;

D O I：

10.1021/bc500453q

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Chemical modification of siRNA is achieved in a high-throughput manner (96-well plate format) by copper catalyzed azide-alkyne cycloadditions. This transformation can be performed in one synthetic operation at up to four positions with complete specificity, good yield, and acceptable purity. As demonstrated here, this approach extends the current synthetic options for oligonucleotide modifications and simultaneously facilitates the systematic, rapid biological evaluation of modified siRNA.

引用

页码：2222 / 2232

页数：11

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