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

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• 作者：Daniel Zewge ; Francis Gosselin ; Denise M. Kenski ; Jenny Li ; Vasant Jadhav ; Yu Yuan ; Sandhya S. Nerurkar ; David M. Tellers ; W. Michael Flanagan ; Ian W. Davies
• 刊名：Bioconjugate Chemistry
• 出版年：2014
• 出版时间：December 17, 2014
• 年：2014
• 卷：25
• 期：12
• 页码：2222-2232
• 全文大小：831K
• ISSN：1520-4812

文摘

Chemical modification of siRNA is achieved in a high-throughput manner (96-well plate format) by copper catalyzed azide鈥揳lkyne 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.