Bioconjugate Chemistry 2014-12-17

High-throughput chemical modification of oligonucleotides for systematic structure-activity relationship evaluation.

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

文献索引：Bioconjug. Chem. 25(12) , 2222-32, (2014)

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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.

相关化合物

  • 2',3'-二脱氧胸苷
  • 咪唑
  • 乙腈
  • 甲醇
  • 氨基甲烷
  • 二氯甲烷
  • 乙酸酐
  • 水
  • 叠氮甲基苯基硫醚
  • 碘

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