Abstract
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.
MeSH terms
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Alkynes / chemistry
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Azides / chemistry
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Catalysis
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Chromatography, High Pressure Liquid / methods
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Click Chemistry
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Copper / chemistry
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Cycloaddition Reaction
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Gene Knockdown Techniques
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HeLa Cells
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High-Throughput Screening Assays / methods*
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Humans
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Oligonucleotides / chemistry*
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Oligonucleotides / pharmacology*
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RNA, Small Interfering / chemistry
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RNA, Small Interfering / pharmacology
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Solid-Phase Synthesis Techniques
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Structure-Activity Relationship*
Substances
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Alkynes
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Azides
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Oligonucleotides
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RNA, Small Interfering
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Copper