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

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

Bioconjugate chemistry (2014-11-15)
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
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Acetonitrile, suitable for HPLC, gradient grade, ≥99.9%
Sigma-Aldrich
Pyridine, ReagentPlus®, ≥99%
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Acetonitrile, anhydrous, 99.8%
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Acetonitrile, ACS reagent, ≥99.5%
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Acetonitrile, electronic grade, 99.999% trace metals basis
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Dichloromethane, anhydrous, ≥99.8%, contains 40-150 ppm amylene as stabilizer
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Dichloromethane, puriss. p.a., ACS reagent, reag. ISO, ≥99.9% (GC)
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Dichloromethane, analytical standard
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Dichloromethane, contains 40-150 ppm amylene as stabilizer, ACS reagent, ≥99.5%
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Acetonitrile, HPLC Plus, ≥99.9%
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Dichloromethane, Selectophore, ≥99.5%
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Acetonitrile, analytical standard
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Methylene Chloride, Pharmaceutical Secondary Standard; Certified Reference Material
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N,N-Dimethylacetamide, Ph. Eur.
USP
Methyl alcohol, United States Pharmacopeia (USP) Reference Standard
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Iodine, puriss., meets analytical specification of Ph. Eur., BP, USP, 99.8-100.5%
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Dichloromethane, biotech. grade, 99.9%, contains 40-150 ppm amylene as stabilizer
Supelco
Iodine, ReagentPlus®, ≥99.8% (titration)
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Pyridine, biotech. grade, ≥99.9%
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Acetonitrile, for preparative HPLC, ≥99.8% (GC)
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Acetic anhydride, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., ≥99% (GC)
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Imidazole buffer Solution, BioUltra, 1 M in H2O
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Iodine, ACS reagent, ≥99.8%, solid
Supelco
Pyridine, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Pyridine, analytical standard
Sigma-Aldrich
N,N-Dimethylacetamide, ReagentPlus®, ≥99%
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N,N-Dimethylacetamide, spectrophotometric grade, ≥99%
Supelco
N,N-Dimethylacetamide, analytical standard