6533b831fe1ef96bd1298dc8

RESEARCH PRODUCT

Chemical Synthesis of 2′-O-Alkylated siRNAs

Romualdas SmiciusJens HaasJoachim W. EngelsDalibor Odadzic

subject

chemistry.chemical_classificationSmall interfering RNADownregulation and upregulationchemistryRNANucleotideAlkylationCombinatorial chemistryChemical synthesisAlkyl

description

Chemical synthesis has been a major endeavor to create active siRNAs. The downregulation of mRNA by 21-mer double-stranded siRNAs can be improved by using modified nucleotides, especially 2'-O-alkylated ones. Besides the commercially available 2 cent-O-methyl ribosides, 2'-alkyl groups bearing positive charges are especially promising candidates. We have shown that in a proper formulation they are superior to unmodified siRNAs. This may be due to enhanced stability and most probably to a better uptake into the cells.

https://doi.org/10.1007/978-1-60761-588-0_10