Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 6, Issue 2, Pages 117-122Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml500260j
Keywords
Short interfering RNAs; nucleic acid chemistry; oligonucleotides; gene expression; down regulation
Categories
Funding
- National Sciences and Engineering Research Council
- Canada Foundation for Innovation
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Short interfering RNAs (siRNAs) have tremendous potential as a new class of next-generation therapeutics; however, their progress is lagging due to issues related to stability, biodistribution, and cell-membrane permeability. To overcome these issues, there is widespread interest in chemically modifying siRNAs. In this study, siRNAs that contain a triazole-backbone unit with pyrimidine-modified hydrophobic substituents were synthesized and examined for their gene-silencing activity. In our study, we generated a library of siRNAs that target both a plasmid reporter system and modifications are well tolerated within the RNA interference pathway. In an endogenous gene target, bcl-2. Our results indicate that these unique addition, a cholesterol-modified triazole-linked siRNA targeting the exogenous target firefly luciferase was capable of gene silencing at levels greater than 80% in the absence of a carrier complex.
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