| Literature DB >> 20722369 |
Animesh Ghosh1, Koushik Mukherjee, Xinpeng Jiang, Ying Zhou, Joshua McCarroll, James Qu, Pamela M Swain, Huricha Baigude, Tariq M Rana.
Abstract
RNA interference (RNAi) is a gene-silencing phenomenon whereby double-stranded RNA (dsRNA) triggers the sequence-specific degradation of homologous mRNA. RNAi has been quickly and widely applied to discover gene functions and holds great potential to provide a new class of therapeutic agents. However, new chemistry and delivery approaches are greatly needed to silence disease-causing genes without toxic effects. We reasoned that conjugation of the cholesterol moiety to cationic lipids would enhance RNAi efficiencies and lower the toxic effects of lipid-mediated RNAi delivery. Here, we report the first design and synthesis of new cholesterol-conjugated cationic lipids for RNAi delivery using microwave-assisted quaternization (MAQ) of tertiary amines. This strategy can be employed to develop new classes of nonviral gene delivery agents under safe and fast reaction conditions.Entities:
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Year: 2010 PMID: 20722369 PMCID: PMC3012264 DOI: 10.1021/bc900482r
Source DB: PubMed Journal: Bioconjug Chem ISSN: 1043-1802 Impact factor: 4.774