rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
9
|
pubmed:dateCreated |
2010-9-15
|
pubmed:abstractText |
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.
|
pubmed:grant |
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Sep
|
pubmed:issn |
1520-4812
|
pubmed:author |
|
pubmed:issnType |
Electronic
|
pubmed:day |
15
|
pubmed:volume |
21
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1581-7
|
pubmed:dateRevised |
2010-12-31
|
pubmed:meshHeading |
pubmed-meshheading:20722369-Amines,
pubmed-meshheading:20722369-Cations,
pubmed-meshheading:20722369-Cholesterol,
pubmed-meshheading:20722369-Drug Delivery Systems,
pubmed-meshheading:20722369-Drug Design,
pubmed-meshheading:20722369-Lipids,
pubmed-meshheading:20722369-Microwaves,
pubmed-meshheading:20722369-RNA, Double-Stranded,
pubmed-meshheading:20722369-RNA, Messenger,
pubmed-meshheading:20722369-RNA, Small Interfering,
pubmed-meshheading:20722369-RNA Interference
|
pubmed:year |
2010
|
pubmed:articleTitle |
Design and assembly of new nonviral RNAi delivery agents by microwave-assisted quaternization (MAQ) of tertiary amines.
|
pubmed:affiliation |
Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, Worcester, Massachusetts 01605, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
|