期刊
APPLIED SCIENCES-BASEL
卷 11, 期 3, 页码 -出版社
MDPI
DOI: 10.3390/app11031174
关键词
therapeutic nucleic acid; drug delivery; nanoparticles; cytotoxicity; macrophages; cellular uptake; small interfering RNA; multiple sclerosis; repulsive guidance molecule a
类别
资金
- Russian Science Foundation [19-74-30011]
- Russian Foundation for Basic Research [18-515-57006]
- Ministry of Science and Higher Education of the Russian Federation [FSUS-2020-0035]
- Japan Medical Research Foundation [2018JP002]
- Russian Science Foundation [19-74-30011] Funding Source: Russian Science Foundation
Novel lipid-conjugated DNA and RNA derivatives with low cytotoxicity and efficient cellular uptake without transfection agents were synthesized. Lipid-conjugated siRNAs targeting RGMa showed comparable gene silencing activity to unmodified control siRNA when delivered into cells via Lipofectamine-mediated transfection.
New lipid conjugates of DNA and RNA incorporating one to four [(4-dodecylphenyl)sulfonyl]phosphoramidate or (hexadecylsulfonyl)phosphoramidate groups at internucleotidic positions near the 3 ' or 5 '-end were synthesized and characterized. Low cytotoxicity of the conjugates and their ability to be taken up into cells without transfection agents were demonstrated. Lipid-conjugated siRNAs targeting repulsive guidance molecules a (RGMa) have shown a comparable gene silencing activity in PK-59 cells to unmodified control siRNA when delivered into the cells via Lipofectamine mediated transfection.
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