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- Title
Novel Lipid-Oligonucleotide Conjugates Containing Long-Chain Sulfonyl Phosphoramidate Groups: Synthesis and Biological Properties.
- Authors
Derzhalova, Alina; Markov, Oleg; Fokina, Alesya; Shiohama, Yasuo; Zatsepin, Timofei; Fujii, Masayuki; Zenkova, Marina; Stetsenko, Dmitry; Endoh, Tamaki; Rozners, Eriks; Ohtsuki, Takashi
- Abstract
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.
- Subjects
BIOSYNTHESIS; SULFONYL group; SULFONYL compounds; GENE silencing; SMALL interfering RNA; NUCLEIC acids
- Publication
Applied Sciences (2076-3417), 2021, Vol 11, Issue 3, p1174
- ISSN
2076-3417
- Publication type
Article
- DOI
10.3390/app11031174