Novel lipid‐oligonucleotide conjugates containing long‐chain sulfonyl phosphoramidate groups: Synthesis and biological properties

Alina Derzhalova, Oleg Markov, Alesya Fokina, Yasuo Shiohama, Timofei Zatsepin, Masayuki Fujii, Marina Zenkova, Dmitry Stetsenko

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

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. Lipidconjugated 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.

Original languageEnglish
Article number1174
Pages (from-to)1-15
Number of pages15
JournalApplied Sciences (Switzerland)
Volume11
Issue number3
DOIs
Publication statusPublished - 1 Feb 2021

Keywords

  • Cellular uptake
  • Cytotoxicity
  • Drug delivery
  • Macrophages
  • Multiple sclerosis
  • Nanoparticles
  • Repulsive guidance molecule a
  • Small interfering RNA
  • Therapeutic nucleic acid

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