Research output: Contribution to journal › Article › peer-review
Novel lipid‐oligonucleotide conjugates containing long‐chain sulfonyl phosphoramidate groups: Synthesis and biological properties. / Derzhalova, Alina; Markov, Oleg; Fokina, Alesya et al.
In: Applied Sciences (Switzerland), Vol. 11, No. 3, 1174, 01.02.2021, p. 1-15.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - Novel lipid‐oligonucleotide conjugates containing long‐chain sulfonyl phosphoramidate groups: Synthesis and biological properties
AU - Derzhalova, Alina
AU - Markov, Oleg
AU - Fokina, Alesya
AU - Shiohama, Yasuo
AU - Zatsepin, Timofei
AU - Fujii, Masayuki
AU - Zenkova, Marina
AU - Stetsenko, Dmitry
N1 - Funding Information: Funding: This research was funded by Russian Science Foundation, grant No. 19‐74‐30011 (cyto‐ toxicity, confocal microscopy, flow cytometry, dynamic light scattering), Russian Foundation for Basic Research, grant No. 18‐515‐57006 (siRNA synthesis), the Ministry of Science and Higher Ed‐ ucation of the Russian Federation, project No. FSUS‐2020‐0035 to Novosibirsk State University (oligodeoxynucleotide synthesis), and Japan Medical Research Foundation, grant No. 2018JP002 (biological activity). Publisher Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland. Copyright: Copyright 2021 Elsevier B.V., All rights reserved.
PY - 2021/2/1
Y1 - 2021/2/1
N2 - 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.
AB - 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.
KW - Cellular uptake
KW - Cytotoxicity
KW - Drug delivery
KW - Macrophages
KW - Multiple sclerosis
KW - Nanoparticles
KW - Repulsive guidance molecule a
KW - Small interfering RNA
KW - Therapeutic nucleic acid
UR - http://www.scopus.com/inward/record.url?scp=85100114976&partnerID=8YFLogxK
U2 - 10.3390/app11031174
DO - 10.3390/app11031174
M3 - Article
AN - SCOPUS:85100114976
VL - 11
SP - 1
EP - 15
JO - Applied Sciences (Switzerland)
JF - Applied Sciences (Switzerland)
SN - 2076-3417
IS - 3
M1 - 1174
ER -
ID: 27707894