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

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Novel lipid‐oligonucleotide conjugates containing long‐chain sulfonyl phosphoramidate groups: Synthesis and biological properties. / Derzhalova, Alina; Markov, Oleg; Fokina, Alesya и др.

в: Applied Sciences (Switzerland), Том 11, № 3, 1174, 01.02.2021, стр. 1-15.

Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование

BibTeX

@article{a34aefa0cc2d408c8afc481911fa60f9,

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

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.",

keywords = "Cellular uptake, Cytotoxicity, Drug delivery, Macrophages, Multiple sclerosis, Nanoparticles, Repulsive guidance molecule a, Small interfering RNA, Therapeutic nucleic acid",

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

note = "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: {\textcopyright} 2021 by the authors. Licensee MDPI, Basel, Switzerland. Copyright: Copyright 2021 Elsevier B.V., All rights reserved.",

year = "2021",

month = feb,

day = "1",

doi = "10.3390/app11031174",

language = "English",

volume = "11",

pages = "1--15",

journal = "Applied Sciences (Switzerland)",

issn = "2076-3417",

publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",

number = "3",

}

RIS

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