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Oligonucleotides conjugated with short chemically defined polyethylene glycol chains are efficient antisense agents.

Shokrzadeh N, Winkler AM, Dirin M, Winkler J - Bioorg. Med. Chem. Lett. (2014)

Bottom Line: We examined the use of short PEG ligands on the in vitro effect of antisense agents.Circular dichroism showed that the tethering of PEG12-chains to phosphodiester and phosphorothioate oligonucleotides had no influence on their secondary structure and did not reduce the affinity to the counter strand.In an in vitro tumor model, a luciferase reporter assay indicated unchanged gene silencing activity compared to unmodified compounds, and even slightly superior target down regulation was found after treatment with a phosphorothioate modified conjugate.

View Article: PubMed Central - PubMed

Affiliation: University of Vienna, Department of Pharmaceutical Chemistry, Althanstraße 14, 1090 Vienna, Austria.

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CD spectra of PEGylated antisense oligonucleotide duplexes. The indicated oligonucleotides were mixed in an equimolar ratio with their counterstrand 6 in a tris buffer solution and subjected to circular dichroism analysis.
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f0005: CD spectra of PEGylated antisense oligonucleotide duplexes. The indicated oligonucleotides were mixed in an equimolar ratio with their counterstrand 6 in a tris buffer solution and subjected to circular dichroism analysis.

Mentions: Circular dichroism spectra were recorded to detect a possible influence of the ligands on the structural properties of the paired oligonucleotide duplexes. Neither 3′- nor 5′-attachment changed the curve shape (Fig. 1). The slightly higher band intensities even indicate a small stabilization of the duplex structure caused by the PEGylation. Similar results were found for the phosphorothioate oligonucleotides 4 and 5 (data not shown).


Oligonucleotides conjugated with short chemically defined polyethylene glycol chains are efficient antisense agents.

Shokrzadeh N, Winkler AM, Dirin M, Winkler J - Bioorg. Med. Chem. Lett. (2014)

CD spectra of PEGylated antisense oligonucleotide duplexes. The indicated oligonucleotides were mixed in an equimolar ratio with their counterstrand 6 in a tris buffer solution and subjected to circular dichroism analysis.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4263527&req=5

f0005: CD spectra of PEGylated antisense oligonucleotide duplexes. The indicated oligonucleotides were mixed in an equimolar ratio with their counterstrand 6 in a tris buffer solution and subjected to circular dichroism analysis.
Mentions: Circular dichroism spectra were recorded to detect a possible influence of the ligands on the structural properties of the paired oligonucleotide duplexes. Neither 3′- nor 5′-attachment changed the curve shape (Fig. 1). The slightly higher band intensities even indicate a small stabilization of the duplex structure caused by the PEGylation. Similar results were found for the phosphorothioate oligonucleotides 4 and 5 (data not shown).

Bottom Line: We examined the use of short PEG ligands on the in vitro effect of antisense agents.Circular dichroism showed that the tethering of PEG12-chains to phosphodiester and phosphorothioate oligonucleotides had no influence on their secondary structure and did not reduce the affinity to the counter strand.In an in vitro tumor model, a luciferase reporter assay indicated unchanged gene silencing activity compared to unmodified compounds, and even slightly superior target down regulation was found after treatment with a phosphorothioate modified conjugate.

View Article: PubMed Central - PubMed

Affiliation: University of Vienna, Department of Pharmaceutical Chemistry, Althanstraße 14, 1090 Vienna, Austria.

Show MeSH
Related in: MedlinePlus