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http://hdl.handle.net/2445/128159
Title: | Retro-1-oligonucleotide conjugates. Synthesis and biological evaluation |
Author: | Agramunt, Jordi Pedroso Muller, Enrique Kreda, Silvia M. Juliano, Rudolph L. Grandas Sagarra, Anna |
Keywords: | Oligonucleòtids Síntesi orgànica Oligonucleotides Organic synthesis |
Issue Date: | 6-Feb-2019 |
Publisher: | MDPI |
Abstract: | Addition of small molecule Retro-1 has been described to enhance antisense and splice switching oligonucleotides. With the aim of assessing the effect of covalently linking Retro-1 to the biologically active oligonucleotide, three different derivatives of Retro-1 were prepared that incorporated a phosphoramidite group, a thiol or a 1,3-diene, respectively. Retro-1-oligonucleotide conjugates were assembled both on-resin (coupling of the phosphoramidite) and from reactions in solution (Michael-type thiol-maleimide reaction and Diels-Alder cycloaddition). Splice switching assays with the resulting conjugates showed that they were active but that they provided little advantage over the unconjugated oligonucleotide in the well-known HeLa Luc705 reporter system. |
Note: | Reproducció del document publicat a: https://doi.org/10.3390/molecules24030579 |
It is part of: | Molecules, 2019, vol. 24, num. 3, p. 579 |
URI: | http://hdl.handle.net/2445/128159 |
Related resource: | https://doi.org/10.3390/molecules24030579 |
ISSN: | 1420-3049 |
Appears in Collections: | Articles publicats en revistes (Química Inorgànica i Orgànica) |
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File | Description | Size | Format | |
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685350.pdf | 2.9 MB | Adobe PDF | View/Open |
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