Title:
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Retro-1-oligonucleotide conjugates. Synthesis and biological evaluation
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Author:
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Agramunt, Jordi; Pedroso Muller, Enrique; Kreda, Silvia M.; Juliano, Rudolph L.; Grandas Segarra, Anna
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Other authors:
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Universitat de Barcelona |
Abstract:
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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. |
Subject(s):
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-Oligonucleòtids -Síntesi orgànica -Oligonucleotides -Organic synthesis |
Rights:
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cc-by (c) Agramunt, Jordi et al., 2019
http://creativecommons.org/licenses/by/3.0/es |
Document type:
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Article Article - Published version |
Published by:
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MDPI
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