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Title: Retro-1-oligonucleotide conjugates. Synthesis and biological evaluation
Author: Agramunt, Jordi
Pedroso Muller, Enrique
Kreda, Silvia M.
Juliano, Rudolph L.
Grandas Segarra, Anna
Keywords: Oligonucleòtids
Síntesi orgànica
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:
It is part of: Molecules, 2019, vol. 24, num. 3, p. 579
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ISSN: 1420-3049
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)

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