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Retro-1-oligonucleotide conjugates. Synthesis and biological evaluation Agramunt, Jordi Pedroso Muller, Enrique Kreda, Silvia M. Juliano, Rudolph L. Grandas Sagarra, Anna Oligonucleòtids Síntesi orgànica Oligonucleotides Organic synthesis 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. 2019-02-12T11:32:24Z 2019-02-12T11:32:24Z 2019-02-06 2019-02-12T11:32:25Z info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion 1420-3049 https://hdl.handle.net/2445/128159 685350 30736307 eng Reproducció del document publicat a: https://doi.org/10.3390/molecules24030579 Molecules, 2019, vol. 24, num. 3, p. 579 https://doi.org/10.3390/molecules24030579 cc-by (c) Agramunt, Jordi et al., 2019 http://creativecommons.org/licenses/by/3.0/es info:eu-repo/semantics/openAccess 17 p. application/pdf MDPI Articles publicats en revistes (Química Inorgànica i Orgànica)