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Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/128159
Retro-1-oligonucleotide conjugates. Synthesis and biological evaluation
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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.
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AGRAMUNT, Jordi, et al. Retro-1-oligonucleotide conjugates. Synthesis and biological evaluation. Molecules. 2019. Vol. 24, num. 3, pags. 579. ISSN 1420-3049. [consulted: 27 of August of 2026]. Available at: https://hdl.handle.net/2445/128159