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|Title:||Retro-1-oligonucleotide conjugates. Synthesis and biological evaluation|
Pedroso Muller, Enrique
Kreda, Silvia M.
Juliano, Rudolph L.
Grandas Segarra, Anna
|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|
|Appears in Collections:||Articles publicats en revistes (Química Inorgànica i Orgànica)|
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