Retro-1-Oligonucleotide Conjugates. Synthesis and Biological Evaluation

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 Hockey Protective - Shin Pads - Senior 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 Panini Grills / Sandwich Presses 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.