Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1355252 | Bioorganic Chemistry | 2010 | 6 Pages |
Three different modified phosphoramidite nucleoside building blocks equipped with additional protected imidazole, masked alcohol and masked carboxylate functionality are synthesized and incorporated into oligonucleotides. Based on the serine-protease active site model, doubly and triply modified duplexes are created and tested for stability. Analysis of different spatial distributions of the extra functionalities shows that careful positioning can even overcome duplex destabilisation caused by the introduction of mismatches.
Graphical abstractBased on the serine-protease active site model, doubly and triply modified duplexes have been synthesized and tested for stability, considering different spatial distributions of functionalities.Figure optionsDownload full-size imageDownload as PowerPoint slide