Enhanced Biological Activity of Antisense Oligonucleotides Containing 5-(1-Hexynyl)-substituted Pyrimidine Nucleotides |
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| Authors: | E Uhlmann L Homung S Hein S Augustin A Peyman D W Will |
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| Institution: | Hoechst Marion Roussel , G 838, D-65926, Frankfurt, Germany |
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| Abstract: | Abstract Antisense oligonucleotides directed against HSV- 1 immediate early gene mRNA were synthesized with replacement of the internal pyrimidine nucleotides by the corresponding 5-(l-hexynyl) analogues and with end-capping by phosphorothioates. These compounds were found to have improved binding affinity, increased stability towards nucleases and enhanced antiviral activity in a cell culture assay. |
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