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Synthesis and properties of triplex-forming oligonucleotides containing 2′-O-(2-methoxyethyl)-5-(3-aminoprop-1-ynyl)-uridine |
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| Authors: | Chenguang Lou Qiang Xiao Lavinia Brennan Mark E Light Nuria Vergara-Irigaray Elizabeth M Atkinson Lindy M Holden-Dye Keith R Fox Tom Brown |
| Institution: | 1. School of Chemistry, University of Southampton, Highfield, Southampton SO17 1BJ, UK;2. School of Biological Sciences, University of Southampton, Bassett Crescent East, Southampton SO16 7PX, UK |
| Abstract: | 2′-O-(2-Methoxyethyl)-5-(3-aminoprop-1-ynyl)-uridine phosphoramidite (MEPU) has been synthesized from d-ribose and 5-iodouracil and incorporated into triplex-forming oligonucleotides (TFOs) by automated solid-phase oligonucleotide synthesis. The TFOs gave very high triplex stability with their target duplexes as measured by ultraviolet/fluorescence melting and DNase I footprinting. The incorporation of MEPU into TFOs renders them resistant to degradation by serum nucleases. |
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