Total stepwise solid-phase synthesis of oligonucleotide-(3'-->N)-peptide conjugates |
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Authors: | Stetsenko Dmitry A Malakhov Andrey D Gait Michael J |
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Institution: | Medical Research Council, Laboratory of Molecular Biology, Cambridge CB2 2QH, UK. |
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Abstract: | structure: see text] An efficient total stepwise solid-phase synthesis of oligonucleotide-(3'-->N)-peptide conjugates is described that makes use of either a controlled pore glass support or macroporous polystyrene beads. Extending our previous homoserine linker approach, we prepared a range of conjugates containing one of four different cell or nuclear penetration peptides together with oligonucleotides containing 2'-deoxynucleoside or 2'-O-methylribonucleoside phosphodiesters, or gapmers containing 2'-deoxyphosphorothioates. The route also allows incorporation of a fluorescent label within the conjugate for cell uptake studies. |
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