2′/3′/5′-(R/S)-serinyl functionalized oligonucleotides
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United States of America Patent
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Mar 20, 2018
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May 2, 2014
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May 3, 2013
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Abstract
The present invention provides novel chiral serinyl functionalized tethered oligunucleotides i.e. R/S serinyl functionalized tethered oligonucleotides and the process of preparation thereof. Specifically, the present invention provides a modified nucleoside unit containing the R/S serinyl derivative at 2′ of the sugar unit which is introduced in a nucleotide sequence. Also, capping of the oligonucleotides with abasic serinyl derivative to render the nuclease stability to the oligonucleotiedds is also disclosed. The chiral serinyl functionalized tethered oligonucleotides, 2′-O-[R/S-(2-amino-3-methoxy)propyl] nucleic acids with both ′3- and 5′-ends capped with two units of abasic serine have antisense activity against the miRNA.
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