Formation of Oligonucleotide Triplexes with Selectively Modified Cytosines

The present invention is based on the finding that it is possible to use the bisulfite-catalyzed transamination reaction to selectively introduce aminoalkyl or carboxyalkyl linker arms at a specific deoxycytidine site within oligonucleotides or analogs thereof which also contain one or more 5-methyldeoxycytidine residues. This enables the provision of oligonucleotides and analogs thereof which contain a single amine or carboxylic acid functionality at a desired deoxycytidine site, which can serve as a linker arm for further selective attachment of a variety of functional groups. The resulting linker arm-conjugated oligomers are capable of forming stable duplexes with complementary single-stranded oligodeoxyribonucleotides as well as triple-stranded structures with target oligodeoxyribonucleotides duplexes. Description (Set) Proposed Use (Set) The invention also contemplates such oligonucleotides wherein the single cytidine residue is transaminated to include an aminoalkyl or carboxyalkyl group with or without one or more further functional groups attached

Patent (Set) 5,407,801

Patents:
US 5,407,801

Inventor(s): Miller, Paul

Type of Offer: Licensing



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