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Amides as Substitute for the Phosphodiester Linkage in Antisense Oligonucleotides
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1993
Year
Bioorganic ChemistryMolecular BiologyNucleic Acid BiomarkersNucleic Acid ChemistryNatural Phosphodiester LinkageAntisense TherapyBiochemistryBioconjugationOligonucleotideNon-peptide LigandSolution Nmr SpectroscopyPhosphodiester LinkageStructural BiologyNew DimerNatural SciencesNucleic Acid BiochemistryMolecular BiophysicsThymidine DimerMedicineDrug Discovery
The synthesis of a thymidine dimer in which the natural phosphodiester linkage has been replaced by an amide (3′-CH2-CH2-NH-CO-4′) is described. This new dimer was incorporated into oligonucleotides. Measurement of melting temperatures (Tm) of DNA/RNA duplexes and the nuclease resistance are presented. Preliminary results of molecular mechanics are included.