Antisense oligonucleotides modifications

Example 56 the Isis Pharmaceutical group in their extensive investigations of antisense oligonucleotides as therapeutics has described the synthesis of 3 -C-methylene nucleoside phosphonoamidites for the new backbone modification of oligonucleotides [90]. This paper gives good insight into tricoordinate phosphorus and related H-phosphonate chemistry in the service of nucleotide synthesis. 

Manoharan, M. 1999. 2 -Carbohydrate modifications in antisense oligonucleotide therapy importance of conformation, configuration and conjugation. Biochim. Biophys. Acta 1489 117-130. 

McKay, R.A. Cummins, L.L. Graham, M.J. Lesnik, E.A. Owens, S.R. Winniman, M. Dean, N.M. Enhanced activity of an antisense oligonucleotide targeting murine protein kinase C-alpha by the incorporation of 2 -0-propyl modifications. Nucleic. Adds. Res. 1996, 24 (3), 411-417. 

Sanghvi, Y S, Heterocyclic Base Modifications in Nucleic Acids and their Applications in Antisense Oligonucleotides, in Antisense Research und Applikations, S.T. Crooke, Lebleu, B., Editor. 1993, CRC Press Inc. Boca Raton FI. p. 273-288. 

Agrawal S (1999). Importance of nucleotide sequence and chemical modifications of antisense oligonucleotides. Biochim. Biophys. Acta. 1489 53-68. 

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