S. Agrawal et al., MIXED-BACKBONE OLIGONUCLEOTIDES CONTAINING PHOSPHOROTHIOATE AND METHYLPHOSPHONATE LINKAGES AS 2ND-GENERATION ANTISENSE OLIGONUCLEOTIDE, Nucleosides & nucleotides, 16(7-9), 1997, pp. 927-936
Antisense oligonucleotides are being studied as novel therapeutic agen
ts. To further improve the properties of antisense oligonucleotides, w
e have synthesized phosphorothioate oligonucleotides containing methyl
phosphonate linkages at the 5'-end, the 3'-end, or in the center, and
have evaluated the impact of these linkages on the biophysical propert
ies, biological properties, and some of the safety parameters.