Physicochemical properties of phosphorothioate oligodeoxynucleotides.

Abstract:

:We have recently shown that phosphorothioate (PS) oligodeoxynucleotide (ODN) analogs, unlike their normal congeners, exhibit significant anti-HIV activity (Matsukura et al., (1987) Proc. Natl. Acad. Sci. USA 84, 7706-7710). We now report the syntheses, melting temperatures (Tm), and nuclease susceptibilities of a series of phosphorothioate ODN analogs. These include all-PS duplexes, duplexes with one normal chain and the other chain either all-PS, or end-capped with several PS groups at both 3' and 5' ends. The DNase susceptibilities of the S-ODNs are much less than the normal phosphodiesters, but by contrast duplexes of poly-rA with S-dT40 are much more susceptible to RNase H digestion. The Tm's for AT base pairs of S-ODNs are significantly depressed relative to normals, while GC base pairs show much less Tm depression. The Tm's of S-dT oligomers with poly-rA are reduced relative to the duplexes with normal dA oligomers. These results have significance for the biological properties of these analogs as anti-message inhibitors of gene expression, and provide a rational basis for the S-dC/G sequences as potential effective anti-AIDS agents.

journal_name

Nucleic Acids Res

journal_title

Nucleic acids research

authors

Stein CA,Subasinghe C,Shinozuka K,Cohen JS

doi

10.1093/nar/16.8.3209

subject

Has Abstract

pub_date

1988-04-25 00:00:00

pages

3209-21

issue

8

eissn

0305-1048

issn

1362-4962

journal_volume

16

pub_type

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