| Literature DB >> 8423598 |
F Morvan1, H Porumb, G Degols, I Lefebvre, A Pompon, B S Sproat, B Rayner, C Malvy, B Lebleu, J L Imbach.
Abstract
12-Mer analogues, representative of seven different classes of structurally modified oligonucleotides and complementary to the same target, have been compared for their binding affinity for both single-stranded DNA and RNA, resistance to hydrolysis by nucleases in culture medium (RPMI 1640 + 10% inactivated fetal calf serum), and inhibition of HIV-1 replication in de novo infected MT4 T lymphocytes. The viral target was the splice acceptor site of the premessenger coding for the regulatory protein tat. The oligo(2'-O-alkyl)ribonucleotides (beta-2'O-allyl-RNA and beta-2'OMe-RNA) were shown to form the most stable hybrids with complementary RNA strands whereas the alpha-anomeric oligodeoxynucleoside phosphorothioate analogue displayed the highest stability in the culture medium. All the modified oligonucleotides examined in the present study exhibited a sequence-nonspecific inhibitory effect on HIV-1 replication, the phosphorothioate analogues being the most active ones (ED50 < 1 microM).Entities:
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Year: 1993 PMID： 8423598 DOI： 10.1021/jm00054a013
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446