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NLM AIDSLINE
Template. Phosphorothioate oligonucleotides duplexes as inhibitors of HIV-1 reverse transcriptase.
Maury G; el Alaoui A; Morvan F; Muller B; Imbach JL; Goody RS;
November 30, 1992
Biochem Biophys Res Commun. 1992 Aug 14;186(3):1249-56. Unique

We have investigated the interaction between a number of 14 mers phosphorothioate oligonucleotides and HIV-1 reverse transcriptase. Two methods were used to measure the affinity of the analogs for the enzyme. In the first, the oligonucleotide or its duplex with Poly(rl) were used as inhibitors of the enzyme using Poly(rA).(dT)14 as template primer. In the second, the oligonucleotides or their duplexes were used to displace a fluorescent template primer complex of known affinity from its binding site on reverse transcriptase. The two methods gave the same relative order of affinity. Phosphorothioate oligodeoxyribonucleotides had a much higher affinity than oligo(dC)14 and it was increased on hybridization. Quantitatively similar results were obtained for S(dC)14 or its analog with bases in the alpha-configuration. Of the analogs tested, only S(dC)14 showed priming activity.

Antiviral Agents/*PHARMACOLOGY Base Sequence Kinetics Molecular Sequence Data Nucleic Acid Denaturation Oligodeoxyribonucleotides/*PHARMACOLOGY Polydeoxyribonucleotides/METABOLISM Recombinant Proteins/ANTAGONISTS & INHIB RNA-Directed DNA Polymerase/*ANTAGONISTS & INHIB Support, Non-U.S. Gov't Templates Thermodynamics Thionucleotides JOURNAL ARTICLE

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