Template. Phosphorothioate oligonucleotides duplexes as inhibitors of HIV-1 reverse transcriptase

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 th...

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Veröffentlicht in:Biochemical and biophysical research communications 1992-08, Vol.186 (3), p.1249-1256
Hauptverfasser: Maury, Georges, alaoui, Abdelaziz El, Morvan, François, Muller, Barbara, Imbach, Jean-Louis, Goody, Roger S.
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container_end_page 1256
container_issue 3
container_start_page 1249
container_title Biochemical and biophysical research communications
container_volume 186
creator Maury, Georges
alaoui, Abdelaziz El
Morvan, François
Muller, Barbara
Imbach, Jean-Louis
Goody, Roger S.
description 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 affinitiy. 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 a-configuration. Of the analogs tested, only S(dC) 14 showed priming activity.
doi_str_mv 10.1016/S0006-291X(05)81540-2
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Phosphorothioate oligonucleotides duplexes as inhibitors of HIV-1 reverse transcriptase</title><source>MEDLINE</source><source>ScienceDirect Journals (5 years ago - present)</source><creator>Maury, Georges ; alaoui, Abdelaziz El ; Morvan, François ; Muller, Barbara ; Imbach, Jean-Louis ; Goody, Roger S.</creator><creatorcontrib>Maury, Georges ; alaoui, Abdelaziz El ; Morvan, François ; Muller, Barbara ; Imbach, Jean-Louis ; Goody, Roger S.</creatorcontrib><description>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 affinitiy. 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 a-configuration. 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Phosphorothioate oligonucleotides duplexes as inhibitors of HIV-1 reverse transcriptase</title><title>Biochemical and biophysical research communications</title><addtitle>Biochem Biophys Res Commun</addtitle><description>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 affinitiy. Phosphorothioate oligodeoxyribonucleotides had a much higher affinity than oligo(dC) 14 and it was increased on hybridization. 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Phosphorothioate oligonucleotides duplexes as inhibitors of HIV-1 reverse transcriptase</title><author>Maury, Georges ; alaoui, Abdelaziz El ; Morvan, François ; Muller, Barbara ; Imbach, Jean-Louis ; Goody, Roger S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c420t-89829fb2575dce663a63217a1373ad51170d180fe3e37891530c7690e6bc62873</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1992</creationdate><topic>AIDS/HIV</topic><topic>Analytical, structural and metabolic biochemistry</topic><topic>Antiviral Agents - pharmacology</topic><topic>Base Sequence</topic><topic>Biological and medical sciences</topic><topic>Enzymes and enzyme inhibitors</topic><topic>Fundamental and applied biological sciences. 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source MEDLINE; ScienceDirect Journals (5 years ago - present)
subjects AIDS/HIV
Analytical, structural and metabolic biochemistry
Antiviral Agents - pharmacology
Base Sequence
Biological and medical sciences
Enzymes and enzyme inhibitors
Fundamental and applied biological sciences. Psychology
HIV Reverse Transcriptase
human immunodeficiency virus 1
Kinetics
Molecular Sequence Data
Nucleic Acid Denaturation
Oligodeoxyribonucleotides - pharmacology
Polydeoxyribonucleotides - metabolism
Recombinant Proteins - antagonists & inhibitors
Reverse Transcriptase Inhibitors
Templates, Genetic
Thermodynamics
Thionucleotides
Transferases
title Template. Phosphorothioate oligonucleotides duplexes as inhibitors of HIV-1 reverse transcriptase
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