Template. Phosphorothioate oligonucleotides duplexes as inhibitors of HIV-1 reverse transcriptase.
Identifieur interne : 000222 ( Ncbi/Checkpoint ); précédent : 000221; suivant : 000223Template. Phosphorothioate oligonucleotides duplexes as inhibitors of HIV-1 reverse transcriptase.
Auteurs : G. Maury [France] ; A. El Alaoui ; F. Morvan ; B. Müller ; J L Imbach ; R S GoodySource :
- Biochemical and biophysical research communications [ 0006-291X ] ; 1992.
Descripteurs français
- KwdFr :
- Antiviraux (pharmacologie), Cinétique, Données de séquences moléculaires, Dénaturation d'acide nucléique, Inhibiteurs de la transcriptase inverse, Matrices (génétique), Oligodésoxyribonucléotides (pharmacologie), Polydésoxyribonucléotides (métabolisme), Protéines recombinantes (antagonistes et inhibiteurs), Séquence nucléotidique, Thermodynamique, Thionucléotides, Transcriptase inverse du VIH.
- MESH :
- antagonistes et inhibiteurs : Protéines recombinantes.
- métabolisme : Polydésoxyribonucléotides.
- pharmacologie : Antiviraux, Oligodésoxyribonucléotides.
- Cinétique, Données de séquences moléculaires, Dénaturation d'acide nucléique, Inhibiteurs de la transcriptase inverse, Matrices (génétique), Séquence nucléotidique, Thermodynamique, Thionucléotides, Transcriptase inverse du VIH.
English descriptors
- KwdEn :
- Antiviral Agents (pharmacology), Base Sequence, HIV Reverse Transcriptase, Kinetics, Molecular Sequence Data, Nucleic Acid Denaturation, Oligodeoxyribonucleotides (pharmacology), Polydeoxyribonucleotides (metabolism), Recombinant Proteins (antagonists & inhibitors), Reverse Transcriptase Inhibitors, Templates, Genetic, Thermodynamics, Thionucleotides.
- MESH :
- chemical , antagonists & inhibitors : Recombinant Proteins.
- chemical , metabolism : Polydeoxyribonucleotides.
- chemical , pharmacology : Antiviral Agents, Oligodeoxyribonucleotides.
- Base Sequence, HIV Reverse Transcriptase, Kinetics, Molecular Sequence Data, Nucleic Acid Denaturation, Reverse Transcriptase Inhibitors, Templates, Genetic, Thermodynamics, Thionucleotides.
Abstract
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.
DOI: 10.1016/s0006-291x(05)81540-2
PubMed: 1380799
Affiliations:
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pubmed:1380799Le document en format XML
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<series><title level="j">Biochemical and biophysical research communications</title>
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<term>Base Sequence</term>
<term>HIV Reverse Transcriptase</term>
<term>Kinetics</term>
<term>Molecular Sequence Data</term>
<term>Nucleic Acid Denaturation</term>
<term>Oligodeoxyribonucleotides (pharmacology)</term>
<term>Polydeoxyribonucleotides (metabolism)</term>
<term>Recombinant Proteins (antagonists & inhibitors)</term>
<term>Reverse Transcriptase Inhibitors</term>
<term>Templates, Genetic</term>
<term>Thermodynamics</term>
<term>Thionucleotides</term>
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<keywords scheme="KwdFr" xml:lang="fr"><term>Antiviraux (pharmacologie)</term>
<term>Cinétique</term>
<term>Données de séquences moléculaires</term>
<term>Dénaturation d'acide nucléique</term>
<term>Inhibiteurs de la transcriptase inverse</term>
<term>Matrices (génétique)</term>
<term>Oligodésoxyribonucléotides (pharmacologie)</term>
<term>Polydésoxyribonucléotides (métabolisme)</term>
<term>Protéines recombinantes (antagonistes et inhibiteurs)</term>
<term>Séquence nucléotidique</term>
<term>Thermodynamique</term>
<term>Thionucléotides</term>
<term>Transcriptase inverse du VIH</term>
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<keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Recombinant Proteins</term>
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<keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Polydeoxyribonucleotides</term>
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<term>Oligodeoxyribonucleotides</term>
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<keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Polydésoxyribonucléotides</term>
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<keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term>
<term>Oligodésoxyribonucléotides</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Base Sequence</term>
<term>HIV Reverse Transcriptase</term>
<term>Kinetics</term>
<term>Molecular Sequence Data</term>
<term>Nucleic Acid Denaturation</term>
<term>Reverse Transcriptase Inhibitors</term>
<term>Templates, Genetic</term>
<term>Thermodynamics</term>
<term>Thionucleotides</term>
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<keywords scheme="MESH" xml:lang="fr"><term>Cinétique</term>
<term>Données de séquences moléculaires</term>
<term>Dénaturation d'acide nucléique</term>
<term>Inhibiteurs de la transcriptase inverse</term>
<term>Matrices (génétique)</term>
<term>Séquence nucléotidique</term>
<term>Thermodynamique</term>
<term>Thionucléotides</term>
<term>Transcriptase inverse du VIH</term>
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<front><div type="abstract" xml:lang="en">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.</div>
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