The adamantane-derived bananins are potent inhibitors of the helicase activities and replication of SARS coronavirus.
Identifieur interne : 000E66 ( Ncbi/Curation ); précédent : 000E65; suivant : 000E67The adamantane-derived bananins are potent inhibitors of the helicase activities and replication of SARS coronavirus.
Auteurs : Julian A. Tanner [République populaire de Chine] ; Bo-Jian Zheng ; Jie Zhou ; Rory M. Watt ; Jie-Qing Jiang ; Kin-Ling Wong ; Yong-Ping Lin ; Lin-Yu Lu ; Ming-Liang He ; Hsiang-Fu Kung ; Andreas J. Kesel ; Jian-Dong HuangSource :
- Chemistry & biology [ 1074-5521 ] ; 2005.
Descripteurs français
- KwdFr :
- Adamantane (), Adamantane (analogues et dérivés), Adamantane (pharmacologie), Animaux, Antienzymes (), Antienzymes (pharmacologie), Antiviraux (), Antiviraux (pharmacologie), Cellules cultivées, Helicase (antagonistes et inhibiteurs), Helicase (métabolisme), Macaca mulatta, Pyridines (), Pyridines (pharmacologie), Relation dose-effet des médicaments, Réplication virale (), Réplication virale (physiologie), Virus du SRAS (), Virus du SRAS (enzymologie), Virus du SRAS (physiologie).
- MESH :
- analogues et dérivés : Adamantane.
- antagonistes et inhibiteurs : Helicase.
- enzymologie : Virus du SRAS.
- métabolisme : Helicase.
- pharmacologie : Adamantane, Antienzymes, Antiviraux, Pyridines.
- physiologie : Réplication virale, Virus du SRAS.
- Adamantane, Animaux, Antienzymes, Antiviraux, Cellules cultivées, Macaca mulatta, Pyridines, Relation dose-effet des médicaments, Réplication virale, Virus du SRAS.
English descriptors
- KwdEn :
- Adamantane (analogs & derivatives), Adamantane (chemistry), Adamantane (pharmacology), Animals, Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Cells, Cultured, DNA Helicases (antagonists & inhibitors), DNA Helicases (metabolism), Dose-Response Relationship, Drug, Enzyme Inhibitors (chemistry), Enzyme Inhibitors (pharmacology), Macaca mulatta, Pyridines (chemistry), Pyridines (pharmacology), SARS Virus (drug effects), SARS Virus (enzymology), SARS Virus (physiology), Virus Replication (drug effects), Virus Replication (physiology).
- MESH :
- chemical , analogs & derivatives : Adamantane.
- chemical , antagonists & inhibitors : DNA Helicases.
- chemical , chemistry : Adamantane, Antiviral Agents, Enzyme Inhibitors, Pyridines.
- chemical , metabolism : DNA Helicases.
- chemical , pharmacology : Adamantane, Antiviral Agents, Enzyme Inhibitors, Pyridines.
- drug effects : SARS Virus, Virus Replication.
- enzymology : SARS Virus.
- physiology : SARS Virus, Virus Replication.
- Animals, Cells, Cultured, Dose-Response Relationship, Drug, Macaca mulatta.
Abstract
Bananins are a class of antiviral compounds with a unique structural signature incorporating a trioxa-adamantane moiety covalently bound to a pyridoxal derivative. Six members of this class of compounds: bananin, iodobananin, vanillinbananin, ansabananin, eubananin, and adeninobananin were synthesized and tested as inhibitors of the SARS Coronavirus (SCV) helicase. Bananin, iodobananin, vanillinbananin, and eubananin were effective inhibitors of the ATPase activity of the SCV helicase with IC50 values in the range 0.5-3 microM. A similar trend, though at slightly higher inhibitor concentrations, was observed for inhibition of the helicase activities, using a FRET-based fluorescent assay. In a cell culture system of SCV, bananin exhibited an EC50 of less than 10 microM and a CC50 of over 300 microM. Kinetics of inhibition are consistent with bananin inhibiting an intracellular process or processes involved in SCV replication.
DOI: 10.1016/j.chembiol.2005.01.006
PubMed: 15797214
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pubmed:15797214Le document en format XML
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<term>Adamantane (pharmacology)</term>
<term>Animals</term>
<term>Antiviral Agents (chemistry)</term>
<term>Antiviral Agents (pharmacology)</term>
<term>Cells, Cultured</term>
<term>DNA Helicases (antagonists & inhibitors)</term>
<term>DNA Helicases (metabolism)</term>
<term>Dose-Response Relationship, Drug</term>
<term>Enzyme Inhibitors (chemistry)</term>
<term>Enzyme Inhibitors (pharmacology)</term>
<term>Macaca mulatta</term>
<term>Pyridines (chemistry)</term>
<term>Pyridines (pharmacology)</term>
<term>SARS Virus (drug effects)</term>
<term>SARS Virus (enzymology)</term>
<term>SARS Virus (physiology)</term>
<term>Virus Replication (drug effects)</term>
<term>Virus Replication (physiology)</term>
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<term>Adamantane (analogues et dérivés)</term>
<term>Adamantane (pharmacologie)</term>
<term>Animaux</term>
<term>Antienzymes ()</term>
<term>Antienzymes (pharmacologie)</term>
<term>Antiviraux ()</term>
<term>Antiviraux (pharmacologie)</term>
<term>Cellules cultivées</term>
<term>Helicase (antagonistes et inhibiteurs)</term>
<term>Helicase (métabolisme)</term>
<term>Macaca mulatta</term>
<term>Pyridines ()</term>
<term>Pyridines (pharmacologie)</term>
<term>Relation dose-effet des médicaments</term>
<term>Réplication virale ()</term>
<term>Réplication virale (physiologie)</term>
<term>Virus du SRAS ()</term>
<term>Virus du SRAS (enzymologie)</term>
<term>Virus du SRAS (physiologie)</term>
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<front><div type="abstract" xml:lang="en">Bananins are a class of antiviral compounds with a unique structural signature incorporating a trioxa-adamantane moiety covalently bound to a pyridoxal derivative. Six members of this class of compounds: bananin, iodobananin, vanillinbananin, ansabananin, eubananin, and adeninobananin were synthesized and tested as inhibitors of the SARS Coronavirus (SCV) helicase. Bananin, iodobananin, vanillinbananin, and eubananin were effective inhibitors of the ATPase activity of the SCV helicase with IC50 values in the range 0.5-3 microM. A similar trend, though at slightly higher inhibitor concentrations, was observed for inhibition of the helicase activities, using a FRET-based fluorescent assay. In a cell culture system of SCV, bananin exhibited an EC50 of less than 10 microM and a CC50 of over 300 microM. Kinetics of inhibition are consistent with bananin inhibiting an intracellular process or processes involved in SCV replication.</div>
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