Serveur d'exploration SRAS

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The adamantane-derived bananins are potent inhibitors of the helicase activities and replication of SARS coronavirus.

Identifieur interne : 000E66 ( Ncbi/Merge ); précédent : 000E65; suivant : 000E67

The 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 Huang

Source :

RBID : pubmed:15797214

Descripteurs français

English descriptors

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:15797214

Le document en format XML

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<term>Antiviral Agents (chemistry)</term>
<term>Antiviral Agents (pharmacology)</term>
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<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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<AbstractText>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.</AbstractText>
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