Identification of a Novel Small Molecule Inhibitor Against SARS Coronavirus Helicase.
Identifieur interne : 001304 ( Main/Exploration ); précédent : 001303; suivant : 001305Identification of a Novel Small Molecule Inhibitor Against SARS Coronavirus Helicase.
Auteurs : Jin-Beom Cho [Corée du Sud] ; Jin-Moo Lee [Corée du Sud] ; Hee-Chul Ahn [Corée du Sud] ; Yong-Joo Jeong [Corée du Sud]Source :
- Journal of microbiology and biotechnology [ 1738-8872 ] ; 2015.
Descripteurs français
- KwdFr :
- MESH :
- antagonistes et inhibiteurs : Helicase.
- enzymologie : Virus du SRAS.
- isolement et purification : Antienzymes, Antiviraux.
- métabolisme : Adénosine triphosphate.
- pharmacologie : Antienzymes, Antiviraux.
- Concentration inhibitrice 50, Hydrolyse.
English descriptors
- KwdEn :
- Adenosine Triphosphate (metabolism), Antiviral Agents (isolation & purification), Antiviral Agents (pharmacology), DNA Helicases (antagonists & inhibitors), Enzyme Inhibitors (isolation & purification), Enzyme Inhibitors (pharmacology), Hydrolysis, Inhibitory Concentration 50, SARS Virus (enzymology).
- MESH :
- chemical , antagonists & inhibitors : DNA Helicases.
- chemical , isolation & purification : Antiviral Agents, Enzyme Inhibitors.
- chemical , metabolism : Adenosine Triphosphate.
- chemical , pharmacology : Antiviral Agents, Enzyme Inhibitors.
- enzymology : SARS Virus.
- Hydrolysis, Inhibitory Concentration 50.
Abstract
A new chemical inhibitor against severe acute respiratory syndrome (SARS) coronavirus helicase, 7-ethyl-8-mercapto-3-methyl-3,7-dihydro-1H-purine-2,6-dione, was identified. We investigated the inhibitory effect of the compound by conducting colorimetry-based ATP hydrolysis assay and fluorescence resonance energy transfer-based double-stranded DNA unwinding assay. The compound suppressed both ATP hydrolysis and double-stranded DNA unwinding activities of helicase with IC50 values of 8.66 ± 0.26 μM and 41.6 ± 2.3 μM, respectively. Moreover, we observed that the compound did not show cytotoxicity up to 80 µMconcentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor.
DOI: 10.4014/jmb.1507.07078
PubMed: 26387819
Affiliations:
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Le document en format XML
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<term>Enzyme Inhibitors (isolation & purification)</term>
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<term>Antienzymes (pharmacologie)</term>
<term>Antiviraux (isolement et purification)</term>
<term>Antiviraux (pharmacologie)</term>
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<term>Helicase (antagonistes et inhibiteurs)</term>
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<front><div type="abstract" xml:lang="en">A new chemical inhibitor against severe acute respiratory syndrome (SARS) coronavirus helicase, 7-ethyl-8-mercapto-3-methyl-3,7-dihydro-1H-purine-2,6-dione, was identified. We investigated the inhibitory effect of the compound by conducting colorimetry-based ATP hydrolysis assay and fluorescence resonance energy transfer-based double-stranded DNA unwinding assay. The compound suppressed both ATP hydrolysis and double-stranded DNA unwinding activities of helicase with IC50 values of 8.66 ± 0.26 μM and 41.6 ± 2.3 μM, respectively. Moreover, we observed that the compound did not show cytotoxicity up to 80 µMconcentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor. </div>
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