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Article: Identification of novel small-molecule inhibitors of severe acute respiratory syndrome-associated coronavirus by chemical genetics
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TitleIdentification of novel small-molecule inhibitors of severe acute respiratory syndrome-associated coronavirus by chemical genetics
 
AuthorsKao, RY1
Tsui, WHW1
Lee, TSW1
Tanner, JA1
Watt, RM1
Huang, JD1
Hu, L1
Chen, G1
Chen, Z2
Zhang, L2
He, T2
Chan, KH1
Tse, H1
To, APC1
Ng, LWY1
Wong, BCW1
Tsoi, HW1
Yang, D1
Ho, DD2
Yuen, KY1
 
Issue Date2004
 
PublisherCell Press. The Journal's web site is located at http://www.elsevier.com/locate/chembiol
 
CitationChemistry And Biology, 2004, v. 11 n. 9, p. 1293-1299 [How to Cite?]
DOI: http://dx.doi.org/10.1016/j.chembiol.2004.07.013
 
AbstractThe severe acute respiratory syndrome-associated coronavirus (SARS-CoV) infected more than 8,000 people across 29 countries and caused more than 900 fatalities. Based on the concept of chemical genetics, we screened 50,240 structurally diverse small molecules from which we identified 104 compounds with anti-SARS-CoV activity. Of these 104 compounds, 2 target the SARS-CoV main protease (M pro), 7 target helicase (Hel), and 18 target spike (S) protein-angiotensin-converting enzyme 2 (ACE2)-mediated viral entry. The EC 50 of the majority of the 104 compounds determined by SARS-CoV plaque reduction assay were found to be at low micromolar range. Three selected compounds, MP576, HE602, and VE607, validated to be inhibitors of SARS-CoV M pro, Hel, and viral entry, respectively, exhibited potent antiviral activity (EC 50 < 10 μM) and comparable inhibitory activities in target-specific in vitro assays.
 
ISSN1074-5521
2012 Impact Factor: 6.157
2012 SCImago Journal Rankings: 2.258
 
DOIhttp://dx.doi.org/10.1016/j.chembiol.2004.07.013
 
ISI Accession Number IDWOS:000224228900012
 
ReferencesReferences in Scopus
 
DC FieldValue
dc.contributor.authorKao, RY
 
dc.contributor.authorTsui, WHW
 
dc.contributor.authorLee, TSW
 
dc.contributor.authorTanner, JA
 
dc.contributor.authorWatt, RM
 
dc.contributor.authorHuang, JD
 
dc.contributor.authorHu, L
 
dc.contributor.authorChen, G
 
dc.contributor.authorChen, Z
 
dc.contributor.authorZhang, L
 
dc.contributor.authorHe, T
 
dc.contributor.authorChan, KH
 
dc.contributor.authorTse, H
 
dc.contributor.authorTo, APC
 
dc.contributor.authorNg, LWY
 
dc.contributor.authorWong, BCW
 
dc.contributor.authorTsoi, HW
 
dc.contributor.authorYang, D
 
dc.contributor.authorHo, DD
 
dc.contributor.authorYuen, KY
 
dc.date.accessioned2010-09-06T06:02:15Z
 
dc.date.available2010-09-06T06:02:15Z
 
dc.date.issued2004
 
dc.description.abstractThe severe acute respiratory syndrome-associated coronavirus (SARS-CoV) infected more than 8,000 people across 29 countries and caused more than 900 fatalities. Based on the concept of chemical genetics, we screened 50,240 structurally diverse small molecules from which we identified 104 compounds with anti-SARS-CoV activity. Of these 104 compounds, 2 target the SARS-CoV main protease (M pro), 7 target helicase (Hel), and 18 target spike (S) protein-angiotensin-converting enzyme 2 (ACE2)-mediated viral entry. The EC 50 of the majority of the 104 compounds determined by SARS-CoV plaque reduction assay were found to be at low micromolar range. Three selected compounds, MP576, HE602, and VE607, validated to be inhibitors of SARS-CoV M pro, Hel, and viral entry, respectively, exhibited potent antiviral activity (EC 50 < 10 μM) and comparable inhibitory activities in target-specific in vitro assays.
 
dc.description.natureLink_to_subscribed_fulltext
 
dc.identifier.citationChemistry And Biology, 2004, v. 11 n. 9, p. 1293-1299 [How to Cite?]
DOI: http://dx.doi.org/10.1016/j.chembiol.2004.07.013
 
dc.identifier.doihttp://dx.doi.org/10.1016/j.chembiol.2004.07.013
 
dc.identifier.epage1299
 
dc.identifier.hkuros95092
 
dc.identifier.isiWOS:000224228900012
 
dc.identifier.issn1074-5521
2012 Impact Factor: 6.157
2012 SCImago Journal Rankings: 2.258
 
dc.identifier.issue9
 
dc.identifier.openurl
 
dc.identifier.pmid15380189
 
dc.identifier.scopuseid_2-s2.0-4644343545
 
dc.identifier.spage1293
 
dc.identifier.urihttp://hdl.handle.net/10722/68193
 
dc.identifier.volume11
 
dc.languageeng
 
dc.publisherCell Press. The Journal's web site is located at http://www.elsevier.com/locate/chembiol
 
dc.publisher.placeUnited States
 
dc.relation.ispartofChemistry and Biology
 
dc.relation.referencesReferences in Scopus
 
dc.subject.meshAntiviral Agents - Chemical Synthesis - Chemistry - Pharmacology
 
dc.subject.meshCarboxypeptidases - Antagonists & Inhibitors - Metabolism
 
dc.subject.meshSars Virus - Drug Effects - Growth & Development - Metabolism - Physiology
 
dc.subject.meshViral Matrix Proteins - Antagonists & Inhibitors - Metabolism
 
dc.subject.meshSevere Acute Respiratory Syndrome - Drug Therapy
 
dc.titleIdentification of novel small-molecule inhibitors of severe acute respiratory syndrome-associated coronavirus by chemical genetics
 
dc.typeArticle
 
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Author Affiliations
  1. The University of Hong Kong
  2. Aaron Diamond AIDS Research Center