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Article: Characterization of SARS-CoV main protease and identification of biologically active small molecule inhibitors using a continuous fluorescence-based assay

TitleCharacterization of SARS-CoV main protease and identification of biologically active small molecule inhibitors using a continuous fluorescence-based assay
Authors
Issue Date2004
PublisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/febslet
Citation
Febs Letters, 2004, v. 576 n. 3, p. 325-330 How to Cite?
AbstractSevere acute respiratory syndrome associated coronavirus main protease (SARS-CoV Mpro) has been proposed as a prime target for anti-SARS drug development. We have cloned and overexpressed the SARS-CoV Mpro in Escherichia coli, and purified the recombinant Mpro to homogeneity. The kinetic parameters of the recombinant SARS-CoV Mpro were characterized by high performance liquid chromatography-based assay and continuous fluorescence-based assay. Two novel small molecule inhibitors of the SARS-CoV Mpro were identified by high-throughput screening using an internally quenched fluorogenic substrate. The identified inhibitors have K i values at low μM range with comparable anti-SARS-CoV activity in cell-based assays. © 2004 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
Persistent Identifierhttp://hdl.handle.net/10722/79267
ISSN
2015 Impact Factor: 3.519
2015 SCImago Journal Rankings: 2.026
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorKao, RYen_HK
dc.contributor.authorTo, APCen_HK
dc.contributor.authorNg, LWYen_HK
dc.contributor.authorTsui, WHWen_HK
dc.contributor.authorLee, TSWen_HK
dc.contributor.authorTsoi, HWen_HK
dc.contributor.authorYuen, KYen_HK
dc.date.accessioned2010-09-06T07:52:37Z-
dc.date.available2010-09-06T07:52:37Z-
dc.date.issued2004en_HK
dc.identifier.citationFebs Letters, 2004, v. 576 n. 3, p. 325-330en_HK
dc.identifier.issn0014-5793en_HK
dc.identifier.urihttp://hdl.handle.net/10722/79267-
dc.description.abstractSevere acute respiratory syndrome associated coronavirus main protease (SARS-CoV Mpro) has been proposed as a prime target for anti-SARS drug development. We have cloned and overexpressed the SARS-CoV Mpro in Escherichia coli, and purified the recombinant Mpro to homogeneity. The kinetic parameters of the recombinant SARS-CoV Mpro were characterized by high performance liquid chromatography-based assay and continuous fluorescence-based assay. Two novel small molecule inhibitors of the SARS-CoV Mpro were identified by high-throughput screening using an internally quenched fluorogenic substrate. The identified inhibitors have K i values at low μM range with comparable anti-SARS-CoV activity in cell-based assays. © 2004 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.en_HK
dc.languageengen_HK
dc.publisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/febsleten_HK
dc.relation.ispartofFEBS Lettersen_HK
dc.rightsF E B S Letters. Copyright © Elsevier BV.en_HK
dc.subject.meshBase Sequenceen_HK
dc.subject.meshChromatography, High Pressure Liquiden_HK
dc.subject.meshCloning, Molecularen_HK
dc.subject.meshCysteine Endopeptidasesen_HK
dc.subject.meshDNA Primersen_HK
dc.subject.meshEndopeptidases - metabolismen_HK
dc.subject.meshEscherichia coli - enzymology - geneticsen_HK
dc.subject.meshKineticsen_HK
dc.subject.meshRecombinant Proteins - antagonists & inhibitors - metabolismen_HK
dc.subject.meshSARS Virus - enzymologyen_HK
dc.subject.meshSpectrometry, Fluorescence - methodsen_HK
dc.subject.meshViral Proteins - antagonists & inhibitors - metabolismen_HK
dc.titleCharacterization of SARS-CoV main protease and identification of biologically active small molecule inhibitors using a continuous fluorescence-based assayen_HK
dc.typeArticleen_HK
dc.identifier.openurlhttp://library.hku.hk:4550/resserv?sid=HKU:IR&issn=0014-5793&volume=576&issue=3&spage=325&epage=30&date=2004&atitle=Characterization+of+SARS-CoV+main+protease+and+identification+of+biologically+active+small+molecule+inhibitors+using+a+continuous+fluorescence-based+assay.en_HK
dc.identifier.emailKao, RY:rytkao@hkucc.hku.hken_HK
dc.identifier.emailTsoi, HW:hwtsoi@hkucc.hku.hken_HK
dc.identifier.emailYuen, KY:kyyuen@hkucc.hku.hken_HK
dc.identifier.authorityKao, RY=rp00481en_HK
dc.identifier.authorityTsoi, HW=rp00439en_HK
dc.identifier.authorityYuen, KY=rp00366en_HK
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/j.febslet.2004.09.026en_HK
dc.identifier.pmid15498556-
dc.identifier.scopuseid_2-s2.0-6344270316en_HK
dc.identifier.hkuros100174en_HK
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-6344270316&selection=ref&src=s&origin=recordpageen_HK
dc.identifier.volume576en_HK
dc.identifier.issue3en_HK
dc.identifier.spage325en_HK
dc.identifier.epage330en_HK
dc.identifier.isiWOS:000224789700009-
dc.publisher.placeNetherlandsen_HK
dc.identifier.scopusauthoridKao, RY=7101675499en_HK
dc.identifier.scopusauthoridTo, APC=36828058300en_HK
dc.identifier.scopusauthoridNg, LWY=7201477846en_HK
dc.identifier.scopusauthoridTsui, WHW=36124344600en_HK
dc.identifier.scopusauthoridLee, TSW=7501439333en_HK
dc.identifier.scopusauthoridTsoi, HW=6603822102en_HK
dc.identifier.scopusauthoridYuen, KY=36078079100en_HK

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