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rdf:type |
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lifeskim:mentions |
umls-concept:C0072323,
umls-concept:C0243077,
umls-concept:C0318467,
umls-concept:C0439851,
umls-concept:C1510941,
umls-concept:C1552596,
umls-concept:C1707689,
umls-concept:C1880355,
umls-concept:C1883254,
umls-concept:C1947931,
umls-concept:C2348042
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pubmed:issue |
10
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pubmed:dateCreated |
2002-5-2
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pubmed:abstractText |
Utilizing the tools of parallel synthesis and structure-based design, a new class of Michael acceptor-containing, irreversible inhibitors of human rhinovirus 3C protease (HRV 3CP) was discovered. These inhibitors are shown to inhibit HRV-14 3CP with rates of inactivation ranging from 886 to 31 400 M(-1) sec(-1). These inhibitors exhibit antiviral activity when tested against HRV-14 infected H1-HeLa cells, with EC(50) values ranging from 1.94 to 0.15 microM. No cytotoxicity was observed at the limits of the assay concentration. A crystal structure of one of the more potent inhibitors covalently bound to HRV-2 3CP is detailed. These compounds were also tested against HRV serotypes other than type 14 and were found to have highly variable activities.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BrownEdward LEL,
pubmed-author:ChanForaF,
pubmed-author:ChuShao SongSS,
pubmed-author:DragovichPeter SPS,
pubmed-author:EastmanBrian WBW,
pubmed-author:FerreRose AnnRA,
pubmed-author:FuhrmanShella ASA,
pubmed-author:GilRR,
pubmed-author:HendricksonThomas FTF,
pubmed-author:JohnsonTheodore OTO,
pubmed-author:LuuHiep THT,
pubmed-author:MaldonadoFausto CFC,
pubmed-author:MatthewsDavid ADA,
pubmed-author:MeadorJames WJW3rd,
pubmed-author:PatickAmy KAK,
pubmed-author:ReichSiegfried HSH,
pubmed-author:SkalitzkyDonald JDJ,
pubmed-author:WorlandStephen TST,
pubmed-author:YangMichelleM,
pubmed-author:ZalmanLeora SLS
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pubmed:issnType |
Print
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pubmed:day |
9
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pubmed:volume |
45
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pubmed:owner |
NLM
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|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
2016-23
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pubmed:dateRevised |
2007-10-11
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pubmed:meshHeading |
pubmed-meshheading:11985469-Antiviral Agents,
pubmed-meshheading:11985469-Combinatorial Chemistry Techniques,
pubmed-meshheading:11985469-Crystallography, X-Ray,
pubmed-meshheading:11985469-Cysteine Endopeptidases,
pubmed-meshheading:11985469-Enzyme Inhibitors,
pubmed-meshheading:11985469-HeLa Cells,
pubmed-meshheading:11985469-Humans,
pubmed-meshheading:11985469-Protein Binding,
pubmed-meshheading:11985469-Rhinovirus,
pubmed-meshheading:11985469-Structure-Activity Relationship,
pubmed-meshheading:11985469-Viral Proteins
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pubmed:year |
2002
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pubmed:articleTitle |
Structure-based design of a parallel synthetic array directed toward the discovery of irreversible inhibitors of human rhinovirus 3C protease.
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pubmed:affiliation |
Pfizer Global R&D-La Jolla/Agouron Pharmaceuticals, Inc., 10770 Science Center Road, San Diego, CA 92121, USA. tjohnson@agouron.com
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pubmed:publicationType |
Journal Article
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