rdf:type |
|
lifeskim:mentions |
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pubmed:issue |
18
|
pubmed:dateCreated |
2006-8-14
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pubmed:abstractText |
A novel class of non-nucleoside HCV NS5B polymerase inhibitors has been identified from screening. A co-crystal structure revealed an allosteric binding site in the protein that required a unique conformational change to accommodate inhibitor binding. Herein we report the structure-activity relationships (SARs) of this novel class of dihydropyrone-containing compounds that show potent inhibitory activities against the HCV RNA polymerase in biochemical assays.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
|
pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BlazelJulieJ,
pubmed-author:BorchardtAllenA,
pubmed-author:DoanChauC,
pubmed-author:DragovichPeterP,
pubmed-author:DuggalRohitR,
pubmed-author:FoàVV,
pubmed-author:FuhrmanShellaS,
pubmed-author:GonzalezJavierJ,
pubmed-author:HickeyMichaelM,
pubmed-author:JewellTanyaT,
pubmed-author:LewisCristinaC,
pubmed-author:LintonAngelicaA,
pubmed-author:LoveRobertR,
pubmed-author:PargeHansH,
pubmed-author:PrinsTomT,
pubmed-author:ShiStephanieS,
pubmed-author:TatlockJohnJ,
pubmed-author:ZhouRuR
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pubmed:issnType |
Print
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pubmed:day |
15
|
pubmed:volume |
16
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
4834-8
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pubmed:meshHeading |
pubmed-meshheading:16824756-Crystallography, X-Ray,
pubmed-meshheading:16824756-DNA-Directed RNA Polymerases,
pubmed-meshheading:16824756-Hepacivirus,
pubmed-meshheading:16824756-Hydrogen,
pubmed-meshheading:16824756-Inhibitory Concentration 50,
pubmed-meshheading:16824756-Models, Molecular,
pubmed-meshheading:16824756-Molecular Structure,
pubmed-meshheading:16824756-Pyrones,
pubmed-meshheading:16824756-RNA Replicase,
pubmed-meshheading:16824756-Structure-Activity Relationship,
pubmed-meshheading:16824756-Viral Nonstructural Proteins
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pubmed:year |
2006
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pubmed:articleTitle |
Identification and structure-based optimization of novel dihydropyrones as potent HCV RNA polymerase inhibitors.
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pubmed:affiliation |
Pfizer Global Research and Development, La Jolla Laboratories, 10770 Science Center Dr., San Diego, CA 92121, USA. hui.li@pfizer.com
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pubmed:publicationType |
Journal Article
|