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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
2006-11-10
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pubmed:abstractText |
The synthesis and structure-activity studies of a series of quinoline-3-carbonitriles as inhibitors of Tpl2 kinase are described. Potent inhibitors of Tpl2 kinase with selectivity against a panel of selected kinases in enzymatic assays and specificity in cell-based phosphorylation assays in LPS-treated human monocytes were identified. Selected inhibitors with moderate activity in human whole blood assay effectively inhibited LPS/D-Gal induced TNFalpha release when administered intraperitoneally in mice.
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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 |
Dec
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:CuozzoJohn WJW,
pubmed-author:GavrinLori KLK,
pubmed-author:GreenNealN,
pubmed-author:HallJ PerryJP,
pubmed-author:HsuSangS,
pubmed-author:HuYonghanY,
pubmed-author:JanzKristinK,
pubmed-author:KailaNeeluN,
pubmed-author:LiHuan-QiuHQ,
pubmed-author:LinLih-LingLL,
pubmed-author:Nickerson-NutterCherylC,
pubmed-author:StentV CVC,
pubmed-author:TelliezJean-BaptisteJB,
pubmed-author:ThomasonJennifer RJR
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6067-72
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:16973359-Arthritis, Rheumatoid,
pubmed-meshheading:16973359-Cross-Linking Reagents,
pubmed-meshheading:16973359-Humans,
pubmed-meshheading:16973359-Imidazoles,
pubmed-meshheading:16973359-MAP Kinase Kinase Kinases,
pubmed-meshheading:16973359-Molecular Structure,
pubmed-meshheading:16973359-Monocytes,
pubmed-meshheading:16973359-Nitriles,
pubmed-meshheading:16973359-Quinolines,
pubmed-meshheading:16973359-Structure-Activity Relationship,
pubmed-meshheading:16973359-Tumor Necrosis Factor-alpha
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pubmed:year |
2006
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pubmed:articleTitle |
Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.
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pubmed:affiliation |
Department of Chemical and Screening Sciences, Wyeth Research, 200 CambridgePark Drive, Cambridge, MA 02140, USA. fhu@wyeth.com <fhu@wyeth.com>
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pubmed:publicationType |
Journal Article
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