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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2007-3-15
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pubmed:databankReference |
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pubmed:abstractText |
The Ras/Raf/MEK/ERK signal transduction is a key oncogenic pathway implicated in a variety of human cancers. We have identified a novel series of pyrazolylpyrroles as inhibitors of ERK. Aided by the discovery of two distinct binding modes for the pyrazolylpyrrole scaffold, structure-guided optimization culminated in the discovery of 6p, a potent and selective inhibitor of ERK.
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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 |
Mar
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AronovAlex MAM,
pubmed-author:BakerChristopherC,
pubmed-author:BemisGuy WGW,
pubmed-author:CaoJingrongJ,
pubmed-author:ChenGuanjingG,
pubmed-author:FordPamella JPJ,
pubmed-author:GermannUrsula AUA,
pubmed-author:GreenJeremyJ,
pubmed-author:HaleMichael RMR,
pubmed-author:JacobsMarcM,
pubmed-author:JanetkaJames WJW,
pubmed-author:MaltaisFrancoisF,
pubmed-author:Martinez-BotellaGabrielG,
pubmed-author:NamchukMark NMN,
pubmed-author:StraubJudyJ,
pubmed-author:TangQingQ,
pubmed-author:XieXiaolingX
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pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1280-7
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:17300186-Binding Sites,
pubmed-meshheading:17300186-Crystallography, X-Ray,
pubmed-meshheading:17300186-Mitogen-Activated Protein Kinase 1,
pubmed-meshheading:17300186-Mitogen-Activated Protein Kinase 3,
pubmed-meshheading:17300186-Models, Molecular,
pubmed-meshheading:17300186-Molecular Structure,
pubmed-meshheading:17300186-Protein Binding,
pubmed-meshheading:17300186-Pyrazoles,
pubmed-meshheading:17300186-Pyrroles,
pubmed-meshheading:17300186-Quantitative Structure-Activity Relationship,
pubmed-meshheading:17300186-Stereoisomerism
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pubmed:year |
2007
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pubmed:articleTitle |
Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.
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pubmed:affiliation |
Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge, Massachusetts 02139-4242, USA. alex_aronov@vrtx.com
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pubmed:publicationType |
Journal Article
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