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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
MK2 is a Ser/Thr kinase of significant interest as an anti-inflammatory drug discovery target. Here we describe the development of in vitro tools for the identification and characterization of MK2 inhibitors, including validation of inhibitor interactions with the crystallography construct and determination of the unique binding mode of 2,4-diaminopyrimidine inhibitors in the MK2 active site. Use of these tools in the optimization of a potent and selective inhibitor lead series is described in the accompanying Letter.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:ArgiriadiMaria AMA,
pubmed-author:BanachDavid LDL,
pubmed-author:BorhaniDavid WDW,
pubmed-author:CalderwoodDavid JDJ,
pubmed-author:DemersMegan DMD,
pubmed-author:DimauroJenniferJ,
pubmed-author:DixonRichard WRW,
pubmed-author:EricssonAnna MAM,
pubmed-author:HardmanJenniferJ,
pubmed-author:HarrisChristopher MCM,
pubmed-author:KwakSilviaS,
pubmed-author:LiBiqinB,
pubmed-author:MankovichJohn AJA,
pubmed-author:MarcotteDouglasD,
pubmed-author:MullenKelly DKD,
pubmed-author:NiBaofuB,
pubmed-author:PietrasMM,
pubmed-author:SadhukhanRamkrishnaR,
pubmed-author:SousaSilvinoS,
pubmed-author:TalanianRobert VRV,
pubmed-author:TomlinsonMedha JMJ,
pubmed-author:WangLuL,
pubmed-author:XiangTaoT
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pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
330-3
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pubmed:meshHeading |
pubmed-meshheading:19919896-Adenosine Triphosphate,
pubmed-meshheading:19919896-Anti-Inflammatory Agents,
pubmed-meshheading:19919896-Binding, Competitive,
pubmed-meshheading:19919896-Binding Sites,
pubmed-meshheading:19919896-Computer Simulation,
pubmed-meshheading:19919896-Intracellular Signaling Peptides and Proteins,
pubmed-meshheading:19919896-Protein Kinase Inhibitors,
pubmed-meshheading:19919896-Protein-Serine-Threonine Kinases,
pubmed-meshheading:19919896-Pyrimidines,
pubmed-meshheading:19919896-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode.
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pubmed:affiliation |
Abbott Laboratories, 100 Research Drive, Worcester, MA 01605-5314, USA.
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pubmed:publicationType |
Journal Article
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