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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
1999-2-2
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pubmed:abstractText |
In search of antiinflammatory drugs with a new mechanism of action, U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with an IC50 of 0.07 microM for MEK 1 and 0.06 microM for MEK 2. U0126 can undergo isomerization and cyclization reactions to form a variety of products, both chemically and in vivo, all of which exhibit less affinity for MEK and lower inhibition of AP-1 activity than parent, U0126.
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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 |
Oct
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BlomK FKF,
pubmed-author:CopelandR ARA,
pubmed-author:DaulerioA JAJ,
pubmed-author:DunciaJ VJV,
pubmed-author:EarlR ARA,
pubmed-author:FavataM FMF,
pubmed-author:FrietzeW EWE,
pubmed-author:HigleyC ACA,
pubmed-author:HobbsF WFW,
pubmed-author:HoriuchiKK,
pubmed-author:MagoldaR LRL,
pubmed-author:MartzR CRC,
pubmed-author:OlsonR ERE,
pubmed-author:PittsW JWJ,
pubmed-author:RankinF WFW,
pubmed-author:SantellaJ BJB3rd,
pubmed-author:ScherleP APA,
pubmed-author:StradleyD ADA,
pubmed-author:SueJ SJS,
pubmed-author:TabakaA CAC,
pubmed-author:TelehaC ACA,
pubmed-author:TrainorG LGL,
pubmed-author:TrzaskosJ MJM,
pubmed-author:WexlerR RRR,
pubmed-author:WityakJJ
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pubmed:issnType |
Print
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pubmed:day |
20
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2839-44
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:9873633-Animals,
pubmed-meshheading:9873633-Anti-Inflammatory Agents,
pubmed-meshheading:9873633-Biotransformation,
pubmed-meshheading:9873633-Butadienes,
pubmed-meshheading:9873633-Cyclization,
pubmed-meshheading:9873633-Enzyme Inhibitors,
pubmed-meshheading:9873633-NF-kappa B,
pubmed-meshheading:9873633-Nitriles,
pubmed-meshheading:9873633-Protein-Serine-Threonine Kinases,
pubmed-meshheading:9873633-Rats,
pubmed-meshheading:9873633-Transcription Factor AP-1
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pubmed:year |
1998
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pubmed:articleTitle |
MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
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pubmed:affiliation |
DuPont Pharmaceuticals Company, Chemical and Physical Sciences Department, Wilmington, DE 19880, USA.
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pubmed:publicationType |
Journal Article
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