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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
17
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pubmed:dateCreated |
2005-8-18
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pubmed:abstractText |
Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a high throughput screen as inducers of human ATP binding cassette transporter A1 expression. Mechanism of action studies led to the identification of GSK3987 as an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC(50)s of 40 nM, profiles as an LXR agonist in functional assays, and activates LXR though a mechanism that is similar to first generation LXR agonists.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/ATP binding cassette transporter 1,
http://linkedlifedata.com/resource/pubmed/chemical/ATP-Binding Cassette Transporters,
http://linkedlifedata.com/resource/pubmed/chemical/Aniline Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/DNA-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Histone Acetyltransferases,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Luciferases,
http://linkedlifedata.com/resource/pubmed/chemical/Maleimides,
http://linkedlifedata.com/resource/pubmed/chemical/NCOA1 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Nuclear Receptor Coactivator 1,
http://linkedlifedata.com/resource/pubmed/chemical/Orphan Nuclear Receptors,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cytoplasmic and Nuclear,
http://linkedlifedata.com/resource/pubmed/chemical/Transcription Factors,
http://linkedlifedata.com/resource/pubmed/chemical/liver X receptor
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:CampobassoNinoN,
pubmed-author:CaravellaJustin AJA,
pubmed-author:CollinsJon LJL,
pubmed-author:De Los Frailes AlvaroMaiteM,
pubmed-author:HaighDavidD,
pubmed-author:JayeMichael CMC,
pubmed-author:KerriganJohn JJJ,
pubmed-author:KrawiecJohn AJA,
pubmed-author:LaffitteBryanB,
pubmed-author:LiuWu-SchyongWS,
pubmed-author:LuQuinnQ,
pubmed-author:MacpheeColin HCH,
pubmed-author:MarinoJoseph PJPJr,
pubmed-author:MeyerCraig RCR,
pubmed-author:NicholsJason AJA,
pubmed-author:ParksDerek JDJ,
pubmed-author:PerezPalomaP,
pubmed-author:QiuChunyanC,
pubmed-author:Sarov-BlatLeaL,
pubmed-author:SeepersaudSheila DSD,
pubmed-author:SmallwoodAngelaA,
pubmed-author:SteplewskiKlaudia MKM,
pubmed-author:ThompsonScott KSK,
pubmed-author:WangPingP,
pubmed-author:WatsonMike AMA,
pubmed-author:WebbChristine LCL,
pubmed-author:WillsonTimothy MTM
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pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5419-22
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:16107141-ATP-Binding Cassette Transporters,
pubmed-meshheading:16107141-Aniline Compounds,
pubmed-meshheading:16107141-Binding Sites,
pubmed-meshheading:16107141-Cell Line,
pubmed-meshheading:16107141-Crystallography, X-Ray,
pubmed-meshheading:16107141-DNA-Binding Proteins,
pubmed-meshheading:16107141-Genes, Reporter,
pubmed-meshheading:16107141-Histone Acetyltransferases,
pubmed-meshheading:16107141-Humans,
pubmed-meshheading:16107141-Ligands,
pubmed-meshheading:16107141-Luciferases,
pubmed-meshheading:16107141-Maleimides,
pubmed-meshheading:16107141-Models, Molecular,
pubmed-meshheading:16107141-Molecular Structure,
pubmed-meshheading:16107141-Monocytes,
pubmed-meshheading:16107141-Nuclear Receptor Coactivator 1,
pubmed-meshheading:16107141-Orphan Nuclear Receptors,
pubmed-meshheading:16107141-Promoter Regions, Genetic,
pubmed-meshheading:16107141-Receptors, Cytoplasmic and Nuclear,
pubmed-meshheading:16107141-Structure-Activity Relationship,
pubmed-meshheading:16107141-Transcription Factors,
pubmed-meshheading:16107141-Up-Regulation
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pubmed:year |
2005
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pubmed:articleTitle |
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
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pubmed:affiliation |
GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina 27709, USA.
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pubmed:publicationType |
Journal Article
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