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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2009-2-23
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pubmed:abstractText |
A series of 4-(amido-biarylether)-quinolines was prepared as potential LXR agonists. Appropriate substitution with amide groups provided high affinity LXR ligands, some with excellent potency and efficacy in functional assays of LXR activity. Novel amide 4g had a binding IC(50)=1.9 nM for LXRbeta and EC(50)=34 nM (96% efficacy relative to T0901317) in an ABCA1 gene expression assay in mouse J774 cells, demonstrating that 4-(biarylether)-quinolines with appropriate amide substitution are potent 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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1464-3391
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pubmed:author |
pubmed-author:BernotasRonald CRC,
pubmed-author:FarnegardhMathiasM,
pubmed-author:FletcherHoraceH3rd,
pubmed-author:Goos-NilssonAnnikaA,
pubmed-author:KaufmanDavid HDH,
pubmed-author:NambiPonnalP,
pubmed-author:QuinetElaineE,
pubmed-author:SinghausRobert RRR,
pubmed-author:UllrichJohnJ,
pubmed-author:UnwallaRayomandR,
pubmed-author:WilhelmssonAnnaA,
pubmed-author:WrobelJayJ
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1663-70
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:19162487-ATP-Binding Cassette Transporters,
pubmed-meshheading:19162487-Amides,
pubmed-meshheading:19162487-Animals,
pubmed-meshheading:19162487-Cell Line,
pubmed-meshheading:19162487-Crystallography, X-Ray,
pubmed-meshheading:19162487-DNA-Binding Proteins,
pubmed-meshheading:19162487-Gene Expression Regulation,
pubmed-meshheading:19162487-Kinetics,
pubmed-meshheading:19162487-Ligands,
pubmed-meshheading:19162487-Mice,
pubmed-meshheading:19162487-Models, Molecular,
pubmed-meshheading:19162487-Orphan Nuclear Receptors,
pubmed-meshheading:19162487-Quinolines,
pubmed-meshheading:19162487-Receptors, Cytoplasmic and Nuclear,
pubmed-meshheading:19162487-Transcriptional Activation,
pubmed-meshheading:19162487-Transfection
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pubmed:year |
2009
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pubmed:articleTitle |
Biarylether amide quinolines as liver X receptor agonists.
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pubmed:affiliation |
Chemical and Screening Sciences, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, PA 19426, USA. bernotr@wyeth.com
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pubmed:publicationType |
Journal Article
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