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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2002-5-2
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pubmed:abstractText |
A potent, selective, orally active LXR agonist was identified from focused libraries of tertiary amines. GW3965 (12) recruits the steroid receptor coactivator 1 to human LXRalpha in a cell-free ligand-sensing assay with an EC(50) of 125 nM and profiles as a full agonist on hLXRalpha and hLXRbeta in cell-based reporter gene assays with EC(50)'s of 190 and 30 nM, respectively. After oral dosing at 10 mg/kg to C57BL/6 mice, 12 increased expression of the reverse cholesterol transporter ABCA1 in the small intestine and peripheral macrophages and increased the plasma concentrations of HDL cholesterol by 30%. 12 will be a valuable chemical tool to investigate the role of LXR in the regulation of reverse cholesterol transport and lipid metabolism.
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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/Amines,
http://linkedlifedata.com/resource/pubmed/chemical/Cholesterol,
http://linkedlifedata.com/resource/pubmed/chemical/Cholesterol, HDL,
http://linkedlifedata.com/resource/pubmed/chemical/DNA-Binding Proteins,
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/Receptors, Retinoic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Thyroid Hormone,
http://linkedlifedata.com/resource/pubmed/chemical/liver X receptor
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BeaudetElizabeth JEJ,
pubmed-author:BinzJane GJG,
pubmed-author:CollinsJon LJL,
pubmed-author:FivushAdam MAM,
pubmed-author:GalardiCristin MCM,
pubmed-author:KliewerSteven ASA,
pubmed-author:LewisMichael CMC,
pubmed-author:MooreLinda BLB,
pubmed-author:MorganDaniel GDG,
pubmed-author:ParksDerek JDJ,
pubmed-author:PlunketKelli DKD,
pubmed-author:TippinTim KTK,
pubmed-author:WatsonMichael AMA,
pubmed-author:WhitneyKarl DKD,
pubmed-author:WillsonTimothy MTM,
pubmed-author:WilsonJoan GJG
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pubmed:issnType |
Print
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pubmed:day |
9
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1963-6
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:11985463-ATP-Binding Cassette Transporters,
pubmed-meshheading:11985463-Administration, Oral,
pubmed-meshheading:11985463-Amines,
pubmed-meshheading:11985463-Animals,
pubmed-meshheading:11985463-Biological Availability,
pubmed-meshheading:11985463-Cell-Free System,
pubmed-meshheading:11985463-Cholesterol,
pubmed-meshheading:11985463-Cholesterol, HDL,
pubmed-meshheading:11985463-DNA-Binding Proteins,
pubmed-meshheading:11985463-Genes, Reporter,
pubmed-meshheading:11985463-Humans,
pubmed-meshheading:11985463-Intestine, Small,
pubmed-meshheading:11985463-Macrophages,
pubmed-meshheading:11985463-Mice,
pubmed-meshheading:11985463-Mice, Inbred C57BL,
pubmed-meshheading:11985463-Orphan Nuclear Receptors,
pubmed-meshheading:11985463-Receptors, Cytoplasmic and Nuclear,
pubmed-meshheading:11985463-Receptors, Retinoic Acid,
pubmed-meshheading:11985463-Receptors, Thyroid Hormone,
pubmed-meshheading:11985463-Structure-Activity Relationship,
pubmed-meshheading:11985463-Up-Regulation
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pubmed:year |
2002
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pubmed:articleTitle |
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
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pubmed:publicationType |
Journal Article
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