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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 |
2007-8-16
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pubmed:abstractText |
We have identified a novel liver X receptor (LXR) agonist (2) that activates the LXRbeta subtype with selectivity over LXRalpha. LXRbeta selectivity was confirmed using macrophages derived from LXR mutant mice. Despite its selectivity and modest potency, the compound can induce APO-AI-dependent cholesterol efflux from macrophages with full efficacy. Our results indicate that it is possible to achieve significant LXRbeta selectivity in a small molecule while maintaining functional LXR activity.
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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 |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BradleyMichelleM,
pubmed-author:BrockAnsgarA,
pubmed-author:CastrilloAntonioA,
pubmed-author:ChowDonaldD,
pubmed-author:FangLiangL,
pubmed-author:HaslamJennifer AJA,
pubmed-author:KoderAlanA,
pubmed-author:LiXiaolinX,
pubmed-author:MakPuiying APA,
pubmed-author:MitroNicoN,
pubmed-author:MolteniValentinaV,
pubmed-author:NabakkaJulietJ,
pubmed-author:RomeoRussellR,
pubmed-author:SaezEnriqueE,
pubmed-author:SeidelH MartinHM,
pubmed-author:SpaldingTracy ATA,
pubmed-author:TontonozPeterP,
pubmed-author:TuntlandToveT,
pubmed-author:VargasLeoL,
pubmed-author:WityakJohnJ
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pubmed:issnType |
Print
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pubmed:day |
23
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4255-9
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:17665897-ATP-Binding Cassette Transporters,
pubmed-meshheading:17665897-Animals,
pubmed-meshheading:17665897-Apolipoprotein A-I,
pubmed-meshheading:17665897-Cell Line,
pubmed-meshheading:17665897-Cholesterol,
pubmed-meshheading:17665897-Crystallography, X-Ray,
pubmed-meshheading:17665897-DNA-Binding Proteins,
pubmed-meshheading:17665897-Hepatocytes,
pubmed-meshheading:17665897-Humans,
pubmed-meshheading:17665897-Macrophages, Peritoneal,
pubmed-meshheading:17665897-Mice,
pubmed-meshheading:17665897-Mice, Knockout,
pubmed-meshheading:17665897-Orphan Nuclear Receptors,
pubmed-meshheading:17665897-Receptors, Cytoplasmic and Nuclear,
pubmed-meshheading:17665897-Stereoisomerism,
pubmed-meshheading:17665897-Structure-Activity Relationship,
pubmed-meshheading:17665897-Thiadiazoles
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pubmed:year |
2007
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pubmed:articleTitle |
N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta.
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pubmed:affiliation |
Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, California 92121, USA. vmolteni@gnf.org
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pubmed:publicationType |
Journal Article
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