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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
2006-12-12
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pubmed:abstractText |
We report the identification of substituted cis-bicyclo[3.3.0]-oct-2-enes as small molecule agonists of subfamily V orphan nuclear receptors (NR5A), liver receptor homolog-1 (LRH-1) and steroidogenic factor-1 (SF-1). Using fluorescence resonance energy transfer (FRET)-based biochemical assays, compound 5a (GSK8470) was identified as a high-affinity ligand for LRH-1 and SF-1. In liver cells, 5a increased the expression of the LRH-1 target gene small heterodimer partner (SHP). Synthesis of analogues modified at three positions led to the development of compounds with functional selectivity between LRH-1 and SF-1.
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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/Alkenes,
http://linkedlifedata.com/resource/pubmed/chemical/Aniline Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/DNA-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Homeodomain Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/NR5A1 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/NR5A2 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cytoplasmic and Nuclear,
http://linkedlifedata.com/resource/pubmed/chemical/Steroidogenic Factor 1,
http://linkedlifedata.com/resource/pubmed/chemical/Transcription Factors,
http://linkedlifedata.com/resource/pubmed/chemical/nuclear receptor subfamily 0...
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
16
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pubmed:volume |
49
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6652-5
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pubmed:dateRevised |
2009-8-12
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pubmed:meshHeading |
pubmed-meshheading:17154495-Alkenes,
pubmed-meshheading:17154495-Aniline Compounds,
pubmed-meshheading:17154495-Bicyclo Compounds,
pubmed-meshheading:17154495-Binding Sites,
pubmed-meshheading:17154495-Cells, Cultured,
pubmed-meshheading:17154495-DNA-Binding Proteins,
pubmed-meshheading:17154495-Fluorescence Resonance Energy Transfer,
pubmed-meshheading:17154495-Genes, Reporter,
pubmed-meshheading:17154495-Hepatocytes,
pubmed-meshheading:17154495-Homeodomain Proteins,
pubmed-meshheading:17154495-Humans,
pubmed-meshheading:17154495-Ligands,
pubmed-meshheading:17154495-Protein Structure, Tertiary,
pubmed-meshheading:17154495-Receptors, Cytoplasmic and Nuclear,
pubmed-meshheading:17154495-Stereoisomerism,
pubmed-meshheading:17154495-Steroidogenic Factor 1,
pubmed-meshheading:17154495-Structure-Activity Relationship,
pubmed-meshheading:17154495-Transcription Factors
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pubmed:year |
2006
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pubmed:articleTitle |
Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1.
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pubmed:affiliation |
School of Chemistry, University of Southampton, Southampton, HANTS, SO17 1BJ, UK.
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pubmed:publicationType |
Journal Article
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