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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2005-2-16
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pubmed:abstractText |
In order to develop agonist ligands that are specific for the estrogen-related receptors ERRbeta/gamma, a hydrazone with a 4-hydroxy group at one phenyl ring and a 4-diethylamino moiety at the other phenyl ring was synthesized. We demonstrate that compound 3 (DY131; N'-{(1E)-[4-(diethylamino)phenyl]methylene}-4-hydroxybenzohydrazide) effectively and selectively activates ERRbeta/gamma. DY131 had no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta). This work defines a convenient synthesis for a novel and selective pharmacologic tool that can be used to elucidate the biological activities of ERRbeta/gamma.
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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/ERRalpha estrogen-related receptor,
http://linkedlifedata.com/resource/pubmed/chemical/ESRRB protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Esrrg protein, mouse,
http://linkedlifedata.com/resource/pubmed/chemical/Hydrazines,
http://linkedlifedata.com/resource/pubmed/chemical/Hydrazones,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cytoplasmic and Nuclear,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Estrogen
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1311-3
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pubmed:dateRevised |
2006-10-7
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pubmed:meshHeading |
pubmed-meshheading:15713377-Animals,
pubmed-meshheading:15713377-Cell Line,
pubmed-meshheading:15713377-Dose-Response Relationship, Drug,
pubmed-meshheading:15713377-Drug Evaluation, Preclinical,
pubmed-meshheading:15713377-Humans,
pubmed-meshheading:15713377-Hydrazines,
pubmed-meshheading:15713377-Hydrazones,
pubmed-meshheading:15713377-Ligands,
pubmed-meshheading:15713377-Mice,
pubmed-meshheading:15713377-Molecular Mimicry,
pubmed-meshheading:15713377-Molecular Structure,
pubmed-meshheading:15713377-Receptors, Cytoplasmic and Nuclear,
pubmed-meshheading:15713377-Receptors, Estrogen,
pubmed-meshheading:15713377-Structure-Activity Relationship,
pubmed-meshheading:15713377-Transfection
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pubmed:year |
2005
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pubmed:articleTitle |
Identification of an agonist ligand for estrogen-related receptors ERRbeta/gamma.
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pubmed:affiliation |
Department of Gene regulation and Drug Discovery, The Beckman Research Institute, The City of Hope National Medical Center, The Gonda Diabetes and Genetic Research Center, Duarte, CA 91010, USA.
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pubmed:publicationType |
Journal Article
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