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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2003-2-4
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pubmed:abstractText |
In this communication, we wish to describe the discovery of a novel series of 6-azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the beta(1)-isoform of the thyroid receptor family. Structure-activity relationship studies on the 3,5- and 3'-positions provided compounds with enhanced TR beta affinity and selectivity. Key binding interactions between the 6-azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
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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 |
0960-894X
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pubmed:author |
pubmed-author:AmmiratiMark JMJ,
pubmed-author:ChiangPhoebeP,
pubmed-author:ChrunykBoris ABA,
pubmed-author:CorneliusPeterP,
pubmed-author:DaSilva-JardinePaulP,
pubmed-author:DanleyDennis EDE,
pubmed-author:DowRobert LRL,
pubmed-author:HankRichard FRF,
pubmed-author:HargroveDiane MDM,
pubmed-author:LeMottePeter KPK,
pubmed-author:LeeEunsunE,
pubmed-author:NewsomeWilliam PWP,
pubmed-author:PaightErnest SES,
pubmed-author:PanditJayvardhanJ,
pubmed-author:PattersonTerrell ATA,
pubmed-author:RosnerMichele HMH,
pubmed-author:SchneiderSteven RSR,
pubmed-author:SchulteGayle KGK,
pubmed-author:SimonsSamuel PSP,
pubmed-author:SpitzerJosephineJ,
pubmed-author:SwickAndrew GAG,
pubmed-author:TateBonnie FBF
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pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
379-82
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:12565933-Crystallography, X-Ray,
pubmed-meshheading:12565933-Drug Design,
pubmed-meshheading:12565933-Humans,
pubmed-meshheading:12565933-Indicators and Reagents,
pubmed-meshheading:12565933-Ligands,
pubmed-meshheading:12565933-Models, Molecular,
pubmed-meshheading:12565933-Molecular Mimicry,
pubmed-meshheading:12565933-Protein Binding,
pubmed-meshheading:12565933-Protein Conformation,
pubmed-meshheading:12565933-Receptors, Thyroid Hormone,
pubmed-meshheading:12565933-Structure-Activity Relationship,
pubmed-meshheading:12565933-Thyroid Hormones,
pubmed-meshheading:12565933-Uracil
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pubmed:year |
2003
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pubmed:articleTitle |
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics.
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pubmed:affiliation |
Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA. robert_l_dow@groton.pfizer.com
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pubmed:publicationType |
Journal Article
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