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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
15
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pubmed:dateCreated |
2007-7-10
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pubmed:abstractText |
Based on the scaffold of the pharmacologically selective thyromimetic 2b, structurally a close analog to KB-141 (2a), a number of novel N-acylated-alpha-amino acid derivatives were synthesized and tested in a TR radioligand binding assay as well as in a reporter cell assay. On the basis of TRbeta(1)-isoform selectivity and affinity, as well as affinity to the reporter cell assay, 3d was selected for further studies in the cholesterol-fed rat model. In this model 3d revealed an improved therapeutic window between cholesterol and TSH lowering but decreased margins versus tachycardia compared with 2a.
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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 |
0960-894X
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pubmed:author |
pubmed-author:AgbackPeterP,
pubmed-author:BriganceRobert PRP,
pubmed-author:CaringalYolandaY,
pubmed-author:Garcia CollazoAna MariaAM,
pubmed-author:GargNeerajN,
pubmed-author:GroverGaryG,
pubmed-author:GrynfarbMarlenaM,
pubmed-author:LiYi-LinYL,
pubmed-author:LittenChrisC,
pubmed-author:MalmJohanJ,
pubmed-author:MellströmKarinK,
pubmed-author:MengWeiW,
pubmed-author:NorinThomasT,
pubmed-author:Rahimi-GhadimMahmoudM,
pubmed-author:RehnmarkStefanS,
pubmed-author:RyonoDenis EDE,
pubmed-author:SandbergJohnnyJ,
pubmed-author:WashburnWilliam NWN,
pubmed-author:ZhangMinshengM
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4131-4
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pubmed:meshHeading |
pubmed-meshheading:17543524-Amino Acids,
pubmed-meshheading:17543524-Animals,
pubmed-meshheading:17543524-CHO Cells,
pubmed-meshheading:17543524-Cholesterol, Dietary,
pubmed-meshheading:17543524-Cricetinae,
pubmed-meshheading:17543524-Cricetulus,
pubmed-meshheading:17543524-Ligands,
pubmed-meshheading:17543524-Molecular Mimicry,
pubmed-meshheading:17543524-Phenyl Ethers,
pubmed-meshheading:17543524-Phenylacetates,
pubmed-meshheading:17543524-Radioligand Assay,
pubmed-meshheading:17543524-Rats,
pubmed-meshheading:17543524-Receptors, Thyroid Hormone
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pubmed:year |
2007
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pubmed:articleTitle |
Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.
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pubmed:affiliation |
Karo Bio AB, Novum, Huddinge S-141 57, Sweden.
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pubmed:publicationType |
Journal Article
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