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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2006-1-9
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pubmed:abstractText |
Based on the examination of the X-ray crystallographic structures of the LBD of TRalpha and TRbeta in complex with KB-141 (2), a number of novel 4'-hydroxy bioisosteric thyromimetics were prepared. Optimal affinity and beta-selectivity (33 times), was found with a medium-sized alkyl-substituted amido group; iso-butyl (12c). It can be concluded that bioisosteric replacements of the 4'-hydroxy position represent a new promising class of TRbeta-selective synthetic thyromimetics.
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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:FärnegårdMathiasM,
pubmed-author:Garcia CollazoAna MariaAM,
pubmed-author:GargNeerajN,
pubmed-author:GrynfarbMarlenaM,
pubmed-author:HusmanBoletteB,
pubmed-author:KoehlerKonrad FKF,
pubmed-author:LiYi-LinYL,
pubmed-author:LittenChrisC,
pubmed-author:MalmJohanJ,
pubmed-author:MellströmKarinK,
pubmed-author:SandbergJohnnyJ
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
884-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16303304-Amides,
pubmed-meshheading:16303304-Crystallography, X-Ray,
pubmed-meshheading:16303304-Drug Design,
pubmed-meshheading:16303304-Humans,
pubmed-meshheading:16303304-Ligands,
pubmed-meshheading:16303304-Models, Molecular,
pubmed-meshheading:16303304-Molecular Conformation,
pubmed-meshheading:16303304-Molecular Structure,
pubmed-meshheading:16303304-Phenyl Ethers,
pubmed-meshheading:16303304-Phenylacetates,
pubmed-meshheading:16303304-Protein Conformation,
pubmed-meshheading:16303304-Protein Structure, Tertiary,
pubmed-meshheading:16303304-Structure-Activity Relationship,
pubmed-meshheading:16303304-Thyroid Hormone Receptors alpha,
pubmed-meshheading:16303304-Thyroid Hormone Receptors beta,
pubmed-meshheading:16303304-Thyroid Hormones,
pubmed-meshheading:16303304-Triiodothyronine
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pubmed:year |
2006
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pubmed:articleTitle |
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.
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pubmed:affiliation |
Karo Bio AB, Novum, Huddinge S-141 57, Sweden.
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pubmed:publicationType |
Journal Article,
Comparative Study
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