Source:http://linkedlifedata.com/resource/pubmed/id/15590892
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2005-2-10
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pubmed:abstractText |
We investigated the effects of phenolic and phenol compounds on 3,3',5-L-125I-triiodothyronine (125I-T3) binding to purified Xenopus laevis transthyretin (xTTR) and to the ligand-binding domain of X. laevis thyroid hormone receptor beta (xTR LBD), on T3-induced metamorphosis in X. laevis tadpoles and on the induction of T3-dependent reporter gene in a X. laevis cell line. Of the halogenated phenolic and phenol compounds tested, 3,3',5-trichlorobisphenol A and 2,4,6-triiodophenol, respectively, were the most potent competitors of 125I-T3 binding to both xTTR and xTR LBD. Most of the halogenated compounds had stronger interactions with xTTR than with xTR LBD. Generally, chlorinated derivatives with a greater degree of chlorination were more efficient competitors of T3 binding to xTTR and xTR LBD. Structures with a halogen in either ortho position or in both ortho positions, with respect to the hydroxy group, were more efficient competitors. 3,3',5-Trichlorobisphenol A and 2,4,6-triiodophenol acted as T3 antagonists in the X. laevis tadpole metamorphosis assay. Interestingly, o-t-butylphenol and 2-isopropylphenol, for which xTTR and xTR LBD had weak or no significant affinity, showed T3 antagonist activity in the metamorphosis assay. T3 antagonist activities of all these chemicals except for o-t-butylphenol were verified by T3-dependent reporter gene assay. Our results suggest that some phenolic and phenol compounds target the process of T3 binding to xTTR and xTR and/or an unknown process, and that they interfere with the intracellular T3 signaling pathway.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Luciferases,
http://linkedlifedata.com/resource/pubmed/chemical/Phenols,
http://linkedlifedata.com/resource/pubmed/chemical/Prealbumin,
http://linkedlifedata.com/resource/pubmed/chemical/Thyroid Hormone Receptors beta,
http://linkedlifedata.com/resource/pubmed/chemical/Thyroid Hormones,
http://linkedlifedata.com/resource/pubmed/chemical/Triiodothyronine
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1096-6080
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
84
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
29-37
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pubmed:dateRevised |
2010-9-17
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pubmed:meshHeading |
pubmed-meshheading:15590892-Animals,
pubmed-meshheading:15590892-Drug Interactions,
pubmed-meshheading:15590892-Genes, Reporter,
pubmed-meshheading:15590892-Larva,
pubmed-meshheading:15590892-Luciferases,
pubmed-meshheading:15590892-Metamorphosis, Biological,
pubmed-meshheading:15590892-Phenols,
pubmed-meshheading:15590892-Prealbumin,
pubmed-meshheading:15590892-Reverse Transcriptase Polymerase Chain Reaction,
pubmed-meshheading:15590892-Thyroid Diseases,
pubmed-meshheading:15590892-Thyroid Hormone Receptors beta,
pubmed-meshheading:15590892-Thyroid Hormones,
pubmed-meshheading:15590892-Triiodothyronine,
pubmed-meshheading:15590892-Xenopus laevis
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pubmed:year |
2005
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pubmed:articleTitle |
In vitro and in vivo analysis of the thyroid disrupting activities of phenolic and phenol compounds in Xenopus laevis.
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pubmed:affiliation |
Department of Biology, Faculty of Science, Shizuoka University, Shizuoka 422-8529, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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