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Text
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URL Address
<a href="http://doi.org/10.1021/cb200092v" target="_blank" rel="noreferrer noopener">http://doi.org/10.1021/cb200092v</a>
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Pages
1096-1106
Issue
10
Volume
6
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Title
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Similarities and Differences between Two Modes of Antagonism of the Thyroid Hormone Receptor
Publisher
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Acs Chemical Biology
Date
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2011
2011-10
Subject
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androgen receptor; Biochemistry & Molecular Biology; coactivator binding; estrogen receptor; gene-expression; growth-hormone; hepatoma-cell line; hepg2; liver; nuclear receptor; small-molecule inhibitors
Creator
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Sadana P; Hwang J Y; Attia R R; Arnold L A; Neale G; Guy R K
Description
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Thyroid hormone (T3) mediates diverse physiological functions including growth, differentiation, and energy homeostasis through the thyroid hormone receptors (TR). The TR binds DNA at specific recognition sequences in the promoter regions of their target genes known as the thyroid, hormone response elements (TREs). Gene expression at TREs regulated by TRs is mediated by coregulator recruitment to the DNA bound receptor. This TR-coregulator interaction controls transcription of target genes by multiple mechanisms including covalent histone modifications and chromatin remodeling. Our previous studies identified a beta-aminoketone as a potent inhibitor of the TR-coactivator interaction. We describe here the activity of one of these inhibitors in modulating effects of T3 signaling in comparison to an established ligand-competitive inhibitor of TR, NH-3. The beta-aminoketone was found to reverse thyroid hormone induced gene expression by inhibiting coactivator recruitment at target gene promoters, thereby regulating downstream effects of thyroid hormone. While mimicking the downstream effects of NH-3 at the molecular level, the beta-aminoketone affects only a subset of the thyroid responsive signaling network. Thus antagonists directed to the coregulator binding site have distinct pharmacological properties relative to ligand-based antagonists and may provide complementary activity in vivo.
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<a href="http://doi.org/10.1021/cb200092v" target="_blank" rel="noreferrer noopener">10.1021/cb200092v</a>
Format
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Journal Article
2011
Acs Chemical Biology
androgen receptor
Arnold L A
Attia R R
Biochemistry & Molecular Biology
coactivator binding
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
estrogen receptor
gene-expression
growth-hormone
Guy R K
hepatoma-cell line
hepg2
Hwang J Y
Journal Article
Liver
Neale G
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Nuclear Receptor
Sadana P
small-molecule inhibitors