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40
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Text
A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text.
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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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
Pages
1096-1106
Issue
10
Volume
6
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Dublin Core
The Dublin Core metadata element set is common to all Omeka records, including items, files, and collections. For more information see, http://dublincore.org/documents/dces/.
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
A point or period of time associated with an event in the lifecycle of the resource
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
An account of the resource
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.
Identifier
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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
-
Text
A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text.
URL Address
<a href="http://doi.org/10.1021/acschembio.0c00380" target="_blank" rel="noreferrer noopener">http://doi.org/10.1021/acschembio.0c00380</a>
ISSN
1554-8937
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<a href="http://neomed.idm.oclc.org/login?url=http://doi.org/10.1021/acschembio.0c00380" target="_blank" rel="noreferrer noopener">NEOMED Full-text Holding (if available) - Proxy DOI: 10.1021/acschembio.0c00380</a>
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Update Year & Number
September 2020 List
NEOMED College
NEOMED College of Pharmacy
NEOMED Department
Department of Pharmaceutical Sciences
Dublin Core
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Title
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Examining targeted protein degradation from physiological and analytical perspectives: Enabling translation between cells and subjects.
Publisher
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ACS Chemical Biology
Date
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2020
2020-09-30
Creator
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Daurio NA;Zhou H;Chen Y;Sheth PR;Imbriglio JE;McLaren DG;Tawa P;Rachdaoui N;Previs MJ;Kasumov T;O'Neil J;Previs SF
Description
An account of the resource
The ability to target specific proteins for degradation may open a new door toward developing therapeutics. Although effort in chemistry is essential for advancing this modality, i.e., one needs to generate proteolysis targeting chimeras (bifunctional molecules, also referred to as PROTACS) or "molecular glues" to accelerate protein degradation, we suspect that investigations could also benefit by directing attention toward physiological regulation surrounding protein homeostasis, including the methods that can be used to examine changes in protein kinetics. This perspective will first consider some metabolic scenarios that might be of importance when one aims to change protein abundance by increasing protein degradation. Specifically, could protein turnover impact the apparent outcome? We will then outline how to study protein dynamics by coupling stable isotope tracer methods with mass spectrometry-based detection; since the experimental conditions could have a dramatic effect on protein turnover, special attention is directed toward the application of methods for quantifying protein kinetics using in vitro and in vivo models. Our goal is to present key concepts that should enable mechanistically informed studies which test targeted protein degradation strategies.
Identifier
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<a href="http://doi.org/10.1021/acschembio.0c00380" target="_blank" rel="noreferrer noopener">10.1021/acschembio.0c00380</a>
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
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journalArticle
2020
Acs Chemical Biology
Chen Y
Daurio NA
Department of Pharmaceutical Sciences
Imbriglio JE
journalArticle
Kasumov T
McLaren DG
NEOMED College of Pharmacy
O'Neil J
Previs MJ
Previs SF
Rachdaoui N
September 2020 List
Sheth PR
Tawa P
Zhou H