Evidence map›Paper›PMID 21815645›Full record

ArticleACS chemical biology2011

Similarities and differences between two modes of antagonism of the thyroid hormone receptor.

Prabodh Sadana, Jong Yeon Hwang, Ramy R Attia, Leggy A Arnold, Geoffrey Neale, R Kiplin Guy

Abstract read
In one paragraph

Article in ACS chemical biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.6field-weighted citation impact, top 16% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed, 19 citations in OpenAlex.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors at 2 institutions in 1 country.

Prabodh SadanaDepartment of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Jong Yeon Hwang
Ramy R Attia
Leggy A Arnold
Geoffrey Neale
R Kiplin Guy
Ohio University · USUniversity of Wisconsin–Milwaukee · US

Funding

Novel Inhibitors of Nuclear Receptor FunctionR01DK058080 · NIDDK · UNIVERSITY OF CALIFORNIA SAN FRANCISCO · PI GUY, RODNEY KIPLIN · 2001 to 2011
$3.0M
NIDDK NIH HHS R01 DK058080NIDDK NIH HHS R01 DK58080
6 · The paper itself

Abstract

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 β-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 β-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 β-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.

Indexed as

Cell LineGene Expression RegulationHep G2 CellsHumansKetonesReceptors, Thyroid HormoneSignal TransductionSulfonesTriiodothyronineKetonesReceptors, Thyroid HormoneSJ 000311413SulfonesTriiodothyronine

Identifiers

PMID21815645
PMCPMC3199310
OpenAlexW2086985369

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.