Evidence map›Paper›PMID 34552311›Full record

ArticleMedicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents2020

Repression of the transcriptional activity of ERRα with sequence-specific DNA-binding polyamides.

Chien-Yu Chen, Yang Li, Tiezheng Jia, Lina He, Alissa A Hare, Amanda Silberstein, John Gallagher, Thomas F Martinez, Joseph W Stiles, Bogdan Olenyuk and 2 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
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

3 citing papers in PubMed.

  1. Review
  2. Article
  3. Transformation of SOX9Scientific reports · 2021
    Article
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

12 authors.

Chien-Yu ChenPharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90033, USA.
Yang LiPharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90033, USA.
Tiezheng JiaDivision of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA.
Lina HePharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90033, USA.
Alissa A HareDivision of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA.
Amanda SilbersteinDivision of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA.
John GallagherPharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90033, USA.
Thomas F MartinezDivision of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA.
Joseph W StilesPharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90033, USA.ORCID 0000-0001-5480-2074
Bogdan OlenyukPharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90033, USA.
Peter B DervanDivision of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA.
Bangyan L StilesPharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90033, USA.

Funding

USC RESEARCH CENTER FOR LIVER DISEASES: PILOT PROGRAMSP30DK048522 · NIDDK · UNIVERSITY OF SOUTHERN CALIFORNIA · PI HAMM-ALVAREZ, SARAH F · 1995 to 2020
$21.8M
The role of PTEN and AKT2 in the malignant transformation of liver progenitor celR01CA154986 · NCI · UNIVERSITY OF SOUTHERN CALIFORNIA · PI STILES, BANGYAN · 2013 to 2017
$1.7M
Interrogation of Androgen Receptor:Forkhead Interaction Using Py-Im PolyamidesF31CA159896 · NCI · CALIFORNIA INSTITUTE OF TECHNOLOGY · PI MARTINEZ, THOMAS FARID · 2011 to 2014
$165k
NCI NIH HHS F31 CA159896NCI NIH HHS R01 CA154986NIDDK NIH HHS P30 DK048522
6 · The paper itself

Abstract

The orphan nuclear receptors estrogen-related receptors (ERRs) bind to the estrogen-related receptor response element (ERRE) to regulate transcriptional programs in cellular metabolism and cancer cell growth. In this study, we evaluated the potential for a pyrrole-imidazole polyamide to block ERRα binding to ERREs to inhibit gene expression. We demonstrated that the ERRE-targeted polyamide 1 blocked the binding of ERRα to the consensus ERRE and reduced the transcriptional activity of ERRα in cell culture. We further showed that inhibiting ERRα transcriptional activity with polyamide 1 led to reduced mitochondrial oxygen consumption, a primary biological effect regulated by ERRα. Finally, our data demonstrated that polyamide 1 is an inhibitor for cancer cell growth.

Indexed as

ERRαMitochondriaPyrrole-imidazole polyamide

Identifiers

PMID34552311
PMCPMC8455084

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Registered trials

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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.