Evidence map›Paper›PMID 24379833›Full record

ArticleObstetrics and gynecology international2013

G protein-coupled estrogen receptor-selective ligands modulate endometrial tumor growth.

Whitney K Petrie, Megan K Dennis, Chelin Hu, Donghai Dai, Jeffrey B Arterburn, Harriet O Smith, Helen J Hathaway, Eric R Prossnitz

Open access · goldAbstract read
In one paragraph

Article in Obstetrics and gynecology international, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 86 papers.

0numbers the graph read from it
0cells of the map it votes in
86citing papers in PubMed
10.2field-weighted citation impact, top 1% 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

86 citing papers in PubMed, 162 citations in OpenAlex.

  1. Trial
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  9. The Role of Estrogen across Multiple Disease Mechanisms.Current issues in molecular biology · 2024
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  15. Deciphering the Influence of Estradiol and Estrogen Receptors on Cognitive Function: A Bibliometric Analysis and Emerging Research Trends.Medical science monitor : international medical journal of experimental and clinical research · 2023
    Article
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26 more citing papers are in PubMed but not listed here.

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

8 authors at 4 institutions in 1 country.

Whitney K PetrieDepartment of Cell Biology and Physiology and UNM Cancer Center, The University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA.
Megan K DennisDepartment of Cell Biology and Physiology and UNM Cancer Center, The University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA.
Chelin HuDepartment of Cell Biology and Physiology and UNM Cancer Center, The University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA.
Donghai DaiDepartment of Obstetrics and Gynecology, UNM Cancer Center, The University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA ; Department of Obstetrics and Gynecology, University of Iowa Carver College of Medicine, Iowa City, IA 52242, USA.
Jeffrey B ArterburnDepartment of Chemistry and Biochemistry, New Mexico State University, Las Cruces, NM 88003, USA.
Harriet O SmithDepartment of Cell Biology and Physiology and UNM Cancer Center, The University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA ; Department of Obstetrics and Gynecology, UNM Cancer Center, The University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA ; Department of Obstetrics and Gynecology and Women's Health, Albert Einstein College of Medicine and Montefiore Medical Center, Bronx, NY 10461, USA.
Helen J HathawayDepartment of Cell Biology and Physiology and UNM Cancer Center, The University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA.
Eric R ProssnitzDepartment of Cell Biology and Physiology and UNM Cancer Center, The University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA.
University of New Mexico · USAlbert Einstein College of Medicine · USNew Mexico State University · USUniversity of Iowa · US

Funding

G protein-coupled estrogen receptor GPER and breast carcinogenesisR01CA163890 · NCI · UNIVERSITY OF NEW MEXICO HEALTH SCIS CTR · PI PROSSNITZ, ERIC R · 2012 to 2023
$3.3M
Development of GPR30-Selective LigandsR01CA127731 · NCI · UNIVERSITY OF NEW MEXICO · PI ARTERBURN, JEFFREY B, OPREA, TUDOR I · 2008 to 2012
$1.7M
The Role of GPR30 in Advanced Endometrial CancerR01CA118743 · NCI · UNIVERSITY OF NEW MEXICO · PI PROSSNITZ, ERIC R · 2007 to 2009
$855k
NCI NIH HHS R01 CA118743NCI NIH HHS R01 CA127731NCI NIH HHS R01 CA163890
6 · The paper itself

Abstract

Endometrial carcinoma is the most common cancer of the female reproductive tract. GPER/GPR30 is a 7-transmembrane spanning G protein-coupled receptor that has been identified as the third estrogen receptor, in addition to ERα and ERβ. High GPER expression is predictive of poor survival in endometrial and ovarian cancer, but despite this, the estrogen-mediated signaling pathways and specific estrogen receptors involved in endometrial cancer remain unclear. Here, employing ERα-negative Hec50 endometrial cancer cells, we demonstrate that GPER mediates estrogen-stimulated activation of ERK and PI3K via matrix metalloproteinase activation and subsequent transactivation of the EGFR and that ER-targeted therapeutic agents (4-hydroxytamoxifen, ICI182,780/fulvestrant, and Raloxifene), the phytoestrogen genistein, and the "ERα-selective" agonist propylpyrazole triol also function as GPER agonists. Furthermore, xenograft tumors of Hec50 cells yield enhanced growth with G-1 and estrogen, the latter being inhibited by GPER-selective pharmacologic antagonism with G36. These results have important implications with respect to the use of putatively ER-selective ligands and particularly for the widespread long-term use of "ER-targeted" therapeutics. Moreover, our findings shed light on the potential mechanisms of SERM/SERD side effects reported in many clinical studies. Finally, our results provide the first demonstration that pharmacological inhibition of GPER activity in vivo prevents estrogen-mediated tumor growth.

Identifiers

PMID24379833
PMCPMC3863501
OpenAlexW1976678368

What OpenQuestion holds

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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.