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Updated: Jan 4, 2026

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
Published on: March 17, 2016
G Protein-Coupled Estrogen Receptor: A Potential Therapeutic Target in Cancer
Shen Xu1, Shan Yu2,3, Daming Dong1
1Department of Orthopedics, The First Affiliated Hospital of Harbin Medical University, Harbin, China.
Abstract:
The G protein-coupled estrogen receptor (GPER) is a seven-transmembrane-domain receptor that mediates non-genomic estrogen related signaling. After ligand activation, GPER triggers multiple downstream pathways that exert diverse biological effects on the regulation of cell growth, migration and programmed cell death in a variety of tissues. A significant correlation between GPER and the progression of multiple cancers has likewise been reported. Therefore, a better understanding of the role GPER plays in cancer biology may lead to the identification of novel therapeutic targets, especially among estrogen-related cancers. Here, we review cell signaling and detail the functions of GPER in malignancies.
Insights
The G protein-coupled estrogen receptor (GPER) regulates cell functions and is linked to cancer progression. Understanding GPER in malignancies may reveal new therapeutic targets for estrogen-related cancers.
Area of Science:
- Endocrinology
- Molecular Biology
- Oncology
Background:
- The G protein-coupled estrogen receptor (GPER) is a key mediator of non-genomic estrogen signaling.
- GPER activation influences cell growth, migration, and apoptosis across various tissues.
- A strong association exists between GPER and the progression of numerous cancers.
Purpose of the Study:
- To review the cell signaling pathways regulated by GPER.
- To detail the specific functions of GPER in the context of cancer biology.
- To explore the potential of GPER as a therapeutic target in malignancies.
Main Methods:
- Literature review of GPER signaling.
- Analysis of GPER's role in different cancer types.
- Synthesis of current research on GPER and cancer.
Main Results:
- GPER mediates diverse cellular responses through multiple downstream pathways.
- GPER's involvement in cancer progression is increasingly recognized.
- Estrogen-related cancers show a significant correlation with GPER.
Conclusions:
- GPER plays a critical role in regulating cellular processes relevant to cancer.
- Targeting GPER may offer novel therapeutic strategies for cancer treatment.
- Further research into GPER functions can identify new avenues for oncology drug development.
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