Article
Medicine, Research & Experimental
Carlotta Boscaro, Giovanni Eugenio Ramaschi, Lucia Trevisi, Andrea Cignarella, Chiara Bolego
Summary: miR-206 can interfere with GPER-mediated signaling and cell motility, and has the potential to act as pathway-selective antagonists in estrogen-dependent EOC.
Review
Biochemistry & Molecular Biology
Marta Justyna Koziel, Agnieszka Wanda Piastowska-Ciesielska
Summary: Ovarian cancer, a common cancer in women, is believed to be influenced by hormonal imbalance. Estrogens, a group of hormones with important roles in physiological and pathological processes, are involved in regulating proliferation, invasiveness, and the epithelial to mesenchymal transition in ovarian cancer. Estrogen signaling also plays a role in the biology of the tumor microenvironment. This review provides information on estrogen receptors, estrogens, and their association with the tumor microenvironment, as well as changes in estrogen receptor expression following exposure to various environmental chemicals.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Cell Biology
Nan Han, Sabine Heublein, Udo Jeschke, Christina Kuhn, Anna Hester, Bastian Czogalla, Sven Mahner, Miriam Rottmann, Doris Mayr, Elisa Schmoeckel, Fabian Trillsch
Summary: The study found a positive correlation between GPER and H3K4me3 expression in ovarian cancer patients, with patients overexpressing both having improved overall survival. Activation of GPER led to increased H3K4me3 and p-ERK1/2 levels, as well as decreased cell proliferation and migration, while antagonizing GPER activity had opposite effects. The interaction between GPER and H3K4me3 is of prognostic significance and GPER agonists like G1 have potential as a therapeutic approach for ovarian cancer.
Review
Cell Biology
Richard A. Pepermans, Geetanjali Sharma, Eric R. Prossnitz
Summary: Estrogen plays crucial roles in various cancers, metabolism, and immune regulation. The G protein-coupled estrogen receptor (GPER) has been found to contribute to endocrine therapy resistance in breast cancer and has potential therapeutic value in targeting other diseases such as obesity and diabetes. Ongoing clinical trials are exploring the use of GPER-selective agonists like G-1 in combination with immune checkpoint inhibition for cancer treatment.
Article
Multidisciplinary Sciences
Zulvikar Syambani Ulhaq, Gita Vita Soraya, Alvi Milliana, William Ka Fai Tse
Summary: This study suggests that GPER gene polymorphisms and expression levels are associated with cancer predisposition and progression, especially in the Asian population. rs3808350 and rs3808351 may serve as potential biomarkers for cancer screening, while rs3808351 and GPER expression could be used to assess the prognosis of cancer patients. Further biological studies are needed to confirm these findings.
Article
Environmental Sciences
Chen Sang, Yu Song, Tong-wang Jin, Shuo Zhang, Linyan Fu, Yi Zhao, Xinxin Zou, Zhe Wang, Hui Gao, Sijin Liu
Summary: The study found that BPA can stimulate proliferation and metastasis of ovarian cancer cells by upregulating various proteins through the ER alpha signaling pathway. These results provide new insights into the carcinogenic effects of BPA on ovarian cancer.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2021)
Article
Cardiac & Cardiovascular Systems
Janet R. Manning, Dharendra Thapa, Manling Zhang, Michael W. Stoner, John C. Sembrat, Mauricio Rojas, Iain Scott
Summary: This study reveals differences in mitochondrial protein acetylation levels in male and female hearts, with an increase in GCN5L1 levels associated with GPER activation. These findings contribute to understanding the metabolic differences between male and female hearts.
AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY
(2022)
Review
Environmental Sciences
Yu Qie, Weiping Qin, Keda Zhao, Chang Liu, Lixia Zhao, Liang-Hong Guo
Summary: Many environmental chemicals exert estrogenic effects by activating estrogen receptors and related receptors, with GPER playing a crucial role in mediating these effects. Even at low concentrations, these chemicals can affect cellular functions, leading to disease progression and adverse effects.
ENVIRONMENTAL POLLUTION
(2021)
Article
Cell Biology
Francesca Cirillo, Marianna Talia, Maria Francesca Santolla, Michele Pellegrino, Domenica Scordamaglia, Asia Spinelli, Salvatore De Rosis, Francesca Giordano, Lucia Muglia, Azzurra Zicarelli, Marika Di Dio, Damiano Cosimo Rigiracciolo, Anna Maria Miglietta, Gianfranco Filippelli, Ernestina Marianna De Francesco, Antonino Belfiore, Rosamaria Lappano, Marcello Maggiolini
Summary: In this study, the researchers used CRISPR/Cas9 technology to knock out GPER expression in TNBC cells and made new mechanistic and biological discoveries. They found that GPER KO led to anti-proliferative and pro-apoptotic effects in TNBC cells, as well as impairments in migratory effects in cancer-associated fibroblasts. These findings suggest that GPER may be a valuable target for comprehensive therapeutic approaches in halting TNBC progression.
CELL DEATH DISCOVERY
(2023)
Review
Biochemistry & Molecular Biology
Aliyu Muhammad, Gilead Ebiegberi Forcados, Abdurrahman Pharmacy Yusuf, Murtala Bello Abubakar, Idris Zubairu Sadiq, Isra Elhussin, Md. Abu Talha Siddique, Suleiman Aminu, Rabiatu Bako Suleiman, Yakubu Saddeeq Abubakar, Babangida Sanusi Katsayal, Clayton C. C. Yates, Sunila Mahavadi
Summary: This review critically examines the role of G-protein-coupled estrogen receptor (GPER) in diabetes mellitus and malignancy, highlighting the potential for GPER as a therapeutic target for management of these diseases. The expression patterns of GPER in diabetic models are currently lacking, while in various malignancies the expression of GPER appears to be complex and debatable. Further research is needed to investigate the expression patterns of GPER and its relationship with signaling pathways in diabetes mellitus and various malignancies.
Review
Cell Biology
Keith A. Hall, Edward J. Filardo
Summary: Estrogens play a crucial role in the pathogenesis of various cancers, especially in relation to environmental estrogens and GPER receptors. However, the current antiestrogen therapy for breast cancer does not consider these factors, indicating the need for a more holistic approach, such as targeting GPER receptors.
Review
Pharmacology & Pharmacy
Jeffrey B. Arterburn, Eric R. Prossnitz
Summary: The actions of estrogens and related estrogenic molecules are complex and multifaceted in both sexes. These molecules target pathways that produce and respond to estrogens, and multiple receptors are involved in the responses. In particular, the G protein-coupled estrogen receptor (GPER) plays important roles in physiological responses to estrogenic compounds and has therapeutic implications for various diseases.
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Alexandra Varga, Eva Marton, Arnold Markovics, Andras Penyige, Istvan Balogh, Balint Nagy, Melinda Szilagyi
Summary: MicroRNAs play an important role in ovarian cancer, and their high expression is correlated with ER α expression. MiR-30d-5p can reduce cell proliferation and increase sensitivity to estrogen, while regulating the expression of SOX4 and the PI3K/AKT pathway. MiR-30d-5p or AZD8835 can sensitize PEO1 cells to tamoxifen.
Review
Endocrinology & Metabolism
Nicolas Chevalier, Charlotte Hinault, Stephan Clavel, Rachel Paul-Bellon, Patrick Fenichel
Summary: GPER/GPR30, a novel estrogen-binding protein structurally distinct from classic estrogen receptors, is involved in male germ cell proliferation in testicular germ cell cancers. Overexpression of GPER/GPR30 in seminomas, potentially linked to genetic variations, suggests it as a therapeutic target.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Fujie Xu, Jipeng Ma, Xiaowu Wang, Xiaoya Wang, Weiyi Fang, Jingwei Sun, Zilin Li, Jincheng Liu
Summary: This article summarizes the function, tissue localization, ligands, and signaling pathways of GPER in different physiological and diseased conditions. It emphasizes the role of GPER in vascular pathology and physiology and presents evidence of GPER as a promising therapeutic target in hypertension, pulmonary hypertension, and atherosclerosis.