scholarly journals G-protein Coupled Estrogen Receptor 1 Expression in Primary Breast Cancers and Its Correlation with Clinicopathological Variables

2011 ◽  
Vol 14 (3) ◽  
pp. 185 ◽  
Author(s):  
Hao-jun Luo ◽  
Ping Luo ◽  
Guang-lun Yang ◽  
Qiong-le Peng ◽  
Man-ran Liu ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
G Protein ◽  
Breast Cancers ◽  
G Protein Coupled ◽  
Clinicopathological Variables ◽  
Estrogen Receptor 1

scholarly journals Berberine Inhibits MDA-MB-231 Cells as an Agonist of G Protein-Coupled Estrogen Receptor 1

2021 ◽  
Vol 22 (21) ◽  
pp. 11466
Author(s):  
Miaomiao Qi ◽  
Xiang Liu ◽  
Ying Zhou ◽  
Haoyu Wang ◽  
Ying Zhao ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
G Protein ◽  
Nuclear Translocation ◽  
Inhibitory Effect ◽  
Isoquinoline Alkaloid ◽  
Breast Cancers ◽  
Sequestosome 1 ◽  
Promotional Effect ◽  
G Protein Coupled ◽  
Estrogen Receptor 1

G protein-coupled estrogen receptor 1 (GPER1) is a potential therapeutic target for treating triple-negative breast cancers (TNBC). However, modulators for GPER1 that can be used to treat TNBC have not appeared. Berberine (BBR) is a bioactive isoquinoline alkaloid with high oral safety. In recent years, BBR has shown an inhibitory effect on TNBC tumors such as MDA-MB-231, but the molecular target remains unclear, which hinders related clinical research. Our work proved that BBR is a modulator of GPER1 that can inhibit cell viability, migration, and autophagy of MDA-MB-231 cells. The inhibitory effect of BBR on MDA-MB-231 cells has a dependence on estrogen levels. Although BBR promoted the proteasome, which is a major factor in the degradation of GPER1, it could still induce the protein level of GPER1. Correspondingly, the transcription of cellular communication network factor 2 (CCN2) was promoted. BBR could bind to GPER1 directly and change the secondary structure of GPER1, as in the case of 17β-estradiol (E2). In addition, BBR induced not only a high degree of co-localization of GPER1 and microtubule-associated protein 1 light chain 3 (MAP1LC3), but also the accumulation of sequestosome 1 (SQSTM1/p62) by the inhibition of the nuclear translocation of the nuclear factor-kappa B (NF-κB) subunit (RELA/p65), which indicates NF-κB inhibition and anti-cancer effects. This result proved that the promotional effect of BBR on the GPER1/NF-κB pathway was closely related to its inhibitory effect on autophagy, which may serve as a new mechanism by which to explain the inhibitory effect of BBR on MDA-MB-231 cells and expand our understanding of the function of both BBR and GPER1.

scholarly journals G Protein-Coupled Estrogen Receptor 1 (GPER) as a Novel Target for Schizophrenia Drug Treatment

2020 ◽  
Vol 1 (1) ◽  
Author(s):  
Danielle S Macêdo ◽  
Lia Lira Olivier Sanders ◽  
Raimunda das Candeias ◽  
Cyntia de Freitas Montenegro ◽  
David Freitas de Lucena ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
G Protein ◽  
Brain Inflammation ◽  
Antipsychotic Treatment ◽  
New Class ◽  
Estrogen Receptor Modulators ◽  
Novel Target ◽  
G Protein Coupled ◽  
Estrogen Receptor 1

Abstract The observation that a person’s sex influences the onset age of schizophrenia, the course of the disease, and antipsychotic treatment response suggests a possible role for estrogen receptors in the pathophysiology of schizophrenia. Indeed, treatment with adjunctive estrogen or selective estrogen receptor modulators (SERMs) are known to reduce schizophrenia symptoms. While estrogen receptors (ER)α and ERβ have been studied, a third and more recently discovered estrogen receptor, the G protein-coupled estrogen receptor 1 (GPER), has been largely neglected. GPER is a membrane receptor that regulates non-genomic estrogen functions, such as the modulation of emotion and inflammatory response. This review discusses the possible role of GPER in brain impairments seen in schizophrenia and in its potential as a therapeutic target. We conducted a comprehensive literature search in the PubMed/MEDLINE database, using the following search terms: “Schizophrenia,” “Psychosis,” “GPER1 protein,” “Estrogen receptors,” “SERMS,” “GPER1 agonism, “Behavioral symptoms,” “Brain Inflammation.” Studies involving GPER in schizophrenia, whether preclinical or human studies, have been scarce, but the results are encouraging. Agonism of the GPER receptor could prove to be an essential mechanism of action for a new class of “anti-schizophrenia” drugs.

scholarly journals G Protein-Coupled Estrogen Receptor in Cancer and Stromal Cells: Functions and Novel Therapeutic Perspectives

Cells ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 672
Author(s):  
Richard A. Pepermans ◽  
Geetanjali Sharma ◽  
Eric R. Prossnitz
Keyword(s):  
Estrogen Receptor ◽  
G Protein ◽  
Inflammatory Diseases ◽  
Therapy Resistance ◽  
Breast Cancers ◽  
Obesity And Diabetes ◽  
Therapeutic Value ◽  
Health And Disease ◽  
Multiple Cells ◽  
G Protein Coupled

Estrogen is involved in numerous physiological and pathophysiological systems. Its role in driving estrogen receptor-expressing breast cancers is well established, but it also has important roles in a number of other cancers, acting both on tumor cells directly as well as in the function of multiple cells of the tumor microenvironment, including fibroblasts, immune cells, and adipocytes, which can greatly impact carcinogenesis. One of its receptors, the G protein-coupled estrogen receptor (GPER), has gained much interest over the last decade in both health and disease. Increasing evidence shows that GPER contributes to clinically observed endocrine therapy resistance in breast cancer while also playing a complex role in a number of other cancers. Recent discoveries regarding the targeting of GPER in combination with immune checkpoint inhibition, particularly in melanoma, have led to the initiation of the first Phase I clinical trial for the GPER-selective agonist G-1. Furthermore, its functions in metabolism and corresponding pathophysiological states, such as obesity and diabetes, are becoming more evident and suggest additional therapeutic value in targeting GPER for both cancer and other diseases. Here, we highlight the roles of GPER in several cancers, as well as in metabolism and immune regulation, and discuss the therapeutic value of targeting this estrogen receptor as a potential treatment for cancer as well as contributing metabolic and inflammatory diseases and conditions.

scholarly journals The G protein-coupled estrogen receptor 1 (GPER-1) contributes to the proliferation and survival of mantle cell lymphoma cells

Haematologica ◽  
2015 ◽  
Vol 100 (11) ◽  
pp. e458-e461 ◽  
Author(s):  
M. Rudelius ◽  
H. Rauert-Wunderlich ◽  
E. Hartmann ◽  
E. Hoster ◽  
M. Dreyling ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Mantle Cell Lymphoma ◽  
G Protein ◽  
Cell Lymphoma ◽  
Lymphoma Cells ◽  
Mantle Cell ◽  
G Protein Coupled ◽  
Estrogen Receptor 1

Expression pattern of estrogen receptors α and β and G-protein-coupled estrogen receptor 1 in the human testis

2014 ◽  
Vol 142 (4) ◽  
pp. 421-432 ◽  
Author(s):  
Daniela Fietz ◽  
Clara Ratzenböck ◽  
Katja Hartmann ◽  
Oksana Raabe ◽  
Sabine Kliesch ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
G Protein ◽  
Expression Pattern ◽  
Human Testis ◽  
G Protein Coupled ◽  
Estrogen Receptor 1

scholarly journals Hetero-oligomeric Complex between the G Protein-coupled Estrogen Receptor 1 and the Plasma Membrane Ca2+-ATPase 4b

2015 ◽  
Vol 290 (21) ◽  
pp. 13293-13307 ◽  
Author(s):  
Quang-Kim Tran ◽  
Mark VerMeer ◽  
Michelle A. Burgard ◽  
Ali B. Hassan ◽  
Jennifer Giles
Keyword(s):  
Estrogen Receptor ◽  
Plasma Membrane ◽  
G Protein ◽  
Oligomeric Complex ◽  
G Protein Coupled ◽  
Estrogen Receptor 1

scholarly journals G-Protein-coupled Estrogen Receptor 1 Agonist G-1 Perturbs Sunitinib Resistance-related Phosphoproteomic Signatures in Renal Cell Carcinoma

2021 ◽  
Vol 18 (3) ◽  
pp. 207-220
Author(s):  
SHAO-KUAN CHEN ◽  
YEN-CHIEH WANG ◽  
TAI-YUAN LIN ◽  
HSIN-JOU WU ◽  
CHI-JUNG HUANG ◽  
...  
Keyword(s):  
Renal Cell Carcinoma ◽  
Estrogen Receptor ◽  
Cell Carcinoma ◽  
G Protein ◽  
Renal Cell ◽  
G Protein Coupled ◽  
Estrogen Receptor 1
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