Role of G Protein-Coupled Estrogen Receptor in Digestive System Carcinomas: A Minireview

Qiu, Yuan; Xiong, Jianping; Yu, Tenghua

doi:10.2147/ott.s291896

Cited by 8 publications

(5 citation statements)

References 107 publications

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“…It is associated with G proteins bridging molecules, and it activates at least three different pathways depending on the ligand concentrations. One pathway is cAMP-dependent and reacts to 1 µM of the agonist G1, while another relies on the Src/EGFR pathways and responds to 0.01 µM of G1 [ 17 ]. Considering these different receptors, their different affinities for estrogens, their different cell locations, their different activation modes, and, finally, their different tissue distributions, it can easily be understood that the effects of estradiol—and also estrogen mimetics—can be very complex and do not follow a linear dose–response curve.…”

Section: Definition and Originmentioning

confidence: 99%

Phytoestrogens and Health Effects

Canivenc-Lavier

Bennetau-Pelissero

2023

Nutrients

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Phytoestrogens are literally estrogenic substances of plant origin. Although these substances are useful for plants in many aspects, their estrogenic properties are essentially relevant to their predators. As such, phytoestrogens can be considered to be substances potentially dedicated to plant–predator interaction. Therefore, it is not surprising to note that the word phytoestrogen comes from the early discovery of estrogenic effects in grazing animals and humans. Here, several compounds whose activities have been discovered at nutritional concentrations in animals and humans are examined. The substances analyzed belong to several chemical families, i.e., the flavanones, the coumestans, the resorcylic acid lactones, the isoflavones, and the enterolignans. Following their definition and the evocation of their role in plants, their metabolic transformations and bioavailabilities are discussed. A point is then made regarding their health effects, which can either be beneficial or adverse depending on the subject studied, the sex, the age, and the physiological status. Toxicological information is given based on official data. The effects are first presented in humans. Animal models are evoked when no data are available in humans. The effects are presented with a constant reference to doses and plausible exposure.

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Section: Definition and Originmentioning

confidence: 99%

Phytoestrogens and Health Effects

Canivenc-Lavier

Bennetau-Pelissero

2023

Nutrients

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“…G protein-coupled oestrogen receptor (GPER), also known as GPR30, first reported in 2005 [167], is a seven-transmembrane receptor that mediates membrane-initiated oestrogen signalling in a wide range of tissues [168]. Initially identified as an alternative oestrogen receptor in breast cancer [169], GPER signalling has emerged as a significant player in colon cancer [170], contributing to various aspects of tumour progression and estrogenic cell signalling responses [171]. While many studies over the past twenty years support an oestrogen-ligand receptor role for GPER [172,173], the involvement of GPER in transducing nongenomic actions of oestrogen in vivo has been challenged [174,175].…”

Section: Oestrogen Signalling Via G Protein-coupled Oestrogen Recepto...mentioning

confidence: 99%

“…The modulation of ATM expression by GPER in low oxygen tension and the sensitivity of its expression to oestrogen in CRC provides an additional mechanism for protumorigenic actions of oestrogen via GPER in colon cancer under hypoxic conditions. Thus, it is important to take into account the CRC stage and tumour microenvironment when interpreting the role of E2-GPER interactions in colon cancer tumorigenesis, sex differences, and patient survival/treatment [170].…”

Section: Hypoxia and Gper Signalling In Colon Cancermentioning

confidence: 99%

Sex Differences in Colon Cancer: Genomic and Nongenomic Signalling of Oestrogen

Harvey,

Harvey

2023

Genes

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Colon cancer (CRC) is a prevalent malignancy that exhibits distinct differences in incidence, prognosis, and treatment responses between males and females. These disparities have long been attributed to hormonal differences, particularly the influence of oestrogen signalling. This review aims to provide a comprehensive analysis of recent advances in our understanding of the molecular mechanisms underlying sex differences in colon cancer and the protective role of membrane and nuclear oestrogen signalling in CRC development, progression, and therapeutic interventions. We discuss the epidemiological and molecular evidence supporting sex differences in colon cancer, followed by an exploration of the impact of oestrogen in CRC through various genomic and nongenomic signalling pathways involving membrane and nuclear oestrogen receptors. Furthermore, we examine the interplay between oestrogen receptors and other signalling pathways, in particular the Wnt/β-catenin proliferative pathway and hypoxia in shaping biological sex differences and oestrogen protective actions in colon cancer. Lastly, we highlight the potential therapeutic implications of targeting oestrogen signalling in the management of colon cancer and propose future research directions to address the current gaps in our understanding of this complex phenomenon.

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“…To understand the action of GPER, several ligands including estrogen have been investigated ( Qiu et al ., 2021 ). G1 Tomoxifen, as a selective ER modulator, and ICI 182,780, as an ER antagonist, are known as GPER agonists, while G15 is known as a GPER antagonist ( Hsu et al ., 2019 ).…”

Section: Introductionmentioning

confidence: 99%

Stimulatory Anticancer Effect of Resveratrol Mediated by G Protein-Coupled Estrogen Receptor in Colorectal Cancer

Kim,

Kwon,

Shin

et al. 2023

Biomol Ther (Seoul)

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Colorectal cancer (CRC) is one of the most high-risk cancers; however, it has been suggested that estrogen signaling in CRC could have a protective effect. Therefore, we focused on the function of the G protein-coupled estrogen receptor (GPER) among the estrogen receptors in CRC. In this study, we investigated the therapeutic effect of resveratrol via GPER in CRC (RKO and WiDr) cells, CRC cell-derived xenograft models, and organoids (30T and 33T). Resveratrol significantly suppressed cell viability and proliferation in highly GPER-expressing RKO cells compared to that in low GPER-expressing WiDr cells. In xenograft models, resveratrol also delayed tumor growth and exhibited a high survival rate depending on GPER expression in RKO-derived tumors. Furthermore, resveratrol significantly inhibited the viability of organoids with high GPER expression. Additionally, the anticancer effect of resveratrol on CRC showed that resveratrol rapidly responded to GPER, while increasing the expression of p-ERK and Bax and cleaving PARP proteins.

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Role of G Protein-Coupled Estrogen Receptor in Digestive System Carcinomas: A Minireview

Cited by 8 publications

References 107 publications

Phytoestrogens and Health Effects

Phytoestrogens and Health Effects

Sex Differences in Colon Cancer: Genomic and Nongenomic Signalling of Oestrogen

Stimulatory Anticancer Effect of Resveratrol Mediated by G Protein-Coupled Estrogen Receptor in Colorectal Cancer

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