Research Topic

Therapeutic Perspectives in the Modulation of the GPER

About this Research Topic

Targeting hepta-helical transmembrane G protein-coupled receptors (GPCRs) has been fruitful for the treatment of a panel of diseases, including immunological, viral, neurological, cardiac and hormonal-related pathologies. In 1997, a gene expressing the class A (rhodopsine) GPCR named GPR30 (now renamed GPER), ...

Targeting hepta-helical transmembrane G protein-coupled receptors (GPCRs) has been fruitful for the treatment of a panel of diseases, including immunological, viral, neurological, cardiac and hormonal-related pathologies. In 1997, a gene expressing the class A (rhodopsine) GPCR named GPR30 (now renamed GPER), was identified by Carmeci et al. This protein, which is functionally activated not only by estrogen but also by growth factor receptors, is intimately linked to kinase pathways. During the last two decades, remarkable progress has been made to better understand the mechanism of action of this membrane receptor and its role in health and disease. GPER is not only active in the male and female reproductive systems, but also in the cardiovascular system and the central nervous system where it modulates pain.
Additionally, it mediates immune and inflammatory responses, and its role in metabolism has been clearly demonstrated.

Moreover, GPER is a potential target for breast cancer treatment including triple negative breast cancer (TNBC), which is particularly aggressive, and which encompasses approximately 20% of breast cancers. In this regard, the use of GPER modulators could constitute an interesting perspective in the context of chemotherapy resistance. Thus, targeting the multifaceted GPER is a promising strategy that could open new exciting perspectives in the clinical realm. Only a few GPER specific ligands have been identified in addition to the high affinity estradiol and its metabolite methoxyestradiol. Members of quinolein compound family include the synthetic agonist G-1 and antagonists G-15 and G-36, and more recently, the first peptidic GPER modulator was reported. Due to the limited number of GPER ligands, strong efforts are required for the design of new modulators, and the resolution of the GPER crystal structure would be particularly helpful.

In this Research Topic for Frontiers in Endocrinology, we will focus on the clinical perspectives in GPER modulation. After a brief overview of the GPER ligands and of the related signaling pathways, we will place a special emphasis on the context of cancerous, neurological and cardiovascular diseases, through multidisciplinary approaches. The emerging role of the GPER in other pathologies will also be addressed. We welcome from authors review and mini review, general commentaries, hypothesis, and perspectives articles. This Research Topic aims to propose an overview of the level of knowledge concerning the GPER.


Keywords: Estrogens, GPER, Pharmacology, Pathologies, Pharmaceuticals


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01 June 2020 Manuscript

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Topic Editors

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Submission Deadlines

01 June 2020 Manuscript

Participating Journals

Manuscripts can be submitted to this Research Topic via the following journals:

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