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The G protein-coupled oestrogen receptor GPER in health and disease: an update

Eric R Prossnitz1,2,3, Matthias Barton4,5

  • 1Department of Internal Medicine, Division of Molecular Medicine, University of New Mexico Health Sciences Center, Albuquerque, NM, USA. eprossnitz@salud.unm.edu.

Nature Reviews. Endocrinology
|May 16, 2023
PubMed

Insights

The G protein-coupled oestrogen receptor (GPER) plays a key role in health and disease. This review covers a decade of GPER research, highlighting its therapeutic potential.

Area of Science:

  • Endocrinology and Molecular Biology

Background:

  • Oestrogens and their receptors are crucial for physiology and disease, including cardiovascular, metabolic, neurological conditions, and hormone-sensitive cancers.
  • Oestrogen receptors include oestrogen receptor-α (ERα), oestrogen receptor-β (ERβ), and the 7-transmembrane G protein-coupled oestrogen receptor (GPER).
  • GPER mediates rapid signaling and transcriptional regulation, and its activity is modulated by oestrogen mimetics and drugs like SERMs and SERDs.

Purpose of the Study:

  • To summarize advancements in GPER research over the past decade, following the 2011 review.
  • To review molecular, cellular, and pharmacological aspects of GPER signaling and function.
  • To explore GPER's contribution to physiology, health, and disease, and its potential as a therapeutic target and prognostic indicator.

Main Methods:

  • Comprehensive literature review of GPER research published in the last decade.
  • Analysis of molecular, cellular, and pharmacological data related to GPER.
  • Examination of clinical trial data and drug repurposing opportunities for GPER.

Main Results:

  • GPER research has significantly progressed over the last decade.
  • GPER is implicated in various physiological and pathological processes.
  • The potential of GPER as a therapeutic target and prognostic marker is increasingly recognized.

Conclusions:

  • GPER is a significant target for therapeutic intervention and disease prognosis.
  • The review discusses the first clinical trial of a GPER-selective drug and drug repurposing strategies.
  • Further research into GPER signaling and pharmacology holds promise for novel treatments.

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