Related Experiment Video

Updated: Aug 10, 2026

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
11:49

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

What does an orphan G-protein-coupled receptor have to do with estrogen?

James M Rae1, Michael D Johnson

  • 1Division of Hematology Oncology, Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor, Michigan, USA. jimmyrae@umich.edu

Breast Cancer Research : BCR
|November 11, 2005
PubMed

Insights

Estrogen impacts female physiology and development through nuclear receptors and rapid signaling pathways. Recent findings suggest a G-protein-coupled receptor, GPR30, mediates these rapid estrogen effects.

Area of Science:

  • Endocrinology
  • Molecular Biology
  • Cell Signaling

Background:

  • Estrogen influences female reproductive tissues, bone integrity, cardiovascular and central nervous system functions.
  • Estrogen signaling involves nuclear estrogen receptors (ERs) acting as transcription factors.
  • Rapid estrogen responses exist that are not explained by classical genomic ER signaling.

Purpose of the Study:

  • To investigate the mechanisms behind rapid estrogen signaling.
  • To identify potential non-genomic estrogen receptors.

Main Methods:

  • Review of existing literature on estrogen signaling pathways.
  • Analysis of recent reports on G-protein-coupled receptors (GPCRs).

Main Results:

  • Estrogen exerts broad physiological effects, including reproductive tissue development and bone health.
  • Classical genomic actions via ER-alpha and ER-beta do not fully explain all estrogen effects.
  • Emerging evidence points to G-protein-coupled receptor 30 (GPR30) as a mediator of rapid, non-genomic estrogen actions.

Conclusions:

  • Estrogen's diverse physiological roles are mediated by both nuclear and potentially membrane-bound receptors.
  • GPR30 is a strong candidate for mediating rapid estrogen signaling, expanding our understanding of estrogen's mechanisms of action.

More Related Videos

Detection of Ligand-activated G Protein-coupled Receptor Internalization by Confocal Microscopy10:24

Detection of Ligand-activated G Protein-coupled Receptor Internalization by Confocal Microscopy

Published on: April 9, 2017

Screening for Phytoestrogens using a Cell-based Estrogen Receptor β Reporter Assay06:07

Screening for Phytoestrogens using a Cell-based Estrogen Receptor β Reporter Assay

Published on: June 7, 2020

Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes: