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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

19.4K
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...
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G Protein-coupled Receptors01:15

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G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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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.
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G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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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,...
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Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

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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:
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Related Experiment Video

Updated: Mar 21, 2026

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

Published on: April 9, 2017

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GPER-novel membrane oestrogen receptor.

Margaret A Zimmerman1, Rebecca A Budish1, Shreya Kashyap1

  • 1Department of Pharmacology, Tulane University, New Orleans, LA, U.S.A.

Clinical Science (London, England : 1979)
|May 8, 2016
PubMed
Summary

The G protein-coupled oestrogen receptor (GPER) is a newly discovered target with implications for numerous diseases. This review explores GPER's role in various conditions and its therapeutic potential.

Keywords:
GPR30cancercardiovascularmenopausemetabolismreproduction

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Area of Science:

  • Endocrinology and pharmacology
  • Molecular biology
  • Disease mechanisms

Background:

  • The G protein-coupled oestrogen receptor (GPER) is a recently identified receptor with diverse physiological roles.
  • Its involvement in various disease states is an emerging area of research.

Purpose of the Study:

  • To review the expression and function of GPER in a wide range of diseases.
  • To highlight GPER as a potential therapeutic target for these conditions.

Main Methods:

  • Literature review and synthesis of existing research on GPER.
  • Analysis of GPER's role in hypertension, kidney disease, atherosclerosis, vascular remodelling, heart failure, reproduction, metabolic disorders, cancer, environmental health, and menopause.

Main Results:

  • GPER is expressed and functionally relevant across multiple organ systems and disease pathologies.
  • Evidence suggests GPER signaling influences cardiovascular, metabolic, reproductive, and oncogenic processes.

Conclusions:

  • GPER represents a significant target for future therapeutic interventions.
  • Further research into GPER's multifaceted roles is warranted to develop novel treatment strategies.