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Related Concept Videos

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...
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.
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...
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high affinity and are together...

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Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET
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The hinge region: an important receptor component for GPHR function.

Sandra Mueller1, Holger Jaeschke, Robert Günther

  • 1Third Medical Department, University of Leipzig, Liebigstrasse 20, 04103 Leipzig, Germany.

Trends in Endocrinology and Metabolism: TEM
|October 13, 2009
PubMed
Summary

The glycoprotein hormone receptor (GPHR) hinge region is crucial for hormone binding and receptor activation. This review highlights its role in linking ligand binding to GPHR activation, despite its structure remaining unknown.

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Last Updated: Jun 19, 2026

Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

Published on: September 10, 2016

Area of Science:

  • Endocrinology
  • Molecular Biology
  • Structural Biology

Background:

  • Glycoprotein hormone receptors (GPHRs) are seven-transmembrane-spanning receptors with large ectodomains.
  • The three-dimensional structure of the GPHR hinge region is currently unknown.
  • The hinge region's role in ligand binding and receptor activation remains incompletely understood.

Purpose of the Study:

  • To review functional data concerning the hinge region of glycoprotein hormone receptors.
  • To elucidate the role of the hinge region in mediating hormone binding and receptor activation.
  • To highlight the hinge region as a critical link between ligand binding and GPHR activation.

Main Methods:

  • This review synthesizes findings from recent publications.
  • Functional data regarding specific hinge region residues are summarized.
  • The review focuses on studies investigating hormone binding, receptor activation, and intramolecular signaling.

Main Results:

  • Specific residues within the GPHR hinge region mediate hormone binding.
  • The hinge region is implicated in GPHR activation.
  • Evidence suggests the hinge region plays a role in intramolecular signaling.

Conclusions:

  • The GPHR hinge region is essential for both hormone binding and receptor activation.
  • This region acts as a crucial interface connecting ligand engagement to receptor signaling.
  • Further structural studies of the hinge region are warranted to fully understand GPHR function.