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Related Concept Videos

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...
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...

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

G protein-mediated stretch reception.

Ursula Storch1, Michael Mederos y Schnitzler, Thomas Gudermann

  • 1Walther-Straub-Institute of Pharmacology and Toxicology, University of Munich, Germany.

American Journal of Physiology. Heart and Circulatory Physiology
|January 10, 2012
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) are emerging as key mechanosensors, translating mechanical stimuli into cellular signals. The angiotensin-II type-1 receptor exemplifies this, showing agonist-independent activation crucial for physiological processes.

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Published on: February 20, 2018

Area of Science:

  • Physiology
  • Biochemistry
  • Cell Biology

Background:

  • Mechanosensation and transduction are vital for senses like touch and hearing.
  • The mechanisms converting mechanical stimuli into biochemical signals are poorly understood.
  • G protein-coupled receptors (GPCRs) are known signal transducers for various stimuli.

Purpose of the Study:

  • To explore the role of GPCRs as potential mechanosensors.
  • To investigate the mechanisms of mechanical activation of GPCRs.
  • To highlight the physiological relevance of ligand-independent GPCR functions.

Main Methods:

  • Investigated the angiotensin-II type-1 (AT(1)) receptor as a candidate mechanosensitive GPCR.
  • Examined agonist-independent mechanical activation of AT(1) receptors.
  • Reviewed evidence for other GPCRs involved in mechanosensation.

Main Results:

  • The AT(1) receptor demonstrates agonist-independent mechanical activation, inducing a distinct active conformation.
  • Mechanically induced AT(1) receptor activation is critical for myogenic vasoconstriction and cardiac hypertrophy.
  • Evidence suggests multiple GPCRs function as mechanosensors.

Conclusions:

  • GPCRs possess physiologically relevant, ligand-independent mechanosensory functions.
  • This expands the known activation spectrum of GPCRs.
  • GPCRs represent a significant, yet understudied, class of mechanosensors.