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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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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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G-protein-coupled receptor structure: what can we learn?

Andrew B Tobin1

  • 1Department of Cell Physiology and Pharmacology, University of Leicester, Hodgkin Building Lancaster Road Leicester LE1 9HN UK.

F1000 Biology Reports
|October 16, 2010
PubMed
Summary

The first crystal structures of non-visual G-protein-coupled receptors, specifically the β(1)- and β(2)-adrenergic receptors, offer key insights into how drugs bind and activate these important cellular signaling proteins.

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET
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Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET

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Area of Science:

  • Structural Biology
  • Biochemistry
  • Pharmacology

Background:

  • G-protein-coupled receptors (GPCRs) are crucial cell surface receptors involved in numerous physiological processes.
  • Non-visual GPCRs, including adrenergic receptors, play vital roles in signaling pathways beyond vision.
  • Understanding GPCR structure is essential for drug discovery and development.

Purpose of the Study:

  • To explore the technological advancements enabling the determination of GPCR crystal structures.
  • To review current knowledge gained from the structures of β(1)- and β(2)-adrenergic receptors.
  • To identify remaining questions and future research directions in GPCR structural biology.

Main Methods:

  • X-ray crystallography was employed to resolve the three-dimensional structures.
  • Advanced imaging techniques and computational modeling were utilized.
  • Structure-based analysis of ligand-receptor interactions was performed.

Main Results:

  • The first crystal structures of non-visual GPCRs, specifically β(1)- and β(2)-adrenergic receptors, have been determined.
  • These structures provide atomic-level details of ligand binding pockets.
  • Insights into the conformational changes associated with receptor activation have been revealed.

Conclusions:

  • The determined GPCR structures represent a significant breakthrough in understanding receptor function.
  • These findings pave the way for structure-based drug design targeting adrenergic receptors.
  • Further research is needed to fully elucidate GPCR activation mechanisms and diverse signaling.