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Related Concept Videos

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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Protein Dynamics in Living Cells01:19

Protein Dynamics in Living Cells

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Different fluorescence-based techniques are used to study the protein dynamics in living cells. These techniques include FRAP, FRET, and PET.
Fluorescent recovery after photobleaching (FRAP) is a fluorescent-protein-based detection technique used to quantify protein movement rates within the cell. This method exposes a small portion of the cell to an intense laser beam. The laser beam causes permanent photobleaching of the fluorophore-tagged proteins in the exposed region. As the bleached...
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GPCR Desensitization01:12

GPCR Desensitization

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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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.
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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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Related Experiment Video

Updated: Dec 5, 2025

Monitoring GPCR-&#946;-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
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Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

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Capturing Peptide-GPCR Interactions and Their Dynamics.

Anette Kaiser1, Irene Coin1

  • 1Faculty of Life Sciences, Institute of Biochemistry, Leipzig University, Brüderstr. 34, D-04103 Leipzig, Germany.

Molecules (Basel, Switzerland)
|October 20, 2020
PubMed
Summary
This summary is machine-generated.

Understanding G protein-coupled receptor (GPCR) dynamics is key for developing targeted drugs. New biochemical and biophysical methods reveal ligand-receptor interactions and conformational changes, improving drug specificity.

Keywords:
EPRGPCR activationNMRcrosslinkingpeptide ligandspeptide–GPCR interactionsstructural dynamics of GPCRs

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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

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Area of Science:

  • Biochemistry and Biophysics
  • Pharmacology
  • Structural Biology

Background:

  • G protein-coupled receptors (GPCRs) mediate numerous biological functions and are crucial pharmacological targets.
  • GPCRs regulate physiological processes, with biased ligands sought for selective effector recruitment.
  • Understanding ligand-GPCR interactions and induced conformational changes is vital for drug development.

Purpose of the Study:

  • To present biochemical and biophysical techniques for studying ligand-receptor interactions in structural and dynamic aspects.
  • To unveil the ligand-receptor contact interface and conformational changes in both ligands and GPCRs, focusing on peptide receptors.
  • To investigate the dynamic nature of ligand-GPCR interactions, often missed in static structural analyses.

Main Methods:

  • Mutagenesis
  • Crosslinking techniques
  • Spectroscopic methods
  • Mass-spectrometry profiling

Main Results:

  • Demonstrated methods to reveal ligand-receptor contact interfaces.
  • Characterized distinct conformational changes in GPCRs upon ligand binding.
  • Highlighted significant dynamics within ligand-GPCR complexes, particularly for peptide receptors.
  • Revealed structural heterogeneity among peptide receptors.

Conclusions:

  • Biochemical and biophysical approaches provide critical insights into ligand-GPCR structural dynamics.
  • Understanding these dynamics is essential for designing more specific and effective biased ligands.
  • Peptide receptors exhibit diverse structures and dynamic interactions crucial for their function.