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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

15.5K
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...
15.5K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

3.5K
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,...
3.5K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

130.0K
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.
130.0K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

9.7K
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...
9.7K
G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

5.4K
GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
5.4K
GPCR Desensitization01:12

GPCR Desensitization

7.5K
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...
7.5K

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Related Experiment Video

Updated: Dec 8, 2025

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

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Illuminating the Path to Target GPCR Structures and Functions.

Christian D-T Nielsen1, Divya Dhasmana2, Giuseppe Floresta3

  • 1Imperial College London, White City Campus, Molecular Sciences Research Hub, 80 Wood Lane, London W12 0BZ, U.K.

Biochemistry
|September 21, 2020
PubMed
Summary
This summary is machine-generated.

Super-resolution imaging offers direct visualization of G-Protein-coupled receptors (GPCRs), moving beyond bulk measurements. This advanced technique provides detailed structural and spatial insights for novel drug development and clinical strategies targeting these crucial receptors.

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

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Related Experiment Videos

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

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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Area of Science:

  • Biochemistry and Molecular Biology
  • Cell Biology
  • Pharmacology

Background:

  • G-Protein-coupled receptors (GPCRs) are vital eukaryotic proteins involved in numerous physiological and pathological processes.
  • GPCRs represent the most heavily targeted protein class in the human genome for drug development.
  • Current understanding of GPCR activity largely relies on indirect measurements from bulk analyses.

Purpose of the Study:

  • To review common indirect methods used for observing GPCR activity.
  • To highlight the potential of super-resolution imaging for direct GPCR visualization.
  • To analyze the benefits of optical imaging for advancing GPCR-targeted therapeutics.

Main Methods:

  • Summary of conventional bulk measurement techniques for GPCR activity.
  • Review of super-resolution imaging approaches applied to GPCR studies.
  • Analysis of direct optical visualization strategies for GPCRs.

Main Results:

  • Existing methods provide indirect insights into GPCR function.
  • Super-resolution imaging enables detailed structural and spatial characterization of GPCRs.
  • Direct visualization offers superior information compared to bulk analyses.

Conclusions:

  • Super-resolution imaging is a powerful tool for detailed GPCR analysis.
  • Direct optical visualization of GPCRs can significantly aid in developing new drugs.
  • This approach holds promise for innovative clinical strategies targeting GPCRs.