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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

11.1K
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...
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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

1.8K
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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G-protein Coupled Receptors01:21

G-protein Coupled Receptors

114.8K
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.
114.8K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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GPCR Desensitization01:12

GPCR Desensitization

5.7K
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...
5.7K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

6.6K
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...
6.6K

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Related Experiment Video

Updated: May 28, 2025

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

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Seeing new partners for GPCRs.

John F Foley1

  • 1Science Signaling, AAAS, Washington, DC 20005, USA.

Science Signaling
|February 11, 2025
PubMed
Summary
This summary is machine-generated.

A novel proximity assay was developed to identify proteins interacting with G protein-coupled receptors (GPCRs) in their natural cell membrane environment. This method helps uncover new regulators of GPCR function.

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A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled 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 "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled 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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Area of Science:

  • Biochemistry
  • Cell Biology
  • Molecular Biology

Background:

  • G protein-coupled receptors (GPCRs) are crucial cell membrane proteins involved in numerous physiological processes.
  • Understanding GPCR regulation and interactions is vital for developing targeted therapeutics.
  • Existing methods often struggle to capture the native interactions of endogenous GPCRs.

Purpose of the Study:

  • To develop and validate a proximity assay for identifying endogenous GPCR interactors.
  • To discover novel regulators of GPCRs within the cell membrane.

Main Methods:

  • Development of a proximity-dependent biotinylation assay.
  • Application of the assay to endogenous GPCRs in cell membranes.
  • Mass spectrometry-based identification of biotinylated proteins.

Main Results:

  • The assay successfully identified known GPCR interactors, validating its efficacy.
  • Putative novel interactors and regulators of endogenous GPCRs were discovered.
  • The assay provides a powerful tool for mapping GPCR interaction networks.

Conclusions:

  • The developed proximity assay is effective for unbiased discovery of GPCR interactors.
  • This approach facilitates a deeper understanding of GPCR regulation in their native cellular context.
  • The findings open new avenues for GPCR-targeted drug discovery.