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Related Concept Videos

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.
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

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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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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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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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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

7.7K
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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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

11.8K
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...
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Related Experiment Video

Updated: Feb 17, 2026

Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization
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GPCRs: What Can We Learn from Molecular Dynamics Simulations?

Naushad Velgy1, George Hedger1, Philip C Biggin2

  • 1Department of Biochemistry, Structural Bioinformatics and Computational Biochemistry, University of Oxford, South Parks Road, Oxford, OX1 3QU, UK.

Methods in Molecular Biology (Clifton, N.J.)
|December 1, 2017
PubMed
Summary

Molecular dynamics simulations reveal the crucial role of G-protein Coupled Receptor (GPCR) dynamics in drug target function. This approach offers unique insights into GPCR conformational changes, ligand binding pathways, and lipid influences.

Keywords:
ComputationalEnhanced samplingLigand bindingLipidMetadynamicsSimulation

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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:

  • Structural biology
  • Computational biophysics
  • Pharmacology

Background:

  • G-protein Coupled Receptors (GPCRs) are key drug targets.
  • GPCRs are highly dynamic molecules.
  • Understanding GPCR dynamics is crucial for drug development.

Purpose of the Study:

  • To investigate GPCR dynamics using molecular dynamics simulations.
  • To provide atomic-level insights into GPCR conformational changes.
  • To elucidate ligand binding/unbinding pathways and lipid influences on GPCRs.

Main Methods:

  • Molecular dynamics (MD) simulations.
  • Computational investigation of atomic-level movements.
  • Analysis of ligand-receptor interactions and lipid-protein dynamics.

Main Results:

  • Detailed atomic-level view of GPCR conformational states.
  • Characterization of ligand pathways during binding and unbinding.
  • Understanding the impact of lipids on GPCR conformational dynamics.

Conclusions:

  • Molecular dynamics simulations offer complementary insights to experimental methods for studying GPCR dynamics.
  • This approach is vital for understanding GPCR function and for rational drug design targeting these receptors.