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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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G Protein-coupled Receptors01:15

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Transducer Mechanism: G Protein–Coupled Receptors01:30

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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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G-protein Coupled Receptors01:21

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The Two-State Receptor Model01:29

The Two-State Receptor Model

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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
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Updated: Mar 24, 2026

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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Resonance Energy Transfer-Based Approaches to Study GPCRs.

Mohammed Akli Ayoub1

  • 1Biologie et Bioinformatique des Systèmes de Signalisation, Institut National de la Recherche Agronomique, UMR85, Unité Physiologie de la Reproduction et des Comportements; CNRS, UMR7247, Nouzilly, France; LE STUDIUM(®) Loire Valley Institute for Advanced Studies, Orléans, France.

Methods in Cell Biology
|March 2, 2016
PubMed
Summary

G protein-coupled receptors (GPCRs) are crucial proteins studied using resonance energy transfer (RET) methods like bioluminescence and fluorescence resonance energy transfer (BRET/FRET). These techniques offer dynamic insights into GPCR function, advancing drug discovery.

Keywords:
BRETG proteinsGPCRsOligomerizationSignalingTR-FRETβ-Arrestins

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Area of Science:

  • Biophysics
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are a major class of cell surface receptors involved in numerous physiological and pathophysiological processes.
  • Advances in biophysical techniques have significantly enhanced the study of GPCRs.
  • Resonance energy transfer (RET)-based approaches, including BRET and FRET, are powerful tools for investigating GPCRs.

Purpose of the Study:

  • To review the application of BRET and FRET in studying GPCRs.
  • To highlight the impact of these techniques on understanding GPCR biology and function.
  • To discuss future prospects for RET-based assays in drug discovery.

Main Methods:

  • Utilizing bioluminescence resonance energy transfer (BRET) and fluorescence resonance energy transfer (FRET) methodologies.
  • Analyzing GPCR activation, regulation, and dynamics in real-time within intact cells.
  • Exploring applications in native tissues and high-throughput screening.

Main Results:

  • BRET and FRET have provided dynamic, real-time insights into GPCR functioning.
  • These methods have significantly advanced the understanding of GPCR activation and regulation.
  • The study of GPCRs in native tissues is now more feasible.

Conclusions:

  • RET-based approaches have revolutionized GPCR research, offering dynamic and detailed functional information.
  • Further technological developments promise new RET assays for high-throughput screening and drug discovery.
  • Understanding GPCRs in their native context is crucial for advancing biological and medical knowledge.