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Related Concept Videos

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 Receptors01:15

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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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Activation and Inactivation of G Proteins01:22

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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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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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Related Experiment Video

Updated: Apr 22, 2026

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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Proton transfer-mediated GPCR activation.

Xuejun C Zhang1, Can Cao, Ye Zhou

  • 1National Laboratory of Macromolecules, National Center of Protein Science-Beijing, Institute of Biophysics, Chinese Academy of Sciences, Beijing, 100101, China, zhangc@ibp.ac.cn.

Protein & Cell
|October 17, 2014
PubMed
Summary
This summary is machine-generated.

G-protein coupled receptors (GPCRs) convert environmental signals into cellular responses. A proposed mechanism involves proton transfer through transmembrane elements, driving signal transduction and receptor activation.

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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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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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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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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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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
  • Molecular Biology
  • Cellular Signaling

Background:

  • G-protein coupled receptors (GPCRs) are crucial cell surface receptors involved in signal transduction.
  • While GPCR structures are well-studied, the precise mechanism of signal conversion from ligand binding to cellular activation remains unclear.
  • Understanding this mechanism is vital for drug development targeting GPCRs.

Purpose of the Study:

  • To elucidate the common functional mechanism of signal transduction in class-A GPCRs.
  • To propose a unifying model for how ligand binding is translated into a conformational change and downstream effector activation.

Main Methods:

  • Analysis of existing structural and functional data for class-A GPCRs.
  • Integration of biophysical and biochemical evidence related to GPCR activation.

Main Results:

  • A novel mechanism for GPCR signal transduction is proposed.
  • This mechanism centers on changes in protonation status within the receptor.
  • Proton transfer through conserved transmembrane elements is identified as a key step.

Conclusions:

  • Proton transfer and altered protonation states are essential for GPCR signal transduction across the membrane.
  • This model provides a framework for understanding ligand-induced conformational changes in GPCRs.
  • The findings offer insights into the fundamental workings of a major class of drug targets.