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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.
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GPCRs Regulate Adenylyl Cylase Activity01:09

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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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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.
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GPCR Desensitization01:12

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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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G-protein Coupled Receptors01:21

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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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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

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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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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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Structural Basis of GPCR-Biased Modulation.

Yan Zhang1

  • 1Zhejiang University, Hangzhou, China. zhang_yan@zju.edu.cn.

Handbook of Experimental Pharmacology
|October 1, 2025
PubMed
Summary

Biased signaling in G protein-coupled receptors (GPCRs) allows drugs to selectively activate specific pathways, improving therapeutic efficacy and reducing side effects. This research explores structural mechanisms for targeted drug design.

Keywords:
Biased signalingG proteinGPCRLigand modulationSelectivityStructureArrestin

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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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Area of Science:

  • Pharmacology
  • Molecular Biology
  • Structural Biology

Background:

  • G protein-coupled receptors (GPCRs) are the largest human membrane receptor family and key drug targets.
  • GPCRs activate diverse downstream pathways (G-proteins, arrestins), influencing physiological and pathological outcomes.
  • Understanding biased signaling is crucial for developing safer, more effective therapeutics.

Purpose of the Study:

  • To summarize current knowledge on GPCR selective coupling to signaling proteins.
  • To explore structural insights into ligand-induced receptor conformations and pathway bias.
  • To highlight biased ligands, their mechanisms, and therapeutic potential.

Main Methods:

  • Review of current literature on GPCR signaling and biased agonism.
  • Analysis of structural studies revealing ligand-stabilized receptor conformations.
  • Compilation of data on biased ligands and their therapeutic applications.

Main Results:

  • GPCRs can selectively engage different signaling partners based on ligand-induced conformations.
  • Structural data elucidates how specific ligands stabilize receptor states favoring particular pathways.
  • Numerous biased ligands with significant therapeutic potential have been identified.

Conclusions:

  • Structural understanding of biased signaling provides a foundation for rational drug discovery.
  • Targeting specific GPCR pathways can lead to enhanced drug efficacy and safety.
  • Further research into biased signaling mechanisms will optimize future pharmacological interventions.