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Related Concept Videos

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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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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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

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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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

7.8K
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...
7.8K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

6.0K
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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Updated: Sep 22, 2025

Detection of Ligand-activated G Protein-coupled Receptor Internalization by Confocal Microscopy
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Detection of Ligand-activated G Protein-coupled Receptor Internalization by Confocal Microscopy

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Posttranslational modifications in GPCR internalization.

Xueqing Tang1,2,3, Jingwei Bian1,2,3, Zijian Li1,2,3,4

  • 1Department of Cardiology and Institute of Vascular Medicine, Peking University Third Hospital, Beijing Key Laboratory of Cardiovascular Receptors Research, Beijing, People's Republic of China.

American Journal of Physiology. Cell Physiology
|May 25, 2022
PubMed
Summary

Internalized G protein-coupled receptors (GPCRs) can activate signals, challenging old views. Posttranslational modifications (PTMs) regulate this internalization, offering new precision medicine targets.

Keywords:
GPCR internalizationinternalization dynamicsinternalization routespostinternalization fatesposttranslational modifications

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Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis
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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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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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Area of Science:

  • Molecular Biology
  • Cell Signaling
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets, with internalization traditionally linked to desensitization.
  • Recent findings reveal internalized GPCRs can initiate distinct signaling pathways.
  • This challenges classical understanding and opens new avenues for therapeutic intervention.

Purpose of the Study:

  • To review the role of posttranslational modifications (PTMs) in regulating GPCR internalization.
  • To analyze how PTMs influence GPCR internalization dynamics, routes, and fates.
  • To highlight the significance of these processes for understanding GPCR signaling and developing precision medicine strategies.

Main Methods:

  • Literature review and synthesis of existing research on GPCR internalization and PTMs.
  • Analysis of studies investigating the functional consequences of GPCR internalization.
  • Examination of the regulatory roles of various PTMs in GPCR trafficking and signaling.

Main Results:

  • GPCR internalization is a highly regulated process, significantly influenced by PTMs.
  • PTMs dictate internalization routes, dynamics, and the ultimate fate of internalized receptors.
  • Internalized GPCRs can mediate signaling distinct from cell surface receptors, termed 'internalized activation'.

Conclusions:

  • GPCR internalization is not solely a desensitization event but can lead to unique signaling outcomes.
  • Posttranslational modifications are critical regulators of GPCR internalization and subsequent signaling.
  • Understanding PTM-mediated GPCR internalization offers novel therapeutic targets for precision medicine.