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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

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 Receptors01:21

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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Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

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Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
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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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Amplifying Signals via Second Messengers01:15

Amplifying Signals via Second Messengers

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Many receptor binding ligands are hydrophilic; they do not cross the cell membrane but bind to cell-surface receptors. Thus, their message must be relayed by second messengers present in the cell cytoplasm. There are several second messenger pathways, each with its own way of relaying information. For example, the G protein-coupled receptors can activate both phosphoinositol and cyclic AMP (cAMP) second messenger pathways. The phosphoinositol pathway is active when the receptor induces...
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Related Experiment Video

Updated: Jul 4, 2025

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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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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Functional diversification of cell signaling by GPCR localization.

Matthew J Klauer1, Blair K A Willette1, Nikoleta G Tsvetanova1

  • 1Department of Pharmacology and Cancer Biology, Duke University, Durham, North Carolina, USA.

The Journal of Biological Chemistry
|January 25, 2024
PubMed
Summary

G protein-coupled receptors (GPCRs), or seven transmembrane receptors, regulate physiology and are major drug targets. Emerging research shows GPCRs signal from intracellular compartments, influencing unique cellular outcomes.

Keywords:
G protein-coupled receptorPDEPKAadenylyl cyclasearrestincAMPendosomal signalingretromerspatial encoding

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Area of Science:

  • Cellular Biology
  • Pharmacology
  • Physiology

Background:

  • G protein-coupled receptors (GPCRs), also known as seven transmembrane receptors (7TMs), are the largest family of cell surface receptors.
  • They are crucial regulators of mammalian physiology, detecting diverse stimuli like hormones and neurotransmitters.
  • GPCRs represent a significant class of drug targets, accounting for over 30% of all prescription medications.

Purpose of the Study:

  • To review the evolving understanding of G protein-coupled receptor (GPCR) signaling.
  • To discuss the roles and regulation of compartmentalized GPCR signaling from intracellular compartments.

Main Methods:

  • Literature review and synthesis of current research on GPCR signaling.
  • Analysis of evidence supporting intracellular GPCR signaling pathways.

Main Results:

  • The traditional view of GPCRs signaling exclusively from the cell surface is being updated.
  • Accumulating evidence demonstrates that GPCRs can initiate signaling cascades from within intracellular compartments.
  • Intracellular GPCR signaling contributes to unique cellular and physiological responses.

Conclusions:

  • Compartmentalized GPCR signaling represents a critical layer of physiological regulation.
  • Further research into intracellular GPCR signaling is essential for understanding complex biological processes.
  • Targeting intracellular GPCR signaling may offer novel therapeutic strategies.