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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.
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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

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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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Interactions Between Signaling Pathways01:19

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Signaling cascades usually lack linearity. Multiple pathways interact and regulate one another, allowing cells to integrate and respond to diverse environmental stimuli.
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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G Protein-Coupled Receptor Signaling Networks from a Systems Perspective.

S Roth1, B N Kholodenko1, M J Smit2

  • 1Systems Bioinformatics (S.R., F.J.B.) and Amsterdam Institute for Molecules, Medicines & Systems, VU University, Amsterdam, The Netherlands (M.J.S.); and Systems Biology Ireland, University College Dublin, Dublin, Ireland (B.N.K.).

Molecular Pharmacology
|July 12, 2015
PubMed
Summary
This summary is machine-generated.

Mammalian cells use complex G protein-coupled receptor (GPCR) networks to process signals. These systems exhibit emergent behaviors, highlighting the need for network theories in systems biology research.

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Area of Science:

  • Cellular biology
  • Systems biology
  • Biochemistry

Background:

  • Cell-surface receptors, particularly G protein-coupled receptors (GPCRs), integrate internal and external cues for adaptive cellular responses.
  • GPCRs stabilize intracellular conformations upon extracellular signal binding, selectively activating downstream proteins.
  • Signaling networks exhibit complex, emergent processing capabilities beyond individual protein functions.

Purpose of the Study:

  • To review key signaling system behaviors observed across diverse cellular networks.
  • To emphasize the underappreciated role of GPCRs in systems biology research.
  • To highlight the necessity of network theories for understanding cellular information processing.

Main Methods:

  • Review of systems-biology studies on cellular signaling networks.
  • Analysis of emergent properties in signal transduction pathways.
  • Focus on G protein-coupled receptors (GPCRs) as central signaling integrators.

Main Results:

  • Signaling networks demonstrate spatiotemporal organization, producing diverse response patterns (gradual, oscillatory, all-or-none).
  • Protein-protein interactions and feedback/feedforward circuits are crucial for these dynamic responses.
  • GPCRs play a significant, yet often underappreciated, role in integrating multiple signals and driving network behaviors.

Conclusions:

  • Understanding cellular information processing requires integrating biochemical, biophysical, and network theories.
  • GPCRs are critical components of sophisticated cellular signal-integration systems.
  • Emergent properties of signaling networks are fundamental to cellular adaptation and function.