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Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

132.1K
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.
132.1K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

17.2K
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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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

4.3K
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,...
4.3K
Internal Receptors01:31

Internal Receptors

74.7K
Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
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Spin–Spin Coupling: Two-Bond Coupling (Geminal Coupling)01:20

Spin–Spin Coupling: Two-Bond Coupling (Geminal Coupling)

1.7K
Two NMR-active nuclei bonded to a central atom can be involved in geminal or two-bond coupling. Geminal coupling is commonly seen between diastereotopic protons in chiral molecules and unsymmetrical alkenes, among others.
The central atom need not be NMR-active because its electrons are affected by the electron polarization of the spin-active atoms. However, spin information is transmitted less effectively than in one-bond coupling, and 2J values are usually weaker than 1J values. The energy of...
1.7K
Spin–Spin Coupling: Three-Bond Coupling (Vicinal Coupling)01:22

Spin–Spin Coupling: Three-Bond Coupling (Vicinal Coupling)

1.5K
Vicinal or three-bond coupling is commonly observed between protons attached to adjacent carbons. Here, nuclear spin information is primarily transferred via electron spin interactions between adjacent C‑H bond orbitals. This generally favors the antiparallel arrangement of spins, so 3J values are usually positive.
The extent of coupling depends on the C‑C bond length, the two H‑C‑C angles, any electron-withdrawing substituents, and the dihedral angle between the involved orbitals. The...
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Quantifying Agonist Activity at G Protein-coupled Receptors
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G Protein-Coupled Receptor Resensitization Paradigms.

Manveen K Gupta1, Maradumane L Mohan1, Sathyamangla V Naga Prasad1

  • 1Department of Molecular Cardiology, Lerner Research Institute, Cleveland Clinic, Cleveland, OH, United States.

International Review of Cell and Molecular Biology
|May 20, 2018
PubMed
Summary

Cell surface receptors, like G protein-coupled receptors (GPCRs), regulate cellular responses. This chapter focuses on the crucial, yet understudied, resensitization process that restores GPCR function.

Keywords:
A-kinase anchoring proteinDesensitizationG protein-coupled receptor kinasesG protein-coupled receptorsInhibitor of protein phosphatase 2APDZ-binding proteinsPhosphoinositide 3-kinase γProtein phosphatase 1Protein phosphatase 2AResensitizationβ-Arrestin

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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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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

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Area of Science:

  • Cellular Biology
  • Molecular Pharmacology

Background:

  • Cell surface receptors, particularly G protein-coupled receptors (GPCRs), are critical for cellular communication and response to environmental cues.
  • GPCRs mediate vital physiological processes including cardiac function, vision, olfaction, and platelet activation.
  • GPCR function is regulated by a cycle of activation, desensitization, and resensitization.

Purpose of the Study:

  • To highlight recent advancements in understanding the mechanistic underpinnings of GPCR regulation.
  • To emphasize the significant role of GPCR resensitization in maintaining cellular signaling fidelity.
  • To provide a focused discussion on the key advances in GPCR resensitization.

Main Methods:

  • Review of existing literature on GPCR signaling pathways.
  • Analysis of molecular mechanisms involved in GPCR activation, desensitization, and resensitization.
  • Synthesis of current research on the regulation of GPCR resensitization.

Main Results:

  • GPCR activation initiates downstream signaling cascades.
  • Desensitization, involving phosphorylation and beta-arrestin binding, reduces signaling.
  • Resensitization, occurring in endosomes via dephosphorylation, recycles GPCRs for re-stimulation.

Conclusions:

  • While GPCR activation and desensitization are well-studied, GPCR resensitization is increasingly recognized as a tightly regulated and vital process.
  • Understanding GPCR resensitization is key to comprehending the dynamic control of cellular responses.
  • Further research into resensitization mechanisms promises new insights into GPCR function and potential therapeutic targets.