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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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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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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

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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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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 Gated Ion Channels01:21

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GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Coding GPCR-G protein specificity.

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  • 1Drug Discovery Biology and Department of Pharmacology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, 3052 Victoria, Australia.

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Summary
This summary is machine-generated.

Researchers developed a model of G protein-coupled receptor (GPCR) and G protein interactions. An interactive database allows exploration of these crucial cellular signaling pathways.

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Area of Science:

  • Cellular Biology
  • Biochemistry
  • Bioinformatics

Background:

  • G protein-coupled receptors (GPCRs) are critical cell surface receptors involved in numerous physiological processes.
  • GPCRs mediate cellular responses primarily through the activation of intracellular G proteins.
  • Understanding GPCR-G protein selectivity is fundamental to deciphering cellular signaling networks.

Purpose of the Study:

  • To develop a predictive model for G protein-coupled receptor (GPCR) and G protein interactions.
  • To create an interactive database for exploring potential GPCR-G protein signaling.
  • To advance the understanding of selectivity in GPCR-mediated signaling.

Main Methods:

  • Large-scale bioinformatics analysis of GPCR and G protein sequences and structures.
  • Development of a computational model to predict receptor-G protein binding and activation.
  • Creation of an interactive, web-based database for data visualization and querying.

Main Results:

  • A comprehensive model elucidating the determinants of GPCR-G protein selectivity was established.
  • The interactive database provides a valuable resource for investigating specific GPCR-G protein pairs.
  • The findings offer insights into the specificity of signal transduction initiated by GPCRs.

Conclusions:

  • The developed model and database offer a powerful tool for studying GPCR-G protein interactions.
  • This work facilitates the prediction of novel signaling pathways and the design of targeted therapeutics.
  • The study significantly enhances our comprehension of cellular signal transduction mechanisms.