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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.
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

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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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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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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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G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

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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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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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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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Many ligands and states of bitter taste GPCRs.

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Taste GPCRs and their ligands.

Nitzan Dubovski1, Fabrizio Fierro1, Eitan Margulis1

  • 1The Institute of Biochemistry, Food Science and Nutrition, Robert H. Smith Faculty of Agriculture, Food and Environment, The Hebrew University of Jerusalem, Rehovot, Israel.

Progress in Molecular Biology and Translational Science
|November 10, 2022
PubMed
Summary

Taste G protein-coupled receptors (GPCRs) are crucial for food choices and have roles beyond the tongue. Discovering their ligands is key to understanding these functions.

Keywords:
AgonistAntagonistComputationalFamily AFamily CFunctional assaysGPCRMachine-learningReceptorTaste

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Area of Science:

  • G protein-coupled receptors (GPCRs)
  • Sensory biology
  • Molecular pharmacology

Background:

  • Taste GPCRs are primarily found in taste buds, influencing food selection and intake.
  • These receptors also have extra-oral expression, with emerging physiological roles under investigation.
  • Understanding taste receptor function necessitates identifying their specific ligands (agonists and antagonists).

Purpose of the Study:

  • To provide an overview of taste receptor families.
  • To summarize recent methodologies for discovering taste receptor ligands.
  • To highlight current resources for known taste receptor ligands.

Main Methods:

  • Integration of sensory, cell-based, and computational approaches for ligand discovery.
  • Review of established and emerging techniques in taste receptor research.
  • Compilation of information from existing ligand databases.

Main Results:

  • Numerous agonists and several antagonists for taste GPCRs have been identified.
  • A comprehensive overview of taste receptor families and ligand discovery methods is presented.
  • Current sources of information on known taste receptor ligands are detailed.

Conclusions:

  • Knowledge of taste GPCR ligands is essential for elucidating their physiological functions.
  • Future research will focus on ligand interactions with genetic polymorphisms and advanced techniques like CryoEM.
  • Advancements in signaling readout technologies will further impact the field of taste GPCR research.