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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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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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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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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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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

6.4K
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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G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

4.4K
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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Related Experiment Video

Updated: May 9, 2025

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
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Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

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The Orphan Receptor GPR151: Discovery, Expression, and Emerging Biological Significance.

Olivia DePasquale1, Chris O'Brien1, Baila Gordon1

  • 1Department of Psychology, Rutgers, The State University of New Jersey, 152 Frelinghuysen Road, Piscataway, New Jersey 08854, United States.

ACS Chemical Neuroscience
|April 28, 2025
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) are key drug targets, but many remain unexplored. GPR151, implicated in pain and reward, is a promising novel target for developing new therapies.

Keywords:
AddictionGPCRIngestionOrphanPainhabenula

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Area of Science:

  • Pharmacology and neuroscience
  • Genomics and drug discovery

Background:

  • G protein-coupled receptors (GPCRs) represent a major class of drug targets, with ~40% of marketed drugs targeting them.
  • However, only ~10% of known GPCRs are currently targeted by therapies, leaving a significant gap in drug discovery.
  • Orphan GPCRs, like GPR151, offer substantial potential for novel therapeutic development.

Purpose of the Study:

  • To review the current literature on GPR151, an orphan GPCR.
  • To explore its potential as a therapeutic target for pain and reward-related disorders.
  • To highlight future research directions for GPR151.

Main Methods:

  • Literature review of GPR151 research.
  • Analysis of GPR151's anatomical distribution and conservation.
  • Summary of implicated functional roles in pain and reward pathways.

Main Results:

  • GPR151 is highly conserved across mammals and expressed in key neural regions (habenula, spinal cord, dorsal root ganglia).
  • GPR151 is strongly implicated in pain modulation and reward-seeking behaviors.
  • Its precise function remains largely unknown, presenting an opportunity for further investigation.

Conclusions:

  • GPR151 is a promising, evolutionarily conserved orphan GPCR target.
  • Its involvement in pain and reward pathways suggests potential for novel pharmacological interventions.
  • Further research into GPR151's mechanisms and functions is warranted for therapeutic development.