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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

16.3K
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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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.
131.3K
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...
5.5K
GPCR Desensitization01:12

GPCR Desensitization

7.8K
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...
7.8K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

10.7K
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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Related Experiment Video

Updated: Jan 7, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

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The Concise Guide to PHARMACOLOGY 2025/26: G protein-coupled receptors.

Stephen P H Alexander1, Anthony P Davenport2, Eamonn Kelly3

  • 1Division of Physiology, Pharmacology & Neuroscience, School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK.

British Journal of Pharmacology
|December 29, 2025
PubMed
Summary
This summary is machine-generated.

The Concise Guide to Pharmacology 2025/26 offers a curated overview of human drug targets and their interactions. This biennial publication provides essential pharmacological data and identifies selective tools for research.

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Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biomedical Sciences

Background:

  • The British Journal of Pharmacology publishes the biennial Concise Guide to Pharmacology.
  • This guide provides a comparative overview of drug target families.
  • It is a condensed version of the comprehensive Guide to Pharmacology website.

Purpose of the Study:

  • To present a clear, accessible, and well-structured summary of human drug targets.
  • To provide expert-curated recommendations of selective pharmacological tools.
  • To serve as a permanent, citable, point-in-time record of pharmacological information.

Main Methods:

  • Summarization of key pharmacological properties for approximately 1900 human drug targets.
  • Inclusion of nearly 7000 interactions involving around 4400 ligands.
  • Collaboration with the International Union of Basic and Clinical Pharmacology (NC-IUPHAR) for official nomenclature.

Main Results:

  • The 2025/26 edition covers six major target families: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes, and transporters.
  • Provides information on nomenclature, concise summaries, and the best available pharmacological tools.
  • Includes key references and suggestions for further reading.

Conclusions:

  • The Concise Guide serves as a valuable resource for researchers needing a stable, citable reference.
  • It complements the online database by offering a permanent record of pharmacological data.
  • The guide facilitates the identification of drug targets and the selection of appropriate pharmacological tools.