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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

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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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G-protein Coupled Receptors01:21

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Transducer Mechanism: G Protein–Coupled Receptors01:30

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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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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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Adhesion G protein-coupled receptors.

Tobias Langenhan1, Garret R Anderson2, Demet Araç3

  • 1Rudolf Schönheimer Institute of Biochemistry, General Biochemistry, Medical Faculty, Leipzig University, Leipzig, Germany; Comprehensive Cancer Center Central Germany (CCCG), Leipzig, Germany; Faculty of Life Sciences, Institute of Biology, Leipzig University, Leipzig, Germany.

Pharmacological Reviews
|March 27, 2026
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Summary
This summary is machine-generated.

Adhesion G protein-coupled receptors (aGPCRs) are key cell-surface proteins with vital roles in health and disease. This review details their molecular features, functions, and therapeutic potential.

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Area of Science:

  • Molecular Biology
  • Cell Biology
  • Biochemistry

Background:

  • Adhesion G protein-coupled receptors (aGPCRs) are a distinct class of GPCRs.
  • Significant advancements have been made since the 2015 nomenclature establishment.
  • Their roles in human health and disease are increasingly recognized.

Purpose of the Study:

  • To provide a comprehensive review of recent progress in aGPCR biology.
  • To assess the current understanding of aGPCRs, focusing on mammalian systems.
  • To highlight emerging therapeutic targeting strategies for aGPCRs.

Main Methods:

  • Literature review and synthesis of current research.
  • Analysis of molecular architecture, biochemical properties, and signaling.
  • Examination of evolutionary origins and model systems.

Main Results:

  • Detailed delineation of aGPCR biological roles, molecular features, and expression profiles.
  • Comprehensive assessment of ligand repertoire and activation mechanisms.
  • Identification of key methodological approaches and model systems for aGPCR research.

Conclusions:

  • aGPCRs are versatile proteins with integrated functions crucial for health and disease.
  • This review serves as a resource connecting basic aGPCR biology with translational applications.
  • Emerging therapeutic strategies offer new opportunities for targeting aGPCRs in various disciplines.