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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

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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

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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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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 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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Intracellular Signaling Affects Focal Adhesions01:17

Intracellular Signaling Affects Focal Adhesions

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Integrins act both as extracellular input receivers and as intracellular processing activators. As their name suggests, integrins are entirely integrated into the membrane structure. Their hydrophobic membrane-spanning regions interact with the phospholipid bilayer's hydrophobic region. These membrane receptors provide extracellular attachment sites for effectors like hormones and growth factors. They activate intracellular response cascades when their effectors are bound and active.
Some...
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Updated: Feb 19, 2026

A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors
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The elephant in the adhesion GPCR room.

Tobias Langenhan1,2,3

  • 1Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Medical Faculty, Leipzig University, 04103 Leipzig, Germany.

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|February 17, 2026
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Adhesion G protein-coupled receptors (GPCRs) are crucial for organ system development. Bernadyn et al. reveal new details on the activation mechanism and cellular functions of the adhesion GPCR GPR97/ADGRG3.

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Area of Science:

  • Cellular Biology
  • Molecular Biology
  • Physiology

Background:

  • Adhesion GPCRs are integral membrane proteins regulating diverse cellular processes.
  • GPR97/ADGRG3 is an adhesion GPCR with incompletely understood functions.
  • Understanding adhesion GPCRs is key to deciphering developmental and physiological regulation.

Purpose of the Study:

  • To elucidate the activation mechanism of the adhesion GPCR GPR97/ADGRG3.
  • To investigate the cellular roles and functions of GPR97/ADGRG3.
  • To provide novel insights into the broader adhesion GPCR family.

Main Methods:

  • Biochemical assays to study receptor activation.
  • Cell-based assays to determine cellular functions.
  • Genetic manipulation to probe GPR97/ADGRG3 roles.

Main Results:

  • Detailed characterization of GPR97/ADGRG3 activation pathways.
  • Identification of specific cellular processes regulated by GPR97/ADGRG3.
  • New data on the structure-function relationship of adhesion GPCRs.

Conclusions:

  • GPR97/ADGRG3 plays a significant role in cellular signaling and organ system physiology.
  • The findings advance our understanding of adhesion GPCR activation.
  • This study offers a foundation for future research into GPR97/ADGRG3 and related receptors.