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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

17.9K
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

132.4K
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.
132.4K
GPCR Desensitization01:12

GPCR Desensitization

8.3K
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...
8.3K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

7.7K
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...
7.7K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

11.8K
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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Updated: Feb 18, 2026

Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons
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Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons

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Extending the Structural View of Class B GPCRs.

Chris de Graaf1, Gaojie Song2, Can Cao3

  • 1Division of Medicinal Chemistry, Faculty of Sciences, Amsterdam Institute for Molecules, Medicines and Systems (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, Amsterdam 1081 HZ, The Netherlands; These authors contributed equally.

Trends in Biochemical Sciences
|November 15, 2017
PubMed
Summary

Recent structural studies reveal how secretin-like class B G protein-coupled receptors (GPCRs) bind ligands and activate signaling pathways. This offers new avenues for drug discovery targeting hormonal homeostasis.

Keywords:
calcitonin receptorclass B G protein-coupled receptorglucagon receptorglucagon-like peptide-1 receptorstructural biologystructure–function relationship

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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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Last Updated: Feb 18, 2026

Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons
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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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Area of Science:

  • Biochemistry
  • Pharmacology
  • Structural Biology

Background:

  • Secretin-like class B G protein-coupled receptors (GPCRs) are crucial for hormonal balance.
  • Recent structural data offers novel insights into their function.

Purpose of the Study:

  • To comprehensively review structural, biochemical, and pharmacological data on class B GPCRs.
  • To understand ligand-receptor interactions and modulation mechanisms.
  • To explore drug discovery potential for the secretin-like GPCR family.

Main Methods:

  • Analysis of recent structural data of class B GPCRs.
  • Biochemical assays.
  • Pharmacological studies.

Main Results:

  • Identified ligand-induced domain reorientation in class B GPCRs.
  • Elucidated intramolecular networks stabilizing G protein binding.
  • Demonstrated allosteric modulation of receptor activation.

Conclusions:

  • Structural insights enhance understanding of class B GPCR mechanisms.
  • Ligand-receptor interactions and allosteric modulation are key.
  • Significant potential for drug discovery in hormonal regulation.