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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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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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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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Protein Organization01:24

Protein Organization

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Proteins are polymers of amino acid residues. They are versatile and responsible for different cellular functions, including DNA replication, molecular transport, catalysis, and structural support. Proteins have a hierarchical structure comprising at least three levels of organization: primary, secondary, and tertiary structure. Some large proteins have a quaternary structure where individual protein subunits are linked together.
The primary structure of a protein is its amino acid sequence....
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Updated: Nov 27, 2025

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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GPCRdb in 2021: integrating GPCR sequence, structure and function.

Albert J Kooistra1, Stefan Mordalski1, Gáspár Pándy-Szekeres1,2

  • 1Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.

Nucleic Acids Research
|December 3, 2020
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Summary
This summary is machine-generated.

The GPCRdb provides researchers with integrated sequence, structure, and function data for G protein-coupled receptors (GPCRs), a major drug target family. This updated resource enhances drug discovery and understanding of GPCRs.

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Area of Science:

  • Biochemistry and Molecular Biology
  • Pharmacology
  • Bioinformatics

Background:

  • G protein-coupled receptors (GPCRs) are the largest membrane protein family and a primary target for one-third of all marketed drugs.
  • The GPCR database (GPCRdb) is a vital resource for over 4,000 researchers monthly, offering data and tools for GPCR research.

Purpose of the Study:

  • To describe new and updated resources within GPCRdb, emphasizing the integration of sequence, structure, and function data.
  • To enhance GPCRdb's utility for researchers by expanding its data coverage and analytical tools.

Main Methods:

  • Integration of comprehensive datasets including all human non-olfactory GPCRs, orthologs, G-proteins, arrestins, drugs, and ligands.
  • Annotation and refinement of all published GPCR structures, including the generation of models for inactive, intermediate, and active receptor states.
  • Development and updating of bioinformatics tools for sequence signature analysis, ligand site mutation design, and structure determination construct design.

Main Results:

  • GPCRdb now includes extensive data on GPCRs, G-proteins, arrestins, drugs, and ligands, with detailed activity and availability information.
  • Annotated and refined GPCR structures are available, alongside predictive models for receptor conformational states.
  • New and updated tools facilitate the identification of functional residues and the design of experiments for GPCR structure determination and mutagenesis.

Conclusions:

  • The enhanced GPCRdb offers a powerful, integrated platform for GPCR research, supporting data analysis, experiment design, and knowledge dissemination.
  • These updates significantly improve the resource's value for researchers investigating GPCRs, their ligands, and their roles in medicine.