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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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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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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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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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Ligand Binding Sites02:40

Ligand Binding Sites

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Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
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GPCRdb in 2018: adding GPCR structure models and ligands.

Gáspár Pándy-Szekeres1,2, Christian Munk1, Tsonko M Tsonkov1

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

Nucleic Acids Research
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Summary
This summary is machine-generated.

This study introduces high-quality G protein-coupled receptor (GPCR) homology models and a comprehensive ligand database, enhancing GPCR research and drug discovery efforts.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Structural Biology

Background:

  • G protein-coupled receptors (GPCRs) are crucial for human signaling and drug development.
  • Existing GPCR resources lack comprehensive, high-quality structural and ligand data.

Purpose of the Study:

  • To develop GPCRome-wide homology models of superior quality.
  • To create an extensive database of GPCR ligands with activity and availability data.
  • To facilitate GPCR research and drug discovery through accessible data and tools.

Main Methods:

  • Utilized a 'Less model - more Xtal' strategy employing main and local templates for homology modeling.
  • Integrated approximately 150,000 GPCR ligands with biological activity and commercial availability data.
  • Developed specialized browsers for receptor and ligand filtering, data download, and analysis.

Main Results:

  • Generated GPCRome-wide homology models with unprecedented quality, outperforming existing resources.
  • Refined crystal structures and modeled missing or distorted regions.
  • Established a versatile ligand database with detailed activity profiles and commercial sourcing information.
  • Provided downloadable SMILES structures and activity spreadsheets.

Conclusions:

  • The enhanced GPCRdb resource significantly advances the investigation of GPCRs.
  • Improved models and comprehensive ligand data empower the wider scientific community in GPCR research.
  • Facilitates analysis of GPCR drugs, G protein selectivity, and genetic variants.