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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

19.4K
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 Receptors01:15

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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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G-protein Coupled Receptors01:21

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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.
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G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

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GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
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GPCRdb: the G protein-coupled receptor database - an introduction.

C Munk1, V Isberg1, S Mordalski2

  • 1Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.

British Journal of Pharmacology
|May 9, 2016
PubMed
Summary

GPCRdb provides integrated data and web tools for G protein-coupled receptors (GPCRs), aiding drug design. This review details GPCRdb services for researchers studying these crucial membrane proteins and drug targets.

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Area of Science:

  • Biochemistry and structural biology
  • Pharmacology and drug discovery
  • Bioinformatics and computational biology

Background:

  • G protein-coupled receptors (GPCRs) represent the largest human membrane protein family and are key drug targets.
  • Advances in GPCR pharmacology and crystallography illuminate signal transduction, allosteric modulation, and biased signaling, informing novel drug design principles.
  • The GPCR database (GPCRdb) has supported the research community for over two decades and now caters to a broader, multidisciplinary audience.

Purpose of the Study:

  • To introduce new users to the comprehensive services offered by GPCRdb.
  • To highlight GPCRdb's role in providing integrated, annotated reference data on GPCRs, including sequences, structures, mutations, and ligand interactions.
  • To showcase GPCRdb's suite of web tools for analyzing GPCR structures, sequences, relationships, and ligand profiles, and to describe its dissemination of interactive data visualizations.

Main Methods:

  • Data integration and annotation of GPCR information, focusing on sequences, structures, mutations, and ligand interactions.
  • Development and description of web-based tools for analyzing GPCR data, including structural and sequence analysis, receptor relationships, and ligand target profiling.
  • Creation of interactive diagrams for visualizing GPCR residue topologies, phylogenetic relationships, and crystal structure statistics.

Main Results:

  • GPCRdb offers a unified platform for accessing structured reference data on GPCRs.
  • A suite of web tools is available for rapid analysis of GPCR sequences, structures, and ligand interactions.
  • Interactive visualizations facilitate the understanding of GPCR properties and relationships.

Conclusions:

  • GPCRdb serves as an essential resource for researchers studying G protein-coupled receptors.
  • The database and its associated tools empower the scientific community with data and analytical capabilities for GPCR research and drug design.
  • GPCRdb facilitates the dissemination of knowledge through accessible data presentation and cross-referenced complementary resources.