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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.
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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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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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Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization
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Galaxy7TM: flexible GPCR-ligand docking by structure refinement.

Gyu Rie Lee1, Chaok Seok2

  • 1Department of Chemistry, Seoul National University, Seoul 151-747, Korea.

Nucleic Acids Research
|May 1, 2016
PubMed
Summary
This summary is machine-generated.

Galaxy7TM enhances G-protein-coupled receptor (GPCR) structure prediction by simultaneously docking ligands and refining structures. This approach improves accuracy over traditional methods for drug discovery.

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Area of Science:

  • Biochemistry
  • Structural Biology
  • Pharmacology

Background:

  • G-protein-coupled receptors (GPCRs) are crucial for signal transduction and represent key drug targets.
  • Accurate prediction of GPCR-ligand complex structures is vital for advancing drug discovery.
  • Existing methods predict GPCR structures first, then dock ligands, potentially leading to inaccuracies as ligand binding influences GPCR conformation.

Purpose of the Study:

  • To develop an improved method for predicting GPCR-ligand complex structures.
  • To address the limitations of sequential structure prediction and ligand docking.
  • To enhance the accuracy of GPCR structure modeling by considering ligand-induced effects.

Main Methods:

  • Introduction of the Galaxy7TM web server for simultaneous GPCR structure improvement and ligand docking.
  • Utilizing GALAXY methods for flexible structure refinement integrated with ligand docking.
  • Comparative analysis against established tools like AutoDock Vina and Rosetta MPrelax.

Main Results:

  • The Galaxy7TM server integrates ligand docking and structure refinement into a single step.
  • Demonstrated superior performance in both ligand docking and GPCR structure refinement compared to existing methods.
  • Provided a more accurate prediction of GPCR structures influenced by specific ligand binding.

Conclusions:

  • Galaxy7TM offers a significant advancement in predicting GPCR-ligand complex structures.
  • The simultaneous approach overcomes limitations of prior sequential methods.
  • This improved accuracy facilitates more effective drug discovery targeting GPCRs.