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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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The Two-State Receptor Model01:29

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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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Biasing the odds: Approaches to capturing, understanding and exploiting functional selectivity in GPCRs.

Terence E Hébert1

  • 1Department of Pharmacology and Therapeutics, McGill University, Canada.

Methods (San Diego, Calif.)
|September 30, 2015
PubMed
Summary

Biased signaling offers potential for new drugs by targeting specific molecular pathways. This issue provides a framework with methods to characterize functional selectivity from cell to organism, aiding drug development.

Keywords:
Biased signallingG protein-coupled receptorsGenomic profilingScreening

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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Molecular Biology

Background:

  • Biased signaling is recognized for its potential to yield novel therapeutics and enhance understanding of molecular targets in vivo.
  • The pharmaceutical industry remains cautious, viewing biased signaling as a potential but unproven area.
  • Translating the promise of biased ligands into clinical success requires robust characterization methods from cellular to in vivo levels.

Purpose of the Study:

  • To establish a methodological and analytical framework for characterizing functional selectivity.
  • To bridge the gap between in vitro findings and in vivo efficacy of biased ligands.
  • To provide researchers with the necessary tools and approaches to advance biased signaling research.

Main Methods:

  • The collection presents a series of articles detailing experimental and analytical approaches.
  • Focus on methods for assessing functional selectivity across different biological scales (in cellulo to in vivo).
  • Emphasis on creating a reproducible and standardized framework for characterizing biased ligands.

Main Results:

  • The compilation offers a comprehensive overview of current methodologies for studying biased signaling.
  • Provides a roadmap for the systematic characterization of functional selectivity.
  • Highlights the importance of integrated approaches for drug development.

Conclusions:

  • A clear plan and appropriate tools are essential for realizing the therapeutic potential of biased signaling.
  • This Methods issue provides a foundational framework to guide future research and development in this field.
  • Successful implementation of these methods will facilitate the translation of biased ligands into effective medicines.