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Related Concept Videos

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 Receptors01:15

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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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Genetic Screens02:46

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Genetic screens are tools used to identify genes and mutations responsible for phenotypes of interest. Genetic screens help identify individuals or a group of people at risk of developing  genetic diseases and help them with early intervention, targeted therapy, and reproductive options.
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Related Experiment Video

Updated: Apr 27, 2026

Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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G-protein-coupled receptor screening technologies.

Peter J Greasley1, Frank P Jansen1

  • 1Lead Discovery Sciences, Department of Molecular Pharmacology, AstraZeneca R&D, SE43183 Mölndal, Sweden.

Drug Discovery Today. Technologies
|July 2, 2014
PubMed
Summary
This summary is machine-generated.

Choosing the right assay for high throughput screening (HTS) is crucial for drug discovery. This review covers technologies for screening G-protein-coupled receptors (GPCRs) and factors influencing assay selection.

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Area of Science:

  • Pharmacology
  • Biotechnology
  • Drug Discovery

Background:

  • High throughput screening (HTS) is vital for identifying potential drug candidates.
  • G-protein-coupled receptors (GPCRs) are a major class of drug targets.
  • Advances in technology have enabled large-scale screening of compound libraries.

Purpose of the Study:

  • To review available technologies for screening GPCRs using HTS.
  • To discuss critical factors influencing the selection of screening methodologies for GPCRs.

Main Methods:

  • Literature review of HTS technologies applicable to GPCR screening.
  • Analysis of strategic considerations for assay selection in drug discovery.

Main Results:

  • Several HTS technologies are available for screening GPCRs.
  • The choice of assay depends on various strategic and technical factors.

Conclusions:

  • Selecting an appropriate HTS assay is a critical step in the drug development pipeline.
  • Understanding available technologies and selection criteria is essential for efficient GPCR drug discovery.