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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

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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Patch Clamp01:18

Patch Clamp

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Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
In this method, a glass micropipette containing electrolyte solution is tightly sealed against a small portion of the cell membrane. As a result, a patch of the cell...
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Related Experiment Video

Updated: Apr 5, 2026

Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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High-Throughput Screening for Allosteric Modulators of GPCRs.

Robert L Bertekap1, Neil T Burford, Zhuyin Li

  • 1Lead Discovery, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT, 06492, USA.

Methods in Molecular Biology (Clifton, N.J.)
|August 12, 2015
PubMed
Summary

Discovering novel drug candidates targeting G protein-coupled receptors (GPCRs) is crucial. This study presents high-throughput screening (HTS) methods optimized for identifying GPCR ligands, especially challenging allosteric modulators.

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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Area of Science:

  • Pharmacology
  • Biochemistry
  • Drug Discovery

Background:

  • G protein-coupled receptor (GPCR) signaling is central to drug discovery.
  • Biased agonism and allosteric modulation are emerging GPCR therapeutic strategies.
  • Novel GPCR-targeted therapeutics offer potential for improved efficacy and safety.

Purpose of the Study:

  • To describe high-throughput screening (HTS) protocols for GPCR ligand identification.
  • To focus on HTS methods for discovering allosteric modulators.
  • To address the challenges in HTS for allosteric GPCR modulators.

Main Methods:

  • Development and application of specialized HTS assays.
  • Screening of large compound libraries for GPCR activity.
  • Protocols tailored for identifying allosteric modulators.

Main Results:

  • Successful implementation of HTS protocols for GPCR ligand discovery.
  • Demonstration of effective strategies for identifying allosteric modulators.
  • Identification of potential chemical leads for GPCR-targeted therapeutics.

Conclusions:

  • Optimized HTS protocols can overcome challenges in identifying GPCR allosteric modulators.
  • These methods facilitate the discovery of novel GPCR-targeted drugs.
  • Advancements in GPCR drug discovery are driven by innovative screening approaches.