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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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Ligand Binding Sites02:40

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Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
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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.
GPCRs are also called heptahelical,...
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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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Related Experiment Video

Updated: Mar 26, 2026

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
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Identifying ligands at orphan GPCRs: current status using structure-based approaches.

Tony Ngo1,2, Irina Kufareva3, James Lj Coleman1,2

  • 1Molecular Cardiology and Biophysics Division, Victor Chang Cardiac Research Institute, Darlinghurst, NSW, Australia.

British Journal of Pharmacology
|February 3, 2016
PubMed
Summary
This summary is machine-generated.

Structure-based drug discovery is crucial for identifying ligands for orphan G protein-coupled receptors (GPCRs). This approach accelerates the exploration of GPCR functions and therapeutic potential, overcoming limitations of traditional methods.

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Area of Science:

  • Pharmacology
  • Molecular Biology
  • Drug Discovery

Background:

  • G protein-coupled receptors (GPCRs) are vital drug targets, but many remain 'orphan' due to undiscovered ligands.
  • Traditional methods for identifying GPCR ligands are slow, necessitating advanced screening approaches.

Purpose of the Study:

  • To review structure-based ligand discovery methods for orphan GPCRs.
  • To highlight the importance of identifying modulators for orphan GPCRs.

Main Methods:

  • Utilizing a growing database of GPCR crystal structures for homology modeling.
  • Establishing appropriate signaling assays to test orphan receptor activity.
  • Applying structure-based drug design to identify small molecule modulators.

Main Results:

  • Structure-based approaches offer efficient strategies for orphan GPCR deorphanization.
  • Recent advances in structural biology provide templates for modeling orphan GPCRs.
  • Examples of successful structure-based ligand identification for orphan GPCRs are presented.

Conclusions:

  • Structure-based ligand discovery is a powerful tool for advancing orphan GPCR pharmacology.
  • This approach facilitates the exploration of physiological functions and therapeutic potential of orphan GPCRs.
  • Continued development of these methods is essential for unlocking the full potential of GPCR-targeted therapeutics.