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Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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.
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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.
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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...
Pharmacogenetics and Pharmacogenomics: Overview01:29

Pharmacogenetics and Pharmacogenomics: Overview

Pharmacogenetics and pharmacogenomics examine how genetic factors influence an individual's response to drugs. While pharmacogenetics focuses on the impact of specific genetic variants on drug effects, pharmacogenomics takes a broader approach, studying how genetic variation across populations contributes to differences in drug responses. These fields aim to explain why individuals may experience varying levels of efficacy or adverse reactions to the same medication.Variability in drug...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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, 7TM, or...

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

G protein-coupled receptor pharmacogenetics.

Miles D Thompson1, Katherine A Siminovitch, David E C Cole

  • 1Department of Laboratory Medicine and Pathobiology, Banting Institute, University of Toronto, Toronto, Ontario, Canada.

Methods in Molecular Biology (Clifton, N.J.)
|March 29, 2008
PubMed
Summary

Common gene variants in G protein-coupled receptors (GPCRs) can change how effective drugs are. Understanding these genetic differences, known as pharmacogenetics, can help personalize medicine and improve drug development.

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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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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

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Last Updated: Jul 6, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

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

Published on: February 20, 2018

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

Area of Science:

  • Pharmacogenetics
  • Molecular biology
  • Drug discovery

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets.
  • Genetic variants in GPCR genes can alter receptor function and drug response.
  • These variants contribute to individual differences in disease susceptibility and treatment outcomes.

Purpose of the Study:

  • To review pharmacogenetic phenomena related to GPCR gene variants.
  • To examine how these variants affect GPCR expression and function.
  • To highlight the potential of pharmacogenomics in drug development and personalized medicine.

Main Methods:

  • Review of existing literature on GPCR pharmacogenetics.
  • Analysis of specific GPCR systems (beta(2)-adrenergic, cysteinyl leukotriene, calcium-sensing receptors).
  • Discussion of variant effects on gene expression, cell surface expression, and receptor activity.

Main Results:

  • GPCR gene variants, including insertions, deletions, and SNPs, impact receptor expression and function.
  • Variants affect receptor trafficking, dimerization, desensitization, ligand binding, and constitutive activity.
  • These alterations contribute to interindividual variability in drug efficacy and disease progression.

Conclusions:

  • Pharmacogenetic assessment is underutilized in GPCR drug development and clinical practice.
  • Personalized pharmacogenomics offers a valuable approach to optimize novel GPCR drug targets.
  • Further integration of pharmacogenetics can enhance drug discovery and clinical application of GPCR-targeting drugs.