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Related Concept Videos

GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...
Amplifying Signals via Enzymatic Cascade01:22

Amplifying Signals via Enzymatic Cascade

When a ligand binds to a cell-surface receptor, the receptor's intracellular domain changes shape, which may either activate its enzyme function or allow its binding to other molecules. The initial signal is amplified by most signal transduction pathways. This means that a single ligand molecule can activate multiple molecules of a downstream target. Proteins that relay a signal are most commonly phosphorylated at one or more sites, activating or inactivating the protein. Kinases catalyze the...
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.
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...
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...

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Related Experiment Video

Updated: Jun 27, 2026

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

Engineered GPCRs as tools to modulate signal transduction.

Ying Pei1, Sarah C Rogan, Feng Yan

  • 1Department of Pharmacology, University of North Carolina, Chapel Hill, North Carolina, USA.

Physiology (Bethesda, Md.)
|December 17, 2008
PubMed
Summary

Engineered receptors, RASSLs and DREADDs, offer exclusive control over G-protein-coupled receptor (GPCR) activation. These tools enable precise study of GPCR signaling in specific cells and organisms.

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Last Updated: Jun 27, 2026

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

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

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

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A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors
08:46

A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors

Published on: December 2, 2022

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Neuroscience

Background:

  • G-protein-coupled receptors (GPCRs) are crucial cell surface receptors involved in numerous physiological processes.
  • Understanding GPCR signaling pathways is essential for developing targeted therapeutics.
  • Existing methods for studying GPCRs can be limited by endogenous ligand interference.

Purpose of the Study:

  • To introduce engineered GPCRs, RASSLs and DREADDs, for exclusive activation by synthetic ligands.
  • To enable precise investigation of GPCR functions in vitro and in vivo.
  • To facilitate selective study of GPCR signaling in specific cell populations.

Main Methods:

  • Engineering of GPCRs (RASSLs and DREADDs) to be insensitive to endogenous ligands.
  • Activation of engineered receptors using specific synthetic drug-like compounds.
  • Application of these modified GPCRs to study Gi, Gq, and Gs signaling pathways.

Main Results:

  • RASSLs and DREADDs provide exclusive control over GPCR activation.
  • These engineered receptors are activated solely by designer drugs.
  • The tools cover key GPCR signaling pathways (Gi, Gq, Gs).

Conclusions:

  • RASSLs and DREADDs are valuable tools for selective GPCR research.
  • These engineered receptors enhance the ability to study GPCR consequences in vitro and in vivo.
  • The technology allows for targeted investigation of GPCR functions in specific cellular contexts.