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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...
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...
GPCR Desensitization01:12

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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.
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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.

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Updated: Jun 1, 2026

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

Examining site-specific GPCR phosphorylation.

Adrian J Butcher1, Andrew B Tobin, Kok Choi Kong

  • 1Department of Cell Physiology and Pharmacology and the Protein and Nucleic Acid Chemistry Laboratory, University of Leicester, Leicester, UK.

Methods in Molecular Biology (Clifton, N.J.)
|May 25, 2011
PubMed
Summary
This summary is machine-generated.

Phosphorylation of G protein-coupled receptors (GPCRs) is a key modification affecting signaling. New methods allow detailed investigation of site-specific phosphorylation, revealing tissue-specific functions.

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Oligopeptide Competition Assay for Phosphorylation Site Determination
09:16

Oligopeptide Competition Assay for Phosphorylation Site Determination

Published on: May 18, 2017

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) undergo phosphorylation upon agonist stimulation.
  • This modification influences receptor desensitization and signaling pathway recruitment via arrestin proteins.
  • Emerging evidence indicates phosphorylation regulates cell-type-specific GPCR signaling and tissue functions.

Purpose of the Study:

  • To present laboratory methods for investigating site-specific phosphorylation of the M₃-muscarinic receptor.
  • To provide a framework for studying GPCR phosphorylation and its functional consequences.

Main Methods:

  • Detailed description of experimental techniques for identifying phospho-acceptor sites on GPCRs.
  • Methodology for analyzing the functional outcomes of site-specific phosphorylation.
  • Application to the M₃-muscarinic receptor as a model system.

Main Results:

  • Established methods for precise determination of M₃-muscarinic receptor phosphorylation sites.
  • Demonstrated the utility of these methods in understanding GPCR regulation.
  • Highlighted the potential for broader application to other GPCRs.

Conclusions:

  • Site-specific phosphorylation is a critical regulator of GPCR function.
  • The presented methods facilitate in-depth analysis of GPCR phosphorylation.
  • These techniques can be adapted for studying diverse receptors and their signaling.