Related Experiment Video
Updated: Jul 29, 2025
08:21
Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
Published on: June 28, 2019
6.9K
Modulating GPCR and 14-3-3 protein interactions: Prospects for CNS drug discovery.
Sathapana Kongsamut1, Haifeng Eishingdrelo2
1Research Institute for Scientists Emeriti, Drew University, 36 Madison Avenue, Madison, NJ 07940, USA.
Drug Discovery Today
|May 26, 2023
Summary
G-protein-coupled receptors (GPCRs) interact with 14-3-3 proteins, revealing new signaling pathways. This discovery offers novel approaches for studying GPCR function and developing therapeutics.
Area of Science:
- Biochemistry
- Cell Biology
- Pharmacology
Background:
- G-protein-coupled receptors (GPCRs) initiate complex signaling cascades upon activation.
- Key pathways include G-protein and β-arrestin signaling, crucial for cellular responses.
- GPCRs regulate processes like protein trafficking and gene expression.
Purpose of the Study:
- To explore the novel role of 14-3-3 proteins in GPCR signaling.
- To investigate the implications of GPCR-14-3-3 protein interactions for signal transduction.
- To highlight the therapeutic potential of this newly identified signaling axis.
Main Methods:
- The study focuses on the biochemical interactions between GPCRs and 14-3-3 proteins.
- Analysis of ligand-induced interactions and their downstream effects.
- Exploration of GPCR trafficking and signal transduction modulation by 14-3-3 proteins.
Main Results:
- Ligand-induced interactions between GPCRs and 14-3-3 proteins have been identified.
- This interaction establishes a new signaling pathway involving 14-3-3 protein hubs.
- 14-3-3 proteins are shown to be integral to GPCR trafficking and signal transduction.
Conclusions:
- The discovery of GPCR-14-3-3 protein interactions expands the understanding of GPCR signaling.
- This pathway presents new opportunities for investigating GPCR function.
- Harnessing GPCR-mediated 14-3-3 protein signaling holds promise for therapeutic development.
More Related Videos
07:16Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
13.7K
07:41A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
8.9K
Related Concept Videos
01:15G Protein-coupled Receptors
12.4K
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...
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...
12.4K
01:30Ligand-Gated Ion Channel Receptor: Gating Mechanism
2.3K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
2.3K
01:30Transducer Mechanism: G Protein–Coupled Receptors
2.1K
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,...
GPCRs are also called heptahelical,...
2.1K
01:12GPCR Desensitization
6.2K
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...
6.2K
01:09GPCRs Regulate Adenylyl Cylase Activity
5.7K
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...
5.7K
01:21G-protein Coupled Receptors
120.5K
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.
120.5K