Enlightening activation gating in P2X receptors

Related Experiment Video

Updated: Oct 3, 2025

Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels
16:36

Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels

Published on: May 18, 2009

14.8K

Christian Sattler1, Klaus Benndorf2

  • 1Institut Für Physiologie II, Universitätsklinikum Jena, Friedrich-Schiller-Universität Jena, 07740, Jena, Germany. christian.sattler@med.uni-jena.de.

Purinergic Signalling
|February 21, 2022
PubMed

Insights

P2X receptors, ATP-gated ion channels, are crucial drug targets. Novel optical methods reveal conformational changes in P2X receptor activation, advancing understanding of pain and inflammation.

Area of Science:

  • Molecular biology
  • Neuroscience
  • Pharmacology

Background:

  • P2X receptors are trimeric cation channels activated by ATP.
  • They are involved in vital physiological processes like pain and inflammation.
  • Their complex structure and function make them challenging pharmacological targets.

Purpose of the Study:

  • To review novel optical and related approaches for studying P2X receptors.
  • To elucidate conformational changes during P2X receptor activation.
  • To enhance understanding of P2X receptor structure-function relationships.

Main Methods:

  • Review of recent crystal and cryo-EM structures of P2X receptors.
  • Integration of electrophysiological characterization with optical techniques.
  • Analysis of functional and biochemical data in relation to structural insights.

Main Results:

  • Structural data provides a basis for interpreting P2X receptor function.
  • Optical methods offer significant insights into P2X receptor dynamics.
  • Conformational changes during activation are better understood through these approaches.

Conclusions:

  • Novel optical techniques are key to understanding P2X receptor activation mechanisms.
  • Improved knowledge of P2X receptors can lead to new therapeutic strategies.
  • This review highlights advancements in studying these critical ion channels.
Keywords:
Activation gatingComputational modelingLigand bindingP2X receptorsPatch-clamp fluorometryVoltage-clamp fluorometry

More Related Videos

Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time08:33

Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time

Published on: March 11, 2021

2.1K
One-channel Cell-attached Patch-clamp Recording13:07

One-channel Cell-attached Patch-clamp Recording

Published on: June 9, 2014

24.7K

Related Concept Videos

Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

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...
2.8K
G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
4.9K
Mechanically-gated Ion Channels01:12

Mechanically-gated Ion Channels

Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
6.8K
Ligand-gated Ion Channels01:19

Ligand-gated Ion Channels

Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
12.9K
Non-gated Ion Channels01:24

Non-gated Ion Channels

Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism....
7.3K
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...
6.0K