Signaling at purinergic P2X receptors

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Annmarie Surprenant1, R Alan North

  • 1Faculty of Life Sciences, University of Manchester, Manchester M13 9PT, United Kingdom. a.surprenant@manchester.ac.uk

Annual Review of Physiology
|October 15, 2008
PubMed

Insights

P2X receptors, ATP-gated ion channels, are crucial in pain, blood flow, and inflammation. Research uses antagonists and knockout mice to understand their molecular properties and functions in vertebrates.

Area of Science:

  • Pharmacology and Molecular Biology
  • Cellular Physiology

Background:

  • P2X receptors are vertebrate membrane cation channels activated by extracellular ATP.
  • Seven P2X receptor subunits (P2X1-7) are expressed in various cell types.
  • These receptors are implicated in pain signaling, renal blood flow, and inflammation.

Purpose of the Study:

  • To review the roles and molecular properties of P2X receptors.
  • To highlight evidence from selective antagonists and knockout mouse models.
  • To discuss insights from biophysical studies and related eukaryotic receptors.

Main Methods:

  • Review of experimental evidence using selective P2X receptor antagonists.
  • Analysis of data from P2X receptor knockout mouse studies.
  • Biophysical characterization of mutated P2X receptor subunits in heterologous cells.

Main Results:

  • P2X receptors are trimeric membrane proteins involved in ATP binding, ion permeation, and trafficking.
  • Evidence supports their roles in afferent signaling, renal blood flow, and inflammatory responses.
  • Studies reveal conserved molecular mechanisms across different P2X receptor subtypes.

Conclusions:

  • P2X receptors are vital for physiological processes including pain and vascular function.
  • Understanding their molecular structure aids in developing targeted therapeutic strategies.
  • Comparative analysis with eukaryotic P2X receptors provides evolutionary and functional insights.

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