P2X receptors in health and disease

G Burnstock1, C Kennedy

  • 1Autonomic Neuroscience Centre, University College Medical School, London, United Kingdom.

Insights

P2X receptors are cation channels crucial for nerve and non-nerve cell function. Targeting these receptors shows therapeutic potential for various diseases, including pain and cancer.

Area of Science:

  • Molecular Biology
  • Neuroscience
  • Pharmacology

Background:

  • P2X receptors are ligand-gated ion channels formed by seven cloned subunits.
  • These receptors are permeable to cations like Na(+), K(+), and Ca(2+).
  • Their structure involves a pore formed by transmembrane region 2 of each subunit.

Purpose of the Study:

  • To describe the structure and function of P2X receptors.
  • To highlight their expression in neuronal and non-neuronal cells.
  • To explore their role in physiological and pathological processes.

Main Methods:

  • Cloning of P2X receptor subunits.
  • Structural analysis of the P2X receptor.
  • Investigation of P2X receptor function upon ATP binding.
  • Analysis of P2X receptor expression patterns.

Main Results:

  • P2X receptors form homo- and heterotrimeric cation channels.
  • ATP binding triggers rapid opening of the channel pore.
  • Receptors are expressed in neurons and various non-neuronal cells, mediating diverse functions.
  • Altered expression is linked to numerous diseases.

Conclusions:

  • P2X receptors play vital roles in neurotransmission, smooth muscle contraction, secretion, and immunomodulation.
  • Dysregulation of P2X receptors is implicated in various pathologies.
  • P2X receptor modulators are promising therapeutic agents for conditions like pain, cystic fibrosis, and cancer.

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