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Updated: Jun 1, 2026

Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels
Published on: May 18, 2009
P2X receptors in health and disease
1Autonomic Neuroscience Centre, University College Medical School, London, United Kingdom.
Abstract:
Seven P2X receptor subunits have been cloned which form functional homo- and heterotrimers. These are cation-selective channels, equally permeable to Na(+) and K(+) and with significant Ca(2+) permeability. The three-dimensional structure of the P2X receptor is described. The channel pore is formed by the α-helical transmembrane spanning region 2 of each subunit. When ATP binds to a P2X receptor, the pore opens within milliseconds, allowing the cations to flow. P2X receptors are expressed on both central and peripheral neurons, where they are involved in neuromuscular and synaptic neurotransmission and neuromodulation. They are also expressed in most types of nonneuronal cells and mediate a wide range of actions, such as contraction of smooth muscle, secretion, and immunomodulation. Changes in the expression of P2X receptors have been characterized in many pathological conditions of the cardiovascular, gastrointestinal, respiratory, and urinogenital systems and in the brain and special senses. The therapeutic potential of P2X receptor agonists and antagonists is currently being investigated in a range of disorders, including chronic neuropathic and inflammatory pain, depression, cystic fibrosis, dry eye, irritable bowel syndrome, interstitial cystitis, dysfunctional urinary bladder, and cancer.
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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