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Updated: May 15, 2026
16:36
Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels
Published on: May 18, 2009
P2X receptors as drug targets
R Alan North1, Michael F Jarvis
1Faculty of Medical and Human Sciences, University of Manchester, Oxford Road, Manchester M13 9PL, UK. r.a.north@manchester.ac.uk
Molecular Pharmacology
|December 21, 2012
Summary
Researchers are developing new small-molecule tools to target P2X receptors for various diseases. Advances in screening and structural biology are accelerating the discovery of potential P2X receptor therapeutics.
Area of Science:
- Pharmacology
- Molecular Biology
- Drug Discovery
Background:
- P2X receptors are crucial ion channels implicated in numerous physiological and pathological processes.
- The development of selective small-molecule modulators for P2X receptors has been historically challenging due to a lack of effective tools.
Purpose of the Study:
- To review the progress in developing selective small-molecule agonists and antagonists for P2X receptors.
- To highlight the therapeutic potential of targeting P2X receptors for various diseases.
Main Methods:
- High-throughput screening of large chemical libraries.
- Structure determination of P2X receptors using X-ray crystallography.
- Molecular modeling, dynamic simulations, and in silico ligand docking.
Main Results:
- Identification of drug-like molecules targeting P2X1, P2X3, and P2X7 receptors.
- Several P2X receptor modulators have entered or are in clinical trials for conditions like rheumatoid arthritis, pain, and cough.
- Ongoing preclinical research explores P2X receptor roles in pain, inflammation, osteoporosis, multiple sclerosis, spinal cord injury, and bladder dysfunction.
Conclusions:
- Significant advancements in small-molecule tool development have been made for P2X receptors.
- Structural biology and computational approaches are enabling new strategies for P2X receptor drug discovery.
- P2X receptors are emerging as important therapeutic targets for a range of human diseases.
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