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Rapid CommunicationMinireview—Special Issue In Memory Of Avram Goldstein

P2X Receptors as Drug Targets

R. Alan North and Michael F. Jarvis
Molecular Pharmacology April 2013, 83 (4) 759-769; DOI: https://doi.org/10.1124/mol.112.083758
R. Alan North
Faculty of Medical and Human Sciences, University of Manchester, Manchester, United Kingdom (R.A.N.); and Early Discovery, AbbVie, Inc., North Chicago, Illinois (M.F.J.)
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Michael F. Jarvis
Faculty of Medical and Human Sciences, University of Manchester, Manchester, United Kingdom (R.A.N.); and Early Discovery, AbbVie, Inc., North Chicago, Illinois (M.F.J.)
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Abstract

The study of P2X receptors has long been handicapped by a poverty of small-molecule tools that serve as selective agonists and antagonists. There has been progress, particularly in the past 10 years, as cell-based high-throughput screening methods were applied, together with large chemical libraries. This has delivered some drug-like molecules in several chemical classes that selectively target P2X1, P2X3, or P2X7 receptors. Some of these are, or have been, in clinical trials for rheumatoid arthritis, pain, and cough. Current preclinical research programs are studying P2X receptor involvement in pain, inflammation, osteoporosis, multiple sclerosis, spinal cord injury, and bladder dysfunction. The determination of the atomic structure of P2X receptors in closed and open (ATP-bound) states by X-ray crystallography is now allowing new approaches by molecular modeling. This is supported by a large body of previous work using mutagenesis and functional expression, and is now being supplemented by molecular dynamic simulations and in silico ligand docking. These approaches should lead to P2X receptors soon taking their place alongside other ion channel proteins as therapeutically important drug targets.

Footnotes

  • This work was supported by the Wellcome Trust [Grant 093140/Z/10/Z].

  • dx.doi.org/10.1124/mol.112.083758.

  • Received November 16, 2012.
  • Accepted December 19, 2012.
  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 83 (4)
Molecular Pharmacology
Vol. 83, Issue 4
1 Apr 2013
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Rapid CommunicationMinireview—Special Issue In Memory Of Avram Goldstein

P2X Receptors as Drug Targets

R. Alan North and Michael F. Jarvis
Molecular Pharmacology April 1, 2013, 83 (4) 759-769; DOI: https://doi.org/10.1124/mol.112.083758

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Rapid CommunicationMinireview—Special Issue In Memory Of Avram Goldstein

P2X Receptors as Drug Targets

R. Alan North and Michael F. Jarvis
Molecular Pharmacology April 1, 2013, 83 (4) 759-769; DOI: https://doi.org/10.1124/mol.112.083758
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