ArticleFrontiers in pharmacology2023
Identification of the molecular determinants of antagonist potency in the allosteric binding pocket of human P2X4.
Article in Frontiers in pharmacology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Novel P2X4 Receptor Antagonist MRS4719 Improves Ischemia/reperfusion Injury in Mice.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Article
- Understanding interspecies drug response variations between human and rodent P2X7 receptors.Nature communications · 2025Article
- Involvement of purinergic signalling in the vasomotor response to hypochlorous acid in porcine coronary artery.Purinergic signalling · 2025Article
- Structural insights into the allosteric inhibition of P2X4 receptors.Nature communications · 2023Article
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Authors and funding
4 authors.
Funding
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Abstract
P2X receptors are a family of ATP-gated cation channels comprising seven subtypes in mammals, which play key roles in nerve transmission, pain sensation and inflammation. The P2X4 receptor in particular has attracted significant interest from pharmaceutical companies due to its physiological roles in neuropathic pain and modulation of vascular tone. A number of potent small-molecule P2X4 receptor antagonists have been developed, including the allosteric P2X4 receptor antagonist BX430, which is approximately 30-fold more potent at human P2X4 compared with the rat isoform. A single amino-acid difference between human and rat P2X4 (I312T), located in an allosteric pocket, has previously been identified as critical for BX430 sensitivity, implying that BX430 binds in this pocket. Using a combination of mutagenesis, functional assay in mammalian cells and
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