Biology:P2RX3
 Generic protein structure example |
P2X purinoceptor 3 is a protein that in humans is encoded by the P2RX3 gene.[1][2]
The product of this gene belongs to the family of purinoceptors for ATP. This receptor functions as a ligand-gated ion channel and may transduce ATP-evoked nociceptor activation. Mouse studies suggest that this receptor is important for peripheral pain responses, and also participates in pathways controlling urinary bladder volume reflexes, platelet aggregation, macrophage activation, apoptosis and neuronal–glial interactions. It is possible that the development of selective antagonists for this receptor may have a therapeutic potential in pain relief and in the treatment of disorders of urine storage.[2]
Ligands
Antagonists
Not true antagonists, but negative allosteric modulators:
- Camlipixant (BLU-5937)
- Gefapixant
- Opiranserin
- Quercetin[3]
- PSFL2915[3]
See also
References
- ↑ "Molecular characterization and pharmacological properties of the human P2X3 purinoceptor". Brain Research. Molecular Brain Research 47 (1–2): 59–66. July 1997. doi:10.1016/S0169-328X(97)00036-3. PMID 9221902.
- ↑ 2.0 2.1 "Entrez Gene: P2RX3 purinergic receptor P2X, ligand-gated ion channel, 3". https://www.ncbi.nlm.nih.gov/gene?Db=gene&Cmd=ShowDetailView&TermToSearch=5024.
- ↑ 3.0 3.1 "Chronic cough relief by allosteric modulation of P2X3 without taste disturbance". Nature Communications 14 (1). September 2023. doi:10.1038/s41467-023-41495-0. PMID 37730705. Bibcode: 2023NatCo..14.5844G.
Further reading
- "Molecular physiology of P2X receptors". Physiological Reviews 82 (4): 1013–1067. October 2002. doi:10.1152/physrev.00015.2002. PMID 12270951.
- "Contributions of P2X3 homomeric and heteromeric channels to acute and chronic pain". Expert Opinion on Therapeutic Targets 7 (4): 513–522. August 2003. doi:10.1517/14728222.7.4.513. PMID 12885270.
- "Painful connection for ATP". Nature 377 (6548): 385–386. October 1995. doi:10.1038/377385a0. PMID 7566110. Bibcode: 1995Natur.377..385K.
- "Coexpression of P2X2 and P2X3 receptor subunits can account for ATP-gated currents in sensory neurons". Nature 377 (6548): 432–435. October 1995. doi:10.1038/377432a0. PMID 7566120. Bibcode: 1995Natur.377..432L.
- "Characterization of recombinant human P2X4 receptor reveals pharmacological differences to the rat homologue". Molecular Pharmacology 51 (1): 109–118. January 1997. doi:10.1124/mol.51.1.109. PMID 9016352.
- "ATP, pain and a full bladder". Nature 407 (6807): 951–952. October 2000. doi:10.1038/35039648. PMID 11069162. Bibcode: 2000Natur.407..951C.
- "Capsaicin receptor VR1 and ATP purinoceptor P2X3 in painful and nonpainful human tooth pulp". Journal of Orofacial Pain 17 (3): 245–250. 2003. PMID 14520770.
- "Selective modulation of ligand-gated P2X purinoceptor channels by acute hypoxia is mediated by reactive oxygen species". Molecular Pharmacology 66 (6): 1525–1535. December 2004. doi:10.1124/mol.104.000851. PMID 15331767.
- "Identification of negative residues in the P2X3 ATP receptor ectodomain as structural determinants for desensitization and the Ca2+-sensing modulatory sites". The Journal of Biological Chemistry 279 (51): 53109–53115. December 2004. doi:10.1074/jbc.M409772200. PMID 15475563.
- "Protein kinase C regulation of P2X3 receptors is unlikely to involve direct receptor phosphorylation". Biochimica et Biophysica Acta (BBA) - Molecular Cell Research 1773 (2): 166–175. February 2007. doi:10.1016/j.bbamcr.2006.09.020. PMID 17052768.
External links
- P2RX3+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH)
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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