P2RX3

P2RX3
Identifiers
Aliases	P2RX3, P2X3, purinergic receptor P2X 3
External IDs	OMIM: 600843; MGI: 1097160; HomoloGene: 1922; GeneCards: P2RX3; OMA:P2RX3 - orthologs
Gene location (Human) Chr. Chromosome 11 (human)[1] Band 11q12.1 Start 57,338,352 bp[1] End 57,372,396 bp[1]
Gene location (Mouse) Chr. Chromosome 2 (mouse)[2] Band 2|2 D Start 84,998,583 bp[2] End 85,037,462 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in gonad testicle apex of heart left testis right testis left ventricle right lobe of liver left adrenal cortex right adrenal gland striated muscle tissue Top expressed in lumbar spinal ganglion spermatid ganglion of vagus nerve trigeminal ganglion blastocyst seminiferous tubule greater petrosal nerve spermatocyte neural tube tail of embryo More reference expression data BioGPS n/a
Gene ontology Molecular function purinergic nucleotide receptor activity ion channel activity ATP binding extracellularly ATP-gated cation channel activity nucleotide binding ATP-gated ion channel activity Cellular component integral component of membrane rough endoplasmic reticulum Golgi apparatus membrane receptor complex dendritic spine integral component of nuclear inner membrane integral component of plasma membrane soma terminal bouton axon membrane raft neuron projection plasma membrane Schaffer collateral - CA1 synapse hippocampal mossy fiber to CA3 synapse integral component of presynaptic membrane Biological process peristalsis response to ATP response to hypoxia positive regulation of calcium-mediated signaling positive regulation of calcium ion transport into cytosol urinary bladder smooth muscle contraction response to mechanical stimulus cation transport response to heat ion transport behavioral response to formalin induced pain response to organic substance cation transmembrane transport regulation of synaptic plasticity neuromuscular synaptic transmission positive regulation of sensory perception of pain behavioral response to pain response to cold protein homooligomerization response to carbohydrate sensory perception of taste signal transduction neuronal action potential response to temperature stimulus chemical synaptic transmission purinergic nucleotide receptor signaling pathway blood coagulation excitatory postsynaptic potential protein homotrimerization cellular response to ATP modulation of chemical synaptic transmission ion transmembrane transport Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 5024 228139 Ensembl ENSG00000109991 ENSMUSG00000027071 UniProt P56373 Q3UR32 RefSeq (mRNA) NM_002559 NM_145526 RefSeq (protein) NP_002550 NP_663501 Location (UCSC) Chr 11: 57.34 – 57.37 Mb Chr 2: 85 – 85.04 Mb PubMed search [3] [4]
Wikidata
View/Edit Human View/Edit Mouse

P2X purinoceptor 3 is a protein that in humans is encoded by the P2RX3 gene.^[5][6]

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.^[6]

Ligands

Antagonists

Not true antagonists, but negative allosteric modulators:

• Camlipixant (BLU-5937)
• Gefapixant
• Opiranserin
• Quercetin^[7]
• PSFL2915^[7]

See also

• P2X purinoreceptor
• Purinergic receptor
• Ligand-gated ion channel
• Nociceptor

References

1. GRCh38: Ensembl release 89: ENSG00000109991 – Ensembl, May 2017
2. GRCm38: Ensembl release 89: ENSMUSG00000027071 – Ensembl, May 2017
3. "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
4. "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
5. Garcia-Guzman M, Stuhmer W, Soto F (Sep 1997). "Molecular characterization and pharmacological properties of the human P2X3 purinoceptor". Brain Res Mol Brain Res. 47 (1–2): 59–66. doi:10.1016/S0169-328X(97)00036-3. PMID 9221902.
6. "Entrez Gene: P2RX3 purinergic receptor P2X, ligand-gated ion channel, 3".
7. Guo, Chang-Run; Zhang, Zhong-Zhe; Zhou, Xing; Sun, Meng-Yang; Li, Tian-Tian; Lei, Yun-Tao; Gao, Yu-Hao; Li, Qing-Quan; Yue, Chen-Xi; Gao, Yu; Lin, Yi-Yu; Hao, Cui-Yun; Li, Chang-Zhu; Cao, Peng; Zhu, Michael X.; Rong, Ming-Qiang; Wang, Wen-Hui; Yu, Ye (20 September 2023). "Chronic cough relief by allosteric modulation of P2X3 without taste disturbance". Nature Communications. 14 (1): 5844. doi:10.1038/s41467-023-41495-0. PMC 10511716. PMID 37730705.

Further reading

• North RA (2002). "Molecular physiology of P2X receptors". Physiol. Rev. 82 (4): 1013–67. doi:10.1152/physrev.00015.2002. PMID 12270951.
• Jarvis MF (2005). "Contributions of P2X3 homomeric and heteromeric channels to acute and chronic pain". Expert Opin. Ther. Targets. 7 (4): 513–22. doi:10.1517/14728222.7.4.513. PMID 12885270. S2CID 25459817.
• Kennedy C, Leff P (1995). "Painful connection for ATP". Nature. 377 (6548): 385–6. Bibcode:1995Natur.377..385K. doi:10.1038/377385a0. PMID 7566110. S2CID 4315283.
• Lewis C, Neidhart S, Holy C, et al. (1995). "Coexpression of P2X2 and P2X3 receptor subunits can account for ATP-gated currents in sensory neurons". Nature. 377 (6548): 432–5. Bibcode:1995Natur.377..432L. doi:10.1038/377432a0. PMID 7566120. S2CID 4361850.
• Garcia-Guzman M, Soto F, Gomez-Hernandez JM, et al. (1997). "Characterization of recombinant human P2X4 receptor reveals pharmacological differences to the rat homologue". Mol. Pharmacol. 51 (1): 109–18. doi:10.1124/mol.51.1.109. PMID 9016352.
• Cook SP, McCleskey EW (2000). "ATP, pain and a full bladder". Nature. 407 (6807): 951–2. Bibcode:2000Natur.407..951C. doi:10.1038/35039648. PMID 11069162. S2CID 4367628.
• Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. Bibcode:2002PNAS...9916899M. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
• Renton T, Yiangou Y, Baecker PA, et al. (2003). "Capsaicin receptor VR1 and ATP purinoceptor P2X3 in painful and nonpainful human tooth pulp". Journal of Orofacial Pain. 17 (3): 245–50. PMID 14520770.
• Mason HS, Bourke S, Kemp PJ (2005). "Selective modulation of ligand-gated P2X purinoceptor channels by acute hypoxia is mediated by reactive oxygen species". Mol. Pharmacol. 66 (6): 1525–35. doi:10.1124/mol.104.000851. PMID 15331767. S2CID 24536809.
• Fabbretti E, Sokolova E, Masten L, et al. (2005). "Identification of negative residues in the P2X3 ATP receptor ectodomain as structural determinants for desensitization and the Ca2+-sensing modulatory sites". J. Biol. Chem. 279 (51): 53109–15. doi:10.1074/jbc.M409772200. PMID 15475563.
• Brown DA, Yule DI (2007). "Protein kinase C regulation of P2X3 receptors is unlikely to involve direct receptor phosphorylation". Biochim. Biophys. Acta. 1773 (2): 166–75. doi:10.1016/j.bbamcr.2006.09.020. PMC 1861828. PMID 17052768.

External links

• P2RX3+protein,+human at the U.S. 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.