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P2RX3
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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
[edit]Antagonists
[edit]Not true antagonists, but negative allosteric modulators:
- Camlipixant (BLU-5937)
- Gefapixant
- Opiranserin
- Quercetin[7]
- PSFL2915[7]
See also
[edit]References
[edit]- ^ a b c GRCh38: Ensembl release 89: ENSG00000109991 – Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000027071 – Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ Garcia-Guzman M, Stühmer W, Soto F (July 1997). "Molecular characterization and pharmacological properties of the human P2X3 purinoceptor". Brain Research. Molecular Brain Research. 47 (1–2): 59–66. doi:10.1016/S0169-328X(97)00036-3. PMID 9221902.
- ^ a b "Entrez Gene: P2RX3 purinergic receptor P2X, ligand-gated ion channel, 3".
- ^ a b Guo CR, Zhang ZZ, Zhou X, Sun MY, Li TT, Lei YT, et al. (September 2023). "Chronic cough relief by allosteric modulation of P2X3 without taste disturbance". Nature Communications. 14 (1) 5844. Bibcode:2023NatCo..14.5844G. doi:10.1038/s41467-023-41495-0. PMC 10511716. PMID 37730705.
Further reading
[edit]- North RA (October 2002). "Molecular physiology of P2X receptors". Physiological Reviews. 82 (4): 1013–1067. doi:10.1152/physrev.00015.2002. PMID 12270951.
- Jarvis MF (August 2003). "Contributions of P2X3 homomeric and heteromeric channels to acute and chronic pain". Expert Opinion on Therapeutic Targets. 7 (4): 513–522. doi:10.1517/14728222.7.4.513. PMID 12885270. S2CID 25459817.
- Kennedy C, Leff P (October 1995). "Painful connection for ATP". Nature. 377 (6548): 385–386. Bibcode:1995Natur.377..385K. doi:10.1038/377385a0. PMID 7566110. S2CID 4315283.
- Lewis C, Neidhart S, Holy C, North RA, Buell G, Surprenant A (October 1995). "Coexpression of P2X2 and P2X3 receptor subunits can account for ATP-gated currents in sensory neurons". Nature. 377 (6548): 432–435. Bibcode:1995Natur.377..432L. doi:10.1038/377432a0. PMID 7566120. S2CID 4361850.
- Garcia-Guzman M, Soto F, Gomez-Hernandez JM, Lund PE, Stühmer W (January 1997). "Characterization of recombinant human P2X4 receptor reveals pharmacological differences to the rat homologue". Molecular Pharmacology. 51 (1): 109–118. doi:10.1124/mol.51.1.109. PMID 9016352.
- Cook SP, McCleskey EW (October 2000). "ATP, pain and a full bladder". Nature. 407 (6807): 951–952. Bibcode:2000Natur.407..951C. doi:10.1038/35039648. PMID 11069162. S2CID 4367628.
- Renton T, Yiangou Y, Baecker PA, Ford AP, Anand P (2003). "Capsaicin receptor VR1 and ATP purinoceptor P2X3 in painful and nonpainful human tooth pulp". Journal of Orofacial Pain. 17 (3): 245–250. PMID 14520770.
- Mason HS, Bourke S, Kemp PJ (December 2004). "Selective modulation of ligand-gated P2X purinoceptor channels by acute hypoxia is mediated by reactive oxygen species". Molecular Pharmacology. 66 (6): 1525–1535. doi:10.1124/mol.104.000851. PMID 15331767. S2CID 24536809.
- Fabbretti E, Sokolova E, Masten L, D'Arco M, Fabbro A, Nistri A, et al. (December 2004). "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. doi:10.1074/jbc.M409772200. PMID 15475563.
- Brown DA, Yule DI (February 2007). "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. doi:10.1016/j.bbamcr.2006.09.020. PMC 1861828. PMID 17052768.
External links
[edit]- 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.
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