Target Information

Target General Infomation
Target ID
T17140
Former ID
TTDR00278
Target Name
P2X purinoceptor 3
Gene Name
P2RX3
Synonyms
ATP receptor; ATP-gated ion channel P2X(3); P2X3; P2X3 receptor; Purinergic receptor; P2RX3
Target Type
Clinical Trial
Disease Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Function
Receptor for ATP that acts as a ligand-gated ionchannel.
BioChemical Class
ATP-gated P2X receptor cation channel
Target Validation
T17140
UniProt ID
P56373
Sequence
MNCISDFFTYETTKSVVVKSWTIGIINRVVQLLIISYFVGWVFLHEKAYQVRDTAIESSV
VTKVKGSGLYANRVMDVSDYVTPPQGTSVFVIITKMIVTENQMQGFCPESEEKYRCVSDS
QCGPERLPGGGILTGRCVNYSSVLRTCEIQGWCPTEVDTVETPIMMEAENFTIFIKNSIR
FPLFNFEKGNLLPNLTARDMKTCRFHPDKDPFCPILRVGDVVKFAGQDFAKLARTGGVLG
IKIGWVCDLDKAWDQCIPKYSFTRLDSVSEKSSVSPGYNFRFAKYYKMENGSEYRTLLKA
FGIRFDVLVYGNAGKFNIIPTIISSVAAFTSVGVGTVLCDIILLNFLKGADQYKAKKFEE
VNETTLKIAALTNPVYPSDQTTAEKQSTDSGAFSIGH
Drugs and Mode of Action
Drug(s) AF-219 Drug Info Phase 2 Overactive bladder disorder [525238]
Antagonist A-317491 Drug Info [535840]
AF-219 Drug Info [533055]
AF353 Drug Info [531000]
MK-3901 Drug Info [543849]
RO3 Drug Info [528022]
TNP-ATP Drug Info [534640]
Inhibitor AVVYPWT Drug Info [528976]
Cyclic LVVYPWT Drug Info [528976]
ISOPPADS Drug Info [526106]
LAVYPWT Drug Info [528976]
LVAYPWT Drug Info [528976]
LVVAPWT Drug Info [528976]
LVVYPWT Drug Info [528976]
Agonist BzATP Drug Info [543849]
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
References
Ref 525238ClinicalTrials.gov (NCT02477709) A Study to Assess the Tolerability of a Single Dose of AF-219 in Subjects With Idiopathic Pulmonary Fibrosis (IPF).
Ref 526106J Med Chem. 2001 Feb 1;44(3):340-9.Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
Ref 528022Purinoceptors as therapeutic targets for lower urinary tract dysfunction. Br J Pharmacol. 2006 Feb;147 Suppl 2:S132-43.
Ref 528976J Med Chem. 2007 Sep 6;50(18):4543-7. Epub 2007 Aug 3.Structure-activity relationship studies of spinorphin as a potent and selective human P2X(3) receptor antagonist.
Ref 531000AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist. Br J Pharmacol. 2010 Jul;160(6):1387-98.
Ref 533055P2X3 receptor antagonist (AF-219) in refractory chronic cough: a randomised, double-blind, placebo-controlled phase 2 study. Lancet. 2015 Mar 28;385(9974):1198-205.
Ref 534640Trinitrophenyl-substituted nucleotides are potent antagonists selective for P2X1, P2X3, and heteromeric P2X2/3 receptors. Mol Pharmacol. 1998 Jun;53(6):969-73.
Ref 535840Crossing the pain barrier: P2 receptors as targets for novel analgesics. J Physiol. 2003 Dec 15;553(Pt 3):683-94. Epub 2003 Sep 26.
Ref 543849(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 480).

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