Target Information
Target General Infomation | |||||
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Target ID |
T17140
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Former ID |
TTDR00278
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Target Name |
P2X purinoceptor 3
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Gene Name |
P2RX3
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Synonyms |
ATP receptor; ATP-gated ion channel P2X(3); P2X3; P2X3 receptor; Purinergic receptor; P2RX3
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Target Type |
Clinical Trial
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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.
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BioChemical Class |
ATP-gated P2X receptor cation channel
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Target Validation |
T17140
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UniProt ID | |||||
Sequence |
MNCISDFFTYETTKSVVVKSWTIGIINRVVQLLIISYFVGWVFLHEKAYQVRDTAIESSV
VTKVKGSGLYANRVMDVSDYVTPPQGTSVFVIITKMIVTENQMQGFCPESEEKYRCVSDS QCGPERLPGGGILTGRCVNYSSVLRTCEIQGWCPTEVDTVETPIMMEAENFTIFIKNSIR FPLFNFEKGNLLPNLTARDMKTCRFHPDKDPFCPILRVGDVVKFAGQDFAKLARTGGVLG IKIGWVCDLDKAWDQCIPKYSFTRLDSVSEKSSVSPGYNFRFAKYYKMENGSEYRTLLKA FGIRFDVLVYGNAGKFNIIPTIISSVAAFTSVGVGTVLCDIILLNFLKGADQYKAKKFEE VNETTLKIAALTNPVYPSDQTTAEKQSTDSGAFSIGH |
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Drugs and Mode of Action | |||||
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 | |||||
References | |||||
Ref 526106 | J 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 528022 | Purinoceptors as therapeutic targets for lower urinary tract dysfunction. Br J Pharmacol. 2006 Feb;147 Suppl 2:S132-43. | ||||
Ref 528976 | J 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 531000 | AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist. Br J Pharmacol. 2010 Jul;160(6):1387-98. | ||||
Ref 533055 | P2X3 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 534640 | Trinitrophenyl-substituted nucleotides are potent antagonists selective for P2X1, P2X3, and heteromeric P2X2/3 receptors. Mol Pharmacol. 1998 Jun;53(6):969-73. |
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