Target Information
Target General Infomation | |||||
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Target ID |
T63414
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Former ID |
TTDC00218
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Target Name |
P2X purinoceptor 7
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Gene Name |
P2RX7
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Synonyms |
ATP receptor; Adenosine P2X7 receptor; P2X7; P2Z receptor; Purinergic receptor; P2RX7
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Target Type |
Clinical Trial
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Disease | Arthralgia [ICD10: M25.5] | ||||
Autoimmune diabetes [ICD10: E08-E13] | |||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
Function |
Receptor for atp that acts as a ligand gatedion channel. Responsible for atp-dependent lysis of macrophages through the formation of membrane pores permeable to large molecules. Could function in both fast synaptic transmission.
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BioChemical Class |
ATP-gated P2X receptor cation channel
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Target Validation |
T63414
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UniProt ID | |||||
Sequence |
MPACCSCSDVFQYETNKVTRIQSMNYGTIKWFFHVIIFSYVCFALVSDKLYQRKEPVISS
VHTKVKGIAEVKEEIVENGVKKLVHSVFDTADYTFPLQGNSFFVMTNFLKTEGQEQRLCP EYPTRRTLCSSDRGCKKGWMDPQSKGIQTGRCVVYEGNQKTCEVSAWCPIEAVEEAPRPA LLNSAENFTVLIKNNIDFPGHNYTTRNILPGLNITCTFHKTQNPQCPIFRLGDIFRETGD NFSDVAIQGGIMGIEIYWDCNLDRWFHHCRPKYSFRRLDDKTTNVSLYPGYNFRYAKYYK ENNVEKRTLIKVFGIRFDILVFGTGGKFDIIQLVVYIGSTLSYFGLAAVFIDFLIDTYSS NCCRSHIYPWCKCCQPCVVNEYYYRKKCESIVEPKPTLKYVSFVDESHIRMVNQQLLGRS LQDVKGQEVPRPAMDFTDLSRLPLALHDTPPIPGQPEEIQLLRKEATPRSRDSPVWCQCG SCLPSQLPESHRCLEELCCRKKPGACITTSELFRKLVLSRHVLQFLLLYQEPLLALDVDS TNSRLRHCAYRCYATWRFGSQDMADFAILPSCCRWRIRKEFPKSEGQYSGFKSPY |
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Drugs and Mode of Action | |||||
Drug(s) | CE-224535 | Drug Info | Phase 2/3 | Arthralgia | [522242] |
AZD9056 | Drug Info | Phase 2 | Chronic obstructive pulmonary disease | [522096], [542771] | |
EVT 401 | Drug Info | Phase 1 | Rheumatoid arthritis | [551888] | |
GSK1482160 | Drug Info | Phase 1 | Pain | [548875] | |
JNJ-479655 | Drug Info | Clinical trial | Alzheimer disease | [532081] | |
Inhibitor | A-740003 | Drug Info | [530221] | ||
ISOPPADS | Drug Info | [528976] | |||
KN-62 | Drug Info | [530421] | |||
STYLISSADINE A | Drug Info | [530221] | |||
STYLISSADINE B | Drug Info | [530221] | |||
[3H]A-804598 | Drug Info | [530221] | |||
Antagonist | A438079 | Drug Info | [528808] | ||
A804598 | Drug Info | [543850] | |||
A839977 | Drug Info | [530161] | |||
AFC-5128 | Drug Info | [543850] | |||
AZ-11657312 | Drug Info | [543850] | |||
AZ11657312 (salt free) | Drug Info | [543850] | |||
AZD9056 | Drug Info | [550288] | |||
brilliant blue G | Drug Info | [525800] | |||
CE-224535 | Drug Info | [531823] | |||
decavanadate | Drug Info | [528045] | |||
EVT 401 | Drug Info | [544235] | |||
GSK1482160 | Drug Info | [550963] | |||
JNJ-479655 | Drug Info | [532440] | |||
P2X7 antagonists | Drug Info | [543850] | |||
Modulator (allosteric modulator) | AZ11645373 | Drug Info | [530033] | ||
chelerythrine | Drug Info | [527114] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 522096 | ClinicalTrials.gov (NCT00520572) A 6-month Randomised, Double-blind, Open Arm Comparator, Phase IIb, With AZD9056, in Patients With Rheumatoid Arthritis (RA). U.S. National Institutes of Health. | ||||
Ref 522242 | ClinicalTrials.gov (NCT00628095) Study of CE-224,535 A Twice Daily Pill To Control Rheumatoid Arthritis In Patients Who Have Not Totally Improved With Methotrexate. U.S. National Institutes of Health. | ||||
Ref 532081 | The role of the innate immune system in psychiatric disorders. Mol Cell Neurosci. 2013 Mar;53:52-62. | ||||
Ref 542771 | (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. (Ligand id: 7826). | ||||
Ref 525800 | Brilliant blue G selectively blocks ATP-gated rat P2X(7) receptors. Mol Pharmacol. 2000 Jul;58(1):82-8. | ||||
Ref 527114 | Chelerythrine and other benzophenanthridine alkaloids block the human P2X7 receptor. Br J Pharmacol. 2004 Jul;142(6):1015-9. Epub 2004 Jun 21. | ||||
Ref 528045 | Decavanadate, a P2X receptor antagonist, and its use to study ligand interactions with P2X7 receptors. Eur J Pharmacol. 2006 Mar 18;534(1-3):19-29. Epub 2006 Feb 17. | ||||
Ref 528808 | Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. Br J Pharmacol. 2007 Jul;151(5):571-9. Epub 2007 Apr 30. | ||||
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 530033 | Mechanism of action of species-selective P2X(7) receptor antagonists. Br J Pharmacol. 2009 Apr;156(8):1312-25. | ||||
Ref 530161 | The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice. Behav Brain Res. 2009 Dec 1;204(1):77-81. | ||||
Ref 530221 | Bioorg Med Chem. 2009 Jul 15;17(14):4861-5. Epub 2009 Jun 12.Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening. | ||||
Ref 530421 | Bioorg Med Chem Lett. 2009 Nov 1;19(21):6053-8. Epub 2009 Sep 17.Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists. | ||||
Ref 531823 | Efficacy and safety of CE-224,535, an antagonist of P2X7 receptor, in treatment of patients with rheumatoid arthritis inadequately controlled by methotrexate. J Rheumatol. 2012 Apr;39(4):720-7. | ||||
Ref 532440 | Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br J Pharmacol. 2013 Oct;170(3):624-40. | ||||
Ref 543850 | (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: 484). |
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