Target Information

Target General Infomation
Target ID
T63414
Former ID
TTDC00218
Target Name
P2X purinoceptor 7
Gene Name
P2RX7
Synonyms
ATP receptor; Adenosine P2X7 receptor; P2X7; P2Z receptor; Purinergic receptor; P2RX7
Target Type
Clinical Trial
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.
BioChemical Class
ATP-gated P2X receptor cation channel
Target Validation
T63414
UniProt ID
Q99572
Sequence
MPACCSCSDVFQYETNKVTRIQSMNYGTIKWFFHVIIFSYVCFALVSDKLYQRKEPVISS
VHTKVKGIAEVKEEIVENGVKKLVHSVFDTADYTFPLQGNSFFVMTNFLKTEGQEQRLCP
EYPTRRTLCSSDRGCKKGWMDPQSKGIQTGRCVVYEGNQKTCEVSAWCPIEAVEEAPRPA
LLNSAENFTVLIKNNIDFPGHNYTTRNILPGLNITCTFHKTQNPQCPIFRLGDIFRETGD
NFSDVAIQGGIMGIEIYWDCNLDRWFHHCRPKYSFRRLDDKTTNVSLYPGYNFRYAKYYK
ENNVEKRTLIKVFGIRFDILVFGTGGKFDIIQLVVYIGSTLSYFGLAAVFIDFLIDTYSS
NCCRSHIYPWCKCCQPCVVNEYYYRKKCESIVEPKPTLKYVSFVDESHIRMVNQQLLGRS
LQDVKGQEVPRPAMDFTDLSRLPLALHDTPPIPGQPEEIQLLRKEATPRSRDSPVWCQCG
SCLPSQLPESHRCLEELCCRKKPGACITTSELFRKLVLSRHVLQFLLLYQEPLLALDVDS
TNSRLRHCAYRCYATWRFGSQDMADFAILPSCCRWRIRKEFPKSEGQYSGFKSPY
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
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Reactome The NLRP3 inflammasome
WikiPathways Nucleotide-binding domain, leucine rich repeat containing receptor (NLR) signaling pathways
References
Ref 522096ClinicalTrials.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 522242ClinicalTrials.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 532081The 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 548875Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029786)
Ref 551888Clinical pipeline report, company report or official report of Evotec.
Ref 525800Brilliant blue G selectively blocks ATP-gated rat P2X(7) receptors. Mol Pharmacol. 2000 Jul;58(1):82-8.
Ref 527114Chelerythrine and other benzophenanthridine alkaloids block the human P2X7 receptor. Br J Pharmacol. 2004 Jul;142(6):1015-9. Epub 2004 Jun 21.
Ref 528045Decavanadate, 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 528808Discovery 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 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 530033Mechanism of action of species-selective P2X(7) receptor antagonists. Br J Pharmacol. 2009 Apr;156(8):1312-25.
Ref 530161The 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 530221Bioorg 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 530421Bioorg 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 531823Efficacy 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 532440Pharmacological 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).
Ref 544235Molecular and functional properties of P2X receptors??ecent progress and persisting challenges. Purinergic Signal. 2012 September; 8(3): 375-417.
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).

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