Inhibition of the human P2X7 receptor by a novel protein tyrosine kinase antagonist

Biochemical and Biophysical Research Communications

Volumn 365, Issue 3, 2008, Pages 515-520

  Shemon, Anne N ^a   Sluyter, Ronald ^a   Stokes, Leanne ^a   Manley, Paul W ^b   Wiley, James S ^a  

^a UNIVERSITY OF SYDNEY   (Australia)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

ATP; Canine; Erythrocyte; Human; Lymphocyte; P2X7 receptor; P2Z receptor; Protein tyrosine kinase

Indexed keywords

5ALPHA PREGNAN 20 ONE 3BETA,17ALPHA,21 TRIOL; AAD 777; AAL 993; ADENOSINE TRIPHOSPHATE; CGP 76030; ETHIDIUM; IMATINIB; MIDOSTAURIN; N [4 (1 METHYLETHYL)PHENYL] 4 [2 (3 PYRIDINYL)ETHYL] 1 PHTHALAZINAMINE; PROTEIN TYROSINE KINASE INHIBITOR; PURINE P2X7 RECEPTOR; UNCLASSIFIED DRUG; VASCULOTROPIN RECEPTOR; ANILINE DERIVATIVE; N (4 (1 METHYLETHYL)PHENYL) 4 (2 (3 PYRIDINYL)ETHYL) 1 PHTHALAZINAMINE; N-(4-(1-METHYLETHYL)PHENYL)-4-(2-(3-PYRIDINYL)ETHYL)-1-PHTHALAZINAMINE; PHTHALAZINE DERIVATIVE; POTASSIUM; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; PURINERGIC P2 RECEPTOR; PURINERGIC P2X7 RECEPTOR; RUBIDIUM;

ANIMAL CELL; ARTICLE; B LYMPHOCYTE; CELL STRAIN HEK293; CELL TYPE; CONTROLLED STUDY; DOG; DOSE RESPONSE; EMBRYO; ERYTHROCYTE; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; IC 50; KINETICS; MEMBRANE CURRENT; NONHUMAN; POTASSIUM TRANSPORT; PRIORITY JOURNAL; ANIMAL; CELL LINE; CHEMISTRY; DRUG ANTAGONISM; DRUG EFFECT; METABOLISM;

ADENOSINE TRIPHOSPHATE; ANILINE COMPOUNDS; ANIMALS; B-LYMPHOCYTES; CELL LINE; DOGS; ERYTHROCYTES; ETHIDIUM; HUMANS; INHIBITORY CONCENTRATION 50; PHTHALAZINES; POTASSIUM; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; RECEPTORS, PURINERGIC P2; RUBIDIUM RADIOISOTOPES;

EID: 36549066553     PISSN: 0006291X     EISSN: 10902104     Source Type: Journal    
DOI: 10.1016/j.bbrc.2007.11.008     Document Type: Article

References (25)

1. North R.A. Molecular physiology of P2X receptors. Physiol. Rev. 82 (2002) 1013-1067
2. 7 receptor. EMBO J. 25 (2006) 5071-5082
3. 7). Science 272 (1996) 735-738
4. Coutinho-Silva R., da Cruz C.M., Persechini P.M., and Ojcius D.M. The role of P2 receptors in controlling infections by intracellular pathogens. Purinergic Signal. 3 (2007) 83-90
5. 7 in pain and inflammation. Purinergic Signal. 3 (2007) 163-169
6. Barden N., Harvey M., Gagne B., Shink E., Tremblay M., Raymond C., Labbe M., Villeneuve A., Rochette D., Bordeleau L., Stadler H., Holsboer F., and Muller-Myhsok B. Analysis of single nucleotide polymorphisms in genes in the chromosome 12Q24.31 region points to P2RX7 as a susceptibility gene to bipolar affective disorder. Am. J. Med. Genet. B, Neuropsychiatr. Genet. 141 (2006) 374-382
7. Chessell I.P., Hatcher J.P., Bountra C., Michel A.D., Hughes J.P., Green P., Egerton J., Murfin M., Richardson J., Peck W.L., Grahames C.B., Casula M.A., Yiangou Y., Birch R., Anand P., and Buell G.N. Disruption of the P2X7 purinoceptor gene abolishes chronic inflammatory and neuropathic pain. Pain 114 (2005) 386-396
8. Fernando S.L., Saunders B.M., Sluyter R., Skarratt K.K., Goldberg H., Marks G.B., Wiley J.S., and Britton W.J. A polymorphism in the P2X7 gene increases susceptibility to extrapulmonary tuberculosis. Am. J. Respir. Crit. Care Med. 175 (2007) 360-366
9. 7 nucleotide receptor reveals its regulatory roles in bone formation and resorption. Mol. Endocrinol. 17 (2003) 1356-1367
10. Labasi J.M., Petrushova N., Donovan C., McCurdy S., Lira P., Payette M.M., Brissette W., Wicks J.R., Audoly L., and Gabel C.A. Absence of the P2X7 receptor alters leukcoyte function and attenuates an inflammatory response. J. Immunol. 168 (2002) 6436-6445
11. Ohlendorff S.D., Tofteng C.L., Jensen J.E., Petersen S., Civitelli R., Fenger M., Abrahamsen B., Hermann A.P., Eiken P., and Jorgensen N.R. Single nucleotide polymorphisms in the P2X7 gene are associated to fracture risk and to effect of estrogen treatment. Pharmacogenet. Genomics 17 (2007) 555-567
12. Donnelly-Roberts D.L., and Jarvis M.F. Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. Br. J. Pharmacol. 151 (2007) 571-579
13. Gunosewoyo H., Coster M.J., and Kassiou M. Molecular probes for P2X7 receptor studies. Curr. Med. Chem. 14 (2007) 1505-1523
14. 7 receptor signalling complex. EMBO J. 20 (2001) 6347-6358
15. 7 function and impairs ATP-induced mycobacterial killing by macrophages. J. Biol. Chem. 281 (2006) 2079-2086
16. 7 receptor: greatly increased function compared with human erythrocytes. Am. J. Physiol. Regul. Integr. Comp. Physiol. 293 (2007) R2090-R2098
17. 7 receptor. Br. J. Pharm. 142 (2004) 1015-1019
18. 7 receptor. J. Biol. Chem. 279 (2004) 44749-44755
19. 7 receptor activation causes phosphatidylserine exposure in human erythrocytes. Biochem. Biophys. Res. Commun. 355 (2007) 169-173
20. 7 antagonists. J. Med. Chem. 49 (2006) 3659-3666
21. Honore P., Donnelly-Roberts D., Namovic M.T., Hsieh G., Zhu C.Z., Mikusa J.P., Hernandez G., Zhong C., Gauvin D.M., Chandran P., Harris R., Medrano A.P., Carroll W., Marsh K., Sullivan J.P., Faltynek C.R., and Jarvis M.F. A-740003 [N-(1-{[(Cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J. Pharmacol. Exp. Ther. 319 (2006) 1376-1385
22. Stokes L., Jiang L.H., Alcaraz L., Bent J., Bowers K., Fagura M., Furber M., Mortimore M., Lawson M., Theaker J., Laurent C., Braddock M., and Surprenant A. Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373. Br. J. Pharmacol. 149 (2006) 880-887
23. Gargett C.E., and Wiley J.S. The isoquinoline derivative KN-62 a potent antagonist of the P2Z-receptor of human lymphocytes. Br. J. Pharmacol. 120 (1997) 1483-1490
24. 7 nucleotide receptor: high selectivity for the human versus rat receptor homolgues. Mol. Pharmacol. 54 (1998) 22-32
25. 7 receptor stimulated phospholipase D activity in chronic lymphocytic leukaemia B-lymphocytes. Immunol. Cell Biol. 85 (2007) 68-72