Recent progress in the discovery of antagonists acting at P2X₇ receptor

Bibliography

• NORTH RA: Molecular physiology of P2X receptors . Physiol Rev. (2002) 82:1013–1067.
   PubMed Web of Science ®Google Scholar
• DI VIRGILIO F, CHIOZZI P, FERRARI D et al.: Nucleotide receptors: an emerging family of regulatory molecules in blood cells. Blood (2001) 97:587–600.
   PubMed Web of Science ®Google Scholar
• MIRAS-PORTUGAL MT, DIAZ -HERNANDEZ M, GIRALDEZ L et al.: P2X7 receptors in rat brain: presence in synaptic terminals and granule cells. Neurochem. Res. (2003) 28:1597–1605.
   PubMed Web of Science ®Google Scholar
• NIKOLIC P, HOUSLEY GD, THORNE PR: Expression of the rat P2X7 receptor subunit of the adenosine 5'-triphosphate-gated ion channel in the developing and adult rat cochlea. Audiol Neurootol (2003) 8:28–37.
   PubMed Web of Science ®Google Scholar
• LEE HY, BARDINI M, BURNSTOCK G: P2X receptor immunoreactivity in the male genital organs of the rat. Cell Tissue Res. (2000) 300:321–330.
   Google Scholar
• BUELL GN, TALABOT F, GOS A et al.: Gene structure and chromosomal localization of the human P2X7 receptor. Reap-. Channels (1998) 5:347–354.
   PubMed Web of Science ®Google Scholar
• GU BJ, ZHANG WY: WORTHINGTON RA et al.: A Glu-496 to Ala polymorphism leads to loss of function of the human P2X7 receptor. J. Biol Chem. (2001) 276:11135–11142.
   Google Scholar
• WILEY JS, DAO-UNG LP, GU BJ et al.: A loss-of-function polymorphic mutation in the cytolytic P2X7 receptor gene and chronic lymphocytic leukemia: a molecular study. Lancet (2002) 359:1114–1119.
   PubMed Web of Science ®Google Scholar
• THUNBERG U, TOBIN G, JOHNSON A et al. Polymorphism in the P2X7 receptor gene and survival in chronic lymphocytic leukaemia. Lancet (2002) 360: 1935-1939.
   Google Scholar
• DI VIRGILIO F, WILEY JS: The P2X7 receptor of CLL lymphocytes - a molecule with a split personality. Lancet (2002) 360: 1898-1899.
   Google Scholar
• ZHANG LY, IBBOTSON RE, ORCHARD JA et al.: P2X7 polymorphism and chronic lymphocytic leukaemia: lack of correlation with incidence, survival and abnormalities of chromosome 12. Leukemia (2003) 17:2097–2100.
   PubMed Web of Science ®Google Scholar
• SURPRENANT A, RASSENDREN F, KAWSHIMA E, NORTH RA, BUELL G: The cytolytic P2Z receptor for extracellular ATP identified as a P2X receptor (P2X7). Science (1996) 272:735–738.
   PubMed Web of Science ®Google Scholar
• SMART ML, PANCHAL RG, WILEY J, CROMER B, WILLIAMS DA, PETROU S: P2X7 receptor cell surface expression and cytolytic pore formation are regulated by a distal C-terminal region. J. Biol. Chem. (2003) 278:8853–8860.
   PubMed Web of Science ®Google Scholar
• DENLINGER LC, FISETTE PL, SOMMER JA et al.: The nucleotide receptor P2X7 contains multiple protein and lipid-interaction motifs including a potential binding site for bacterial lipopolysaccharide. j Immunol (2001) 167: 1871-1876.
   Google Scholar
• TORRES GE, EGAN TM, VOIGT MM: Hetero-oligomeric assembly of P2X receptor subunits. J. Biol Chem. (1999) 274:6653–6659.
   PubMed Web of Science ®Google Scholar
• KIM M, SPELTA V, SIM JA, NORTH RA, SURPRENANT A: Differential assembly of rat purinergic P2X7 receptor in immune cells of the brain and the periphery. J. Biol. Chem. (2001) 276:23262–23267.
   PubMed Web of Science ®Google Scholar
• SMART ML, PANCHAL RG, BOWSER DN, WILLIAMS DA, PETROU S: Pore formation is not associated with macroscopic redistribution of P2X7 receptors. Am. J. Physiol Cell Physiol (2002) 283:C77–C84.
   Web of Science ®Google Scholar
• FALZONI S, MUNERATI M, FERRARI D, SPISANI S, MORETTI S, DI VIRGILIO F: The purinergic P2Z receptor of human macrophage cells. Characterization and possible physiological role. J. Clin. Invest. (1995) 95:1207–1216.
   PubMed Web of Science ®Google Scholar
• STEINBERG TH, NEWMAN AS, SWANSON JA, SILVERSTEIN SC: ATP4-permeabilizes the plasma membrane of mouse macrophages to fluorescent dyes. J. Biol. Chem. (1987) 262:8884–8888.
   PubMed Web of Science ®Google Scholar
• FILIPPINI A, TAFFS RE, AGUI T, SITKOVSKY MV: Ecto-ATPase activity in cytolytic T lymphocytes. Protection from the cytolytic effects of extracellular ATP. J. Biol. Chem. (1990) 265:334–340.
   Google Scholar
• GROESCHEL-STEWART U, BARDINI M, ROBSON T, BURNSTOCK G. Localisation of P2X5 and P2X7 receptors by immunohistochemistry in rat stratified squamous epithelia. Cell Tissue Res. (1999) 296:599–605.
   Google Scholar
• RAMIREZ AN, KUNZE DL: P 2X purinergic receptor channel expression and function in bovine aortic endothelium. Am. J. Physiol Heart Circ. Physiol (2002) 282:H2106–2116.
   Web of Science ®Google Scholar
• PERREGAUX D, GABEL C: Interleukin-ly maturation and release in response to ATP and nigericin. Evidence that potassium depletion mediated by these agents is a necessary and common feature of their activity .j Biol Chem. (1994) 269:15195–15203.
   Google Scholar
• SANZ JM, DI VIRGILIO F: Kinetics and mechanism ofATP-dependent IL-10 release from microglial cells. J. Immunol (2000) 164:4893–4898.
   PubMed Web of Science ®Google Scholar
• SUZUKI T, HIDE I, IDO K, KOHSAKA S, INOUE K, NAKATA Y: Production and release of neuroprotective tumor necrosis factor by P2X7 receptor-activated microglia. J. Neurosci. (2004) 24:1–7.
   PubMed Web of Science ®Google Scholar
• FERRARI D, WESSELBORG S, BAUER MK, SCHULZE-OSTHOFF K: Extracellular ATP activates transcription factor NF-6B through the P2Z purinoceptor by selectively targeting NF-6B p65. J. Cell Biol. (1997) 139:1635–1643.
   PubMed Web of Science ®Google Scholar
• FERRARI D, STROH C, SCHULZE -OSTHOFF K: P2X7/P2Z purinoreceptor-mediated activation of transcription factor NFAT in microglial cells. J. Biol. Chem. (1999) 274:13205–13210.
   PubMed Web of Science ®Google Scholar
• BRADFORD MD, SOLTOFF SP: P2X7 receptors activate protein kinase D and p42/ p44 mitogen-activated protein kinase (MAPK) downstream of protein kinase C. Biochem. J. (2002) 366:745–755.
   PubMed Web of Science ®Google Scholar
• HUMPHREY BD, RICE J, KERTESY SB, DUBYAK GR: Stress-activated protein kinase/JNK activation and apoptotic induction by the macrophage P2X7 nucleotide receptor. J. Biol Chem. (2000) 275:26792–16798.
   PubMed Web of Science ®Google Scholar
• DI VIRGILIO F, BRONTE COLLAVO D, ZANOVELLO P: Responses of mouse lymphocytes to extracellular adenosine 5'-triphosphate (ATP). J. Immunol (1989) 143:1955–1960.
   PubMed Web of Science ®Google Scholar
• FERRARI D, LOS M, BAUER MK, VANDENABEELE P, WESSELBORG S, SCHULZE-OSTHOFF K: P 2Z purinoreceptor ligation induces activation of caspases with distinct roles in apoptotic and necrotic alterations of cell death. FEBS Lett (1999) 447:71–75.
   PubMed Web of Science ®Google Scholar
• BARICORDI OR, MELCHIORRI L, ADINOLFI E et al.: Increased proliferation rate of lymphoid cells transfected with the P2X7 ATP receptor. J. Biol. Chem. (1999) 274:33206–33208.
   PubMed Web of Science ®Google Scholar
• SLATER M, DANIELETTO S, POOLEY M, TEH L C, GIDLEY -BAIRD A. BARDEN JA: Differentiation between cancerous and normal hyperplastic lobules in breast lesions. Breast Cancer Res Treat. (2004) 83:1–10.
   PubMed Web of Science ®Google Scholar
• SLATER M, ANIELETTO S, GILEY -BAIRD A, TEH LC, BARDEN JA: Early prostate cancer detected using expression of non-functional cytolytic P2X7 receptors. Histopatho/ogy (2004) 4:206–215.
   Google Scholar
• MURGIA M, HANAU S, PIZZO P, RIPPA M, DI VIRGILIO F: Oxidised ATP. An irreversible inhibitor of the macrophage purinergic P2Z receptor. J. Biol. Chem. (1993) 268 8199–8203.
   Google Scholar
• WILEY JS, CHEN JR, SNOOK MB, JAMIESON GP: The P2Z-purinoceptor of human lymphocytes: actions of nucleotide agonists and irreversible inhibition by oxidized ATP. Br. J. Pharmacol (1994) 112:946–950.
   PubMed Web of Science ®Google Scholar
• LEFF P: WOOD BE, O'CONNOR SE: Suramin is a slowly-equilibrating but competitive antagonist at P2X-receptors in the rabbit isolated ear artery. Br. J. Pharmacol (1990) 101:645–649.
   PubMed Web of Science ®Google Scholar
• WILEY JS, CHEN R, JAMIESON GP: The ATP4- receptor-operated channelm (P2Z class) of human lymphocytes allows Ba2* and ethidium* uptake: inhibition of fluxes by suramin. Arch. Biochem. Biophys. (1993) 305:54–60.
   PubMed Web of Science ®Google Scholar
• VIRGINIO C, CHURCH D, NORTH RA, SURPRENANT A: Effects of divalent cations, protons and calmidazolium at the rat P2X7 receptor. NeuropharmacoL (1997) 36:1285–1294.
   PubMed Web of Science ®Google Scholar
• JIANG LH, MACKENZIE AB, NORTH RA, SURPRENANT A: Brilliant Blue G selectively blocks ATP-gated rat P2X7 receptors. MoL Pharmacol (2000) 58:82–88.
   PubMed Web of Science ®Google Scholar
• GARGETT CE, WILEY JS: The isoquinoline derivative KN-62: a potent antagonist of the P2Z receptor of human lymphocytes. Br. J. Pharmacol (1997) 120:1483–1490.
   PubMed Web of Science ®Google Scholar
• HIDAKA H, KOBAYASHI R: Pharmacology of protein kinase inhibitors. Ann. Rev. Pharmacol Toxicol (1992) 32:377–397.
   PubMed Web of Science ®Google Scholar
• TOKUMITSU H, CHIJIWA T, HAGIWARA M, MIZUTANI A. TERASAWA M, HIDAKA H: KN-62, (1,5-isoquinolinesulfonyfi-N-methyl-L-tyrosy1]-4-phenylpiperazine, a specific inhibitor of Ca2*/calmodulin protein kinase II. J. Biol. Chem. (1990) 8:4315–4320.
   Google Scholar
• ISHIKAWA N, HASHIBA Y, HIDAKA H:Effect of a new Ca2*-calmodulin-dependent protein kinase I inhibitor on GABA release in cerebrospinal fluid of the rat. J . Pharmacol Exp. Ther. (1990) 2:598–602.
   Google Scholar
• BARALDI PG, MAKAEVA R, PAVANI MG et al.: Synthesis, biological activity and molecular modeling studies of 1,2,3,4-tetrahydroisoquinoline derivatives as conformationally constrained analogues of KN-62, a potent antagonist of the P2X7-receptor containing the tyrosine moiety Arzneimittelfirschung (2002) 52:273–285.
   Google Scholar
• BARALDI PG, ROMAGNOLI R, TABRIZI MA, FALZONI S, DI VIRGILIO F: Synthesis of conformationally constrained analogues of KN-62, a potent antagonist of the P2X7-receptor. Bioorg. Med. Chem. Lett. (2000) 10:681–684.
   PubMed Web of Science ®Google Scholar
• RAW RG, KERTESY SB, DUBYAK GR, JACOBSON KA: Potent P2X7 receptor antagonists: tyrosyl derivatives synthesized using a sequential parallel synthetic approach. Drug. Dev. Res. (2001) 54:75–87.
   PubMed Web of Science ®Google Scholar
• CHEN W, RAW RG, KERTESY SB, DUBYAK GR, JACOBSON KA: Functionalized congeners of tyrosine-based P2X7 receptor antagonists: probing multiple sites for linking and dimerization. Bioconj. Chem. (2002) 13:1100–1111.
   PubMed Web of Science ®Google Scholar
• BARALDI PG, NUNEZ MC, MORELLI k FALZONI S, DI VIRGILIO F, ROMAGNOLI R: Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor. J. Med. Chem. (2003) 46:1318–1329.
   PubMed Web of Science ®Google Scholar
• ALCARAZ L, BAXTER A, BENT J et al.: Novel P2X7 receptor antagonists. Bioorg Med. Chem. Lett. (2003) 13:4043–4046.
   PubMed Web of Science ®Google Scholar
• BAXTER A, BENT J, BOWERS K et aL: Hit-to-lead studies: the discovery of potent adamantine amide P2X7 receptor antagonists. Bioorg. Med. Chem. Lett. (2003) 13:4047–4050.
   PubMed Web of Science ®Google Scholar
• GARDLAND A, BUCKLEY KA, BOWLER WB, GALLAGHER JA: Blockade of the pore-forming P2X7 receptor inhibits formation of multinucleated human osteoclasts in vitro. Cala": Tissue Int. (2003) 73:361–369.
   Google Scholar