메뉴 건너뛰기




Volumn 288, Issue 8, 2013, Pages 5840-5848

Small molecule inhibitors of phospholipase C from a novel high-throughput screen

Author keywords

[No Author keywords available]

Indexed keywords

HIGH-THROUGHPUT SCREENS; PHOSPHOLIPASE C; SMALL MOLECULE INHIBITOR; SMALL MOLECULES; THERAPEUTIC TARGETS;

EID: 84874336095     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M112.422501     Document Type: Article
Times cited : (30)

References (53)
  • 1
    • 33144456377 scopus 로고    scopus 로고
    • Regulation of phospholipase c isozymes by ras superfamily gtpases
    • Harden, T. K., and Sondek, J. (2006) Regulation of phospholipase C isozymes by Ras superfamily GTPases. Annu. Rev. Pharmacol. Toxicol. 46, 355-379
    • (2006) Annu. Rev. Pharmacol. Toxicol. , vol.46 , pp. 355-379
    • Harden, T.K.1    Sondek, J.2
  • 3
    • 34248358157 scopus 로고    scopus 로고
    • Plc+ contributes to metastasis of in situ-occurring mammary and prostate tumors
    • Shepard, C. R., Kassis, J., Whaley, D. L., Kim, H. G., and Wells, A. (2007) PLC+ contributes to metastasis of in situ-occurring mammary and prostate tumors. Oncogene 26, 3020-3026
    • (2007) Oncogene , vol.26 , pp. 3020-3026
    • Shepard, C.R.1    Kassis, J.2    Whaley, D.L.3    Kim, H.G.4    Wells, A.5
  • 5
    • 79959572816 scopus 로고    scopus 로고
    • Phospholipase c+ scaffolds to muscle-specific a kinase anchoring protein (makap+) and integrates multiple hypertrophic stimuli in cardiac myocytes
    • Zhang, L., Malik, S., Kelley, G. G., Kapiloff, M. S., and Smrcka, A. V. (2011) Phospholipase C+ scaffolds to muscle-specific A kinase anchoring protein (mAKAP+) and integrates multiple hypertrophic stimuli in cardiac myocytes. J. Biol. Chem. 286, 23012-23021
    • (2011) J. Biol. Chem. , vol.286 , pp. 23012-23021
    • Zhang, L.1    Malik, S.2    Kelley, G.G.3    Kapiloff, M.S.4    Smrcka, A.V.5
  • 6
    • 77956896618 scopus 로고    scopus 로고
    • Potential treatment of cardiac hypertrophy and heart failure by inhibiting the sarcolemmal binding of phospholipase c+1b
    • Woodcock, E. A., Grubb, D. R., and Iliades, P. (2010) Potential treatment of cardiac hypertrophy and heart failure by inhibiting the sarcolemmal binding of phospholipase C+1b. Curr. Drug Targets 11, 1032-1040
    • (2010) Curr. Drug Targets , vol.11 , pp. 1032-1040
    • Woodcock, E.A.1    Grubb, D.R.2    Iliades, P.3
  • 8
    • 0025201019 scopus 로고
    • Selective inhibition of receptorcoupled phospholipase c-dependent processes in human platelets and polymorphonuclear neutrophils
    • Bleasdale, J. E., Thakur, N. R., Gremban, R. S., Bundy, G. L., Fitzpatrick, F. A., Smith, R. J., and Bunting, S. (1990) Selective inhibition of receptorcoupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J. Pharmacol. Exp. Ther. 255, 756-768
    • (1990) J. Pharmacol. Exp. Ther. , vol.255 , pp. 756-768
    • Bleasdale, J.E.1    Thakur, N.R.2    Gremban, R.S.3    Bundy, G.L.4    Fitzpatrick, F.A.5    Smith, R.J.6    Bunting, S.7
  • 9
    • 0025185768 scopus 로고
    • Characterization of the major phosphoinositide-specific phospholipase c of human amnion
    • Bala, G. A., Thakur, N. R., and Bleasdale, J. E. (1990) Characterization of the major phosphoinositide-specific phospholipase C of human amnion. Biol. Reprod. 43, 704-711
    • (1990) Biol. Reprod. , vol.43 , pp. 704-711
    • Bala, G.A.1    Thakur, N.R.2    Bleasdale, J.E.3
  • 10
    • 77954047142 scopus 로고    scopus 로고
    • The pi-plc inhibitor u-73122 is a potent inhibitor of the serca pump in smooth muscle
    • Hollywood, M. A., Sergeant, G. P., Thornbury, K. D., and McHale, N. G. (2010) The PI-PLC inhibitor U-73122 is a potent inhibitor of the SERCA pump in smooth muscle. Br. J. Pharmacol. 160, 1293-1294
    • (2010) Br. J. Pharmacol. , vol.160 , pp. 1293-1294
    • Hollywood, M.A.1    Sergeant, G.P.2    Thornbury, K.D.3    McHale, N.G.4
  • 11
    • 0031770306 scopus 로고    scopus 로고
    • Evidence for separate effects of u73122 on phospholipase c and calcium channels in human platelets
    • Pulcinelli, F. M., Gresele, P., Bonuglia, M., and Gazzaniga, P. P. (1998) Evidence for separate effects of U73122 on phospholipase C and calcium channels in human platelets. Biochem. Pharmacol. 56, 1481-1484
    • (1998) Biochem. Pharmacol. , vol.56 , pp. 1481-1484
    • Pulcinelli, F.M.1    Gresele, P.2    Bonuglia, M.3    Gazzaniga, P.P.4
  • 12
    • 0029028219 scopus 로고
    • Evidence obtained using single hepatocytes for inhibition by the phospholipase c inhibitor u73122 of store-operated ca2+ inflow
    • Berven, L. A., and Barritt, G. J. (1995) Evidence obtained using single hepatocytes for inhibition by the phospholipase C inhibitor U73122 of store-operated Ca2+ inflow. Biochem. Pharmacol. 49, 1373-1379
    • (1995) Biochem. Pharmacol. , vol.49 , pp. 1373-1379
    • Berven, L.A.1    Barritt, G.J.2
  • 13
    • 0029940418 scopus 로고    scopus 로고
    • U-73122, an aminosteroid phospholipase c inhibitor, may also block ca2+ influx through phospholipase c-independent mechanism in neutrophil activation
    • Wang, J. P. (1996) U-73122, an aminosteroid phospholipase C inhibitor, may also block Ca2+ influx through phospholipase C-independent mechanism in neutrophil activation. Naunyn-Schmiedebergs Arch. Pharmacol. 353, 599-605
    • (1996) Naunyn-Schmiedebergs Arch. Pharmacol. , vol.353 , pp. 599-605
    • Wang, J.P.1
  • 14
    • 34250746387 scopus 로고    scopus 로고
    • The phosphoinositide-specific phospholipase c inhibitor u73122 (1-(6-((17 β-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1hpyrrole-2,5-dione) spontaneously forms conjugates with common components of cell culture medium
    • Wilsher, N. E., Court, W. J., Ruddle, R., Newbatt, Y. M., Aherne, W., Sheldrake, P. W., Jones, N. P., Katan, M., Eccles, S. A., and Raynaud, F. I. (2007) The phosphoinositide-specific phospholipase C inhibitor U73122 (1-(6-((17 β-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1Hpyrrole-2,5-dione) spontaneously forms conjugates with common components of cell culture medium. Drug Metab. Dispos. 35, 1017-1022
    • (2007) Drug Metab. Dispos. , vol.35 , pp. 1017-1022
    • Wilsher, N.E.1    Court, W.J.2    Ruddle, R.3    Newbatt, Y.M.4    Aherne, W.5    Sheldrake, P.W.6    Jones, N.P.7    Katan, M.8    Eccles, S.A.9    Raynaud, F.I.10
  • 15
    • 77953749904 scopus 로고    scopus 로고
    • U73122, an aminosteroid phospholipase c inhibitor, is a potent inhibitor of cardiac phospholipasedby a pip2-dependent mechanism
    • Burgdorf, C., Schäfer, U., Richardt, G., and Kurz, T. (2010) U73122, an aminosteroid phospholipase C inhibitor, is a potent inhibitor of cardiac phospholipaseDby a PIP2-dependent mechanism. J. Cardiovasc. Pharmacol. 55, 555-559
    • (2010) J. Cardiovasc. Pharmacol. , vol.55 , pp. 555-559
    • Burgdorf, C.1    Schäfer, U.2    Richardt, G.3    Kurz, T.4
  • 16
    • 17844397683 scopus 로고    scopus 로고
    • The aminosteroid phospholipase c antagonist u-73122 (1-[6-[[17-β-3- methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1h-pyrrole-2,5-dione) potently inhibits human 5-lipoxygenase in vivo and in vitro
    • Feisst, C., Albert, D., Steinhilber, D., and Werz, O. (2005) The aminosteroid phospholipase C antagonist U-73122 (1-[6-[[17-β-3- methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione) potently inhibits human 5-lipoxygenase in vivo and in vitro. Mol. Pharmacol. 67, 1751-1757
    • (2005) Mol. Pharmacol. , vol.67 , pp. 1751-1757
    • Feisst, C.1    Albert, D.2    Steinhilber, D.3    Werz, O.4
  • 17
    • 0027887279 scopus 로고
    • U73122 affects the equilibria between the phosphoinositides as well as phospholipase c activity in unstimulated and thrombin-stimulated human and rabbit platelets
    • Vickers, J. D. (1993) U73122 affects the equilibria between the phosphoinositides as well as phospholipase C activity in unstimulated and thrombin-stimulated human and rabbit platelets. J. Pharmacol. Exp. Ther. 266, 1156-1163
    • (1993) J. Pharmacol. Exp. Ther. , vol.266 , pp. 1156-1163
    • Vickers, J.D.1
  • 19
    • 0035078124 scopus 로고    scopus 로고
    • Synthesis of fluorogenic substrates for continuous assay of phosphatidylinositol-specific phospholipase c
    • Zaikova, T. O., Rukavishnikov, A. V., Birrell, G. B., Griffith, O. H., and Keana, J. F. (2001) Synthesis of fluorogenic substrates for continuous assay of phosphatidylinositol-specific phospholipase C. Bioconjug. Chem. 12, 307-313
    • (2001) Bioconjug. Chem. , vol.12 , pp. 307-313
    • Zaikova, T.O.1    Rukavishnikov, A.V.2    Birrell, G.B.3    Griffith, O.H.4    Keana, J.F.5
  • 20
    • 0344577852 scopus 로고    scopus 로고
    • Fluorescent inhibitors for the qualitative and quantitative analysis of lipolytic enzymes
    • Scholze, H., Stütz, H., Paltauf, F., and Hermetter, A. (1999) Fluorescent inhibitors for the qualitative and quantitative analysis of lipolytic enzymes. Anal. Biochem. 276, 72-80
    • (1999) Anal. Biochem. , vol.276 , pp. 72-80
    • Scholze, H.1    Stütz, H.2    Paltauf, F.3    Hermetter, A.4
  • 21
    • 0026043036 scopus 로고
    • A fluorescent substrate for the assay of phosphatidylinositol-specific phospholipase c: 4-(1-pyreno)butylphosphoryl-1-myo-inositol
    • Hendrickson, E. K., Johnson, J. L., and Hendrickson, H. S. (1991) A fluorescent substrate for the assay of phosphatidylinositol-specific phospholipase C: 4-(1-pyreno)butylphosphoryl-1-myo-inositol. Bioorg. Med. Chem. Lett. 1, 619-662
    • (1991) Bioorg. Med. Chem. Lett. , vol.1 , pp. 619-662
    • Hendrickson, E.1    Johnson, J.2    Hendrickson, H.3
  • 22
    • 0032505195 scopus 로고    scopus 로고
    • Synthesis of a new fluorogenic substrate for the assay of phosphoinositide-specific phospholipase c
    • Rukavishnikov, A. V., Smith, M. P., Birrell, G. B., Keana, J. F., and Griffith, O. H. (1998) Synthesis of a new fluorogenic substrate for the assay of phosphoinositide-specific phospholipase C. Tetrahedron Lett. 39, 6637-6640
    • (1998) Tetrahedron Lett. , vol.39 , pp. 6637-6640
    • Rukavishnikov, A.V.1    Smith, M.P.2    Birrell, G.B.3    Keana, J.F.4    Griffith, O.H.5
  • 23
    • 0026094461 scopus 로고
    • A fluorescent substrate for the continuous assay of phosphatidylinositolspecific phospholipase c: Synthesis and application of 2-naphthyl-myoinositol 1-phosphate
    • Shashidhar, M. S., Volwerk, J. J., Keana, J. F., and Griffith, O. H. (1991) A fluorescent substrate for the continuous assay of phosphatidylinositolspecific phospholipase C: synthesis and application of 2-naphthyl-myoinositol 1-phosphate. Anal. Biochem. 198, 10-14
    • (1991) Anal. Biochem. , vol.198 , pp. 10-14
    • Shashidhar, M.S.1    Volwerk, J.J.2    Keana, J.F.3    Griffith, O.H.4
  • 24
    • 0032579314 scopus 로고    scopus 로고
    • Structural and mechanistic comparison of prokaryotic and eukaryotic phosphoinositidespecific phospholipases c
    • Heinz, D. W., Essen, L. O., and Williams, R. L. (1998) Structural and mechanistic comparison of prokaryotic and eukaryotic phosphoinositidespecific phospholipases C. J. Mol. Biol. 275, 635-650
    • (1998) J. Mol. Biol. , vol.275 , pp. 635-650
    • Heinz, D.W.1    Essen, L.O.2    Williams, R.L.3
  • 25
    • 33745558112 scopus 로고    scopus 로고
    • Synthesis and evaluation of fluorogenic substrates for phospholipase d and phospholipase c
    • Rose, T. M., and Prestwich, G. D. (2006) Synthesis and evaluation of fluorogenic substrates for phospholipase D and phospholipase C. Org. Lett. 8, 2575-2578
    • (2006) Org. Lett. , vol.8 , pp. 2575-2578
    • Rose, T.M.1    Prestwich, G.D.2
  • 26
    • 0033583496 scopus 로고    scopus 로고
    • Synthesis of a new fluorogenic substrate for the continuous assay of mammalian phosphoinositide-specific phospholipase c
    • Rukavishnikov, A. V., Zaikova, T. O., Birrell, G. B., Keana, J. F., and Griffith, O. H. (1999) Synthesis of a new fluorogenic substrate for the continuous assay of mammalian phosphoinositide-specific phospholipase C. Bioorg. Med. Chem. Lett. 9, 1133-1136
    • (1999) Bioorg. Med. Chem. Lett. , vol.9 , pp. 1133-1136
    • Rukavishnikov, A.V.1    Zaikova, T.O.2    Birrell, G.B.3    Keana, J.F.4    Griffith, O.H.5
  • 27
    • 0027389760 scopus 로고
    • Hydrolysis of short acyl chain inositol lipids by phospholipase c+1
    • Rebecchi, M. J., Eberhardt, R., Delaney, T., Ali, S., and Bittman, R. (1993) Hydrolysis of short acyl chain inositol lipids by phospholipase C+1. J. Biol. Chem. 268, 1735-1741
    • (1993) J. Biol. Chem. , vol.268 , pp. 1735-1741
    • Rebecchi, M.J.1    Eberhardt, R.2    Delaney, T.3    Ali, S.4    Bittman, R.5
  • 28
    • 34548133100 scopus 로고    scopus 로고
    • Phosphorothiolate analogues of phosphatidylinositols as assay substrates for phospholipase c
    • Liu, Y., Mihai, C., Kubiak, R. J., Rebecchi, M., and Bruzik, K. S. (2007) Phosphorothiolate analogues of phosphatidylinositols as assay substrates for phospholipase C. ChemBioChem 8, 1430-1439
    • (2007) ChemBioChem , vol.8 , pp. 1430-1439
    • Liu, Y.1    Mihai, C.2    Kubiak, R.J.3    Rebecchi, M.4    Bruzik, K.S.5
  • 29
    • 79955578040 scopus 로고    scopus 로고
    • A fluorogenic, small molecule reporter for mammalian phospholipase c isozymes
    • Huang, W., Hicks, S. N., Sondek, J., and Zhang, Q. (2011) A fluorogenic, small molecule reporter for mammalian phospholipase C isozymes. ACS Chem. Biol. 6, 223-228
    • (2011) ACS Chem. Biol. , vol.6 , pp. 223-228
    • Huang, W.1    Hicks, S.N.2    Sondek, J.3    Zhang, Q.4
  • 31
    • 0020049863 scopus 로고
    • Differential modification of the interaction of cardiac muscarinic cholinergic and betaadrenergic receptors with a guanine nucleotide binding component(s)
    • Harden, T. K., Scheer, A. G., and Smith, M. M. (1982) Differential modification of the interaction of cardiac muscarinic cholinergic and betaadrenergic receptors with a guanine nucleotide binding component(s). Mol. Pharmacol. 21, 570-580
    • (1982) Mol. Pharmacol. , vol.21 , pp. 570-580
    • Harden, T.K.1    Scheer, A.G.2    Smith, M.M.3
  • 32
    • 0016374975 scopus 로고
    • A highly sensitive adenylate cyclase assay
    • Salomon, Y., Londos, C., and Rodbell, M. (1974) A highly sensitive adenylate cyclase assay. Anal. Biochem. 58, 541-548
    • (1974) Anal. Biochem. , vol.58 , pp. 541-548
    • Salomon, Y.1    Londos, C.2    Rodbell, M.3
  • 33
    • 33751321865 scopus 로고    scopus 로고
    • A detergent-based assay for the detection of promiscuous inhibitors
    • Feng, B. Y., and Shoichet, B. K. (2006) A detergent-based assay for the detection of promiscuous inhibitors. Nat. Protoc. 1, 550-553
    • (2006) Nat. Protoc. , vol.1 , pp. 550-553
    • Feng, B.Y.1    Shoichet, B.K.2
  • 38
    • 32144459473 scopus 로고    scopus 로고
    • Quantification of isozyme-specific activation of phospholipasec+2 by rac gtpases and phospholipase c+ by rho gtpases in an intact cell assay system
    • Bourdon, D. M., Wing, M. R., Edwards, E. B., Sondek, J., and Harden, T. K. (2006) Quantification of isozyme-specific activation of phospholipaseC+2 by Rac GTPases and phospholipase C+ by Rho GTPases in an intact cell assay system. Methods Enzymol. 406, 489-499
    • (2006) Methods Enzymol. , vol.406 , pp. 489-499
    • Bourdon, D.M.1    Wing, M.R.2    Edwards, E.B.3    Sondek, J.4    Harden, T.K.5
  • 40
    • 0029917899 scopus 로고    scopus 로고
    • Aurin tricarboxylic acid inhibits adhesion of platelets to subendothelium
    • Owens, M. R., and Holme, S. (1996) Aurin tricarboxylic acid inhibits adhesion of platelets to subendothelium. Thrombosis Res. 81, 177-185
    • (1996) Thrombosis Res. , vol.81 , pp. 177-185
    • Owens, M.R.1    Holme, S.2
  • 41
    • 63849273722 scopus 로고    scopus 로고
    • Discovery of selective glucocorticoid receptor modulators by multiplexed reporter screening
    • Gerber, A. N., Masuno, K., and Diamond, M. I. (2009) Discovery of selective glucocorticoid receptor modulators by multiplexed reporter screening. Proc. Natl. Acad. Sci. U.S.A. 106, 4929-4934
    • (2009) Proc. Natl. Acad. Sci. U.S.A. , vol.106 , pp. 4929-4934
    • Gerber, A.N.1    Masuno, K.2    Diamond, M.I.3
  • 42
    • 0033967235 scopus 로고    scopus 로고
    • Aurintricarboxylic acid promotes survival and regeneration of axotomised retinal ganglion cells in vivo
    • Heiduschka, P., and Thanos, S. (2000) Aurintricarboxylic acid promotes survival and regeneration of axotomised retinal ganglion cells in vivo. Neuropharmacology 39, 889-902
    • (2000) Neuropharmacology , vol.39 , pp. 889-902
    • Heiduschka, P.1    Thanos, S.2
  • 43
    • 0028896030 scopus 로고
    • Aurintricarboxylic acid, a putative inhibitor of apoptosis, is a potent inhibitor of dna topoisomerase ii in vitro and in chinese hamster fibrosarcoma cells
    • Benchokroun, Y., Couprie, J., and Larsen, A. K. (1995) Aurintricarboxylic acid, a putative inhibitor of apoptosis, is a potent inhibitor of DNA topoisomerase II in vitro and in Chinese hamster fibrosarcoma cells. Biochemical Pharmacol. 49, 305-313
    • (1995) Biochemical Pharmacol. , vol.49 , pp. 305-313
    • Benchokroun, Y.1    Couprie, J.2    Larsen, A.K.3
  • 48
    • 69449092270 scopus 로고    scopus 로고
    • Phospholipase c+ promotes intestinal tumorigenesis of apcmin/+ mice through augmentation of inflammation and angiogenesis
    • Li, M., Edamatsu, H., Kitazawa, R., Kitazawa, S., and Kataoka, T. (2009) Phospholipase C+ promotes intestinal tumorigenesis of ApcMin/+ mice through augmentation of inflammation and angiogenesis. Carcinogenesis 30, 1424-1432
    • (2009) Carcinogenesis , vol.30 , pp. 1424-1432
    • Li, M.1    Edamatsu, H.2    Kitazawa, R.3    Kitazawa, S.4    Kataoka, T.5
  • 49
    • 0032803235 scopus 로고    scopus 로고
    • A role for phospholipase c β-mediated signaling in tumor cell invasion. Clin
    • Kassis, J., Moellinger, J., Lo, H., Greenberg, N. M., Kim, H. G., and Wells, A. (1999) A role for phospholipase C β-mediated signaling in tumor cell invasion. Clin. Cancer Res. 5, 2251-2260
    • (1999) Cancer Res. , vol.5 , pp. 2251-2260
    • Kassis, J.1    Moellinger, J.2    Lo, H.3    Greenberg, N.M.4    Kim, H.G.5    Wells, A.6
  • 51
    • 10844263476 scopus 로고    scopus 로고
    • Crucial role of phospholipase c+ in chemical carcinogen-induced skin tumor development
    • Bai, Y., Edamatsu, H., Maeda, S., Saito, H., Suzuki, N., Satoh, T., and Kataoka, T. (2004) Crucial role of phospholipase C+ in chemical carcinogen-induced skin tumor development. Cancer Res. 64, 8808-8810
    • (2004) Cancer Res. , vol.64 , pp. 8808-8810
    • Bai, Y.1    Edamatsu, H.2    Maeda, S.3    Saito, H.4    Suzuki, N.5    Satoh, T.6    Kataoka, T.7
  • 52
    • 38149076535 scopus 로고    scopus 로고
    • Phospholipase c+3 deficiency leads to macrophage hypersensitivity to apoptotic induction and reduction of atherosclerosis in mice
    • Wang, Z., Liu, B., Wang, P., Dong, X., Fernandez-Hernando, C., Li, Z., Hla, T., Li, Z., Claffey, K., Smith, J. D., and Wu, D. (2008) Phospholipase C+3 deficiency leads to macrophage hypersensitivity to apoptotic induction and reduction of atherosclerosis in mice. J. Clin. Invest. 118, 195-204
    • (2008) J. Clin. Invest. , vol.118 , pp. 195-204
    • Wang, Z.1    Liu, B.2    Wang, P.3    Dong, X.4    Fernandez-Hernando, C.5    Li, Z.6    Hla, T.7    Li, Z.8    Claffey, K.9    Smith, J.D.10    Wu, D.11
  • 53
    • 50249118640 scopus 로고    scopus 로고
    • Plc+1 knockout mice as a model of disrupted cortical development and plasticity: Behavioral endophenotypes and dysregulation of rgs4 gene expression
    • McOmish, C. E., Burrows, E. L., Howard, M., and Hannan, A. J. (2008) PLC+1 knockout mice as a model of disrupted cortical development and plasticity: behavioral endophenotypes and dysregulation of RGS4 gene expression. Hippocampus 18, 824-834
    • (2008) Hippocampus , vol.18 , pp. 824-834
    • McOmish, C.E.1    Burrows, E.L.2    Howard, M.3    Hannan, A.J.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.