Inhibition of protein kinase C - Do we, can we, and should we?

Pharmacology and Therapeutics

Volumn 82, Issue 2-3, 1999, Pages 263-267

  Parker, Peter J ^a  

^a IMPERIAL CANCER RESEARCH FUND   (United Kingdom)

Author keywords

Inhibitor; Kinase; Protein kinase C; Signal transduction

Indexed keywords

12 (2 CYANOETHYL) 6,7,12,13 TETRAHYDRO 13 METHYL 5 OXOINDOLO[2,3 A]PYRROLO[3,4 C]CARBAZOLE; 2 [1 (3 DIMETHYLAMINOPROPYL) 3 INDOLYL] 3 (3 INDOLYL)MALEIMIDE; 2 [1 (3 DIMETHYLAMINOPROPYL) 5 METHOXY 1H INDOL 3 YL] 3 (1H INDOL 3 YL)MALEIMIDE; BALANOL; PROTEIN KINASE C; PROTEIN KINASE C INHIBITOR; RUBOXISTAURIN; UNCLASSIFIED DRUG;

CONFERENCE PAPER; DRUG SELECTIVITY; ENZYME ACTIVE SITE; ENZYME INHIBITION; GENERAL ASPECTS OF DISEASE; NONHUMAN; PRIORITY JOURNAL; PROTEIN FAMILY; SECOND MESSENGER; SIGNAL TRANSDUCTION;

ENZYME INHIBITORS; FORECASTING; MODELS, BIOLOGICAL; PROTEIN KINASE C; SIGNAL TRANSDUCTION;

EID: 0032987224     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0163-7258(98)00047-3     Document Type: Conference Paper

References (37)

1. Abeliovich A., Chen C., Goda Y., Silva A.J., Stevens C.F., Tonegawa S. Modified hippocampal long-term potentiation in PKC gamma-mutant mice. Cell. 75:1993;1253-1262. a.
2. Abeliovich A., Paylor R., Chen C., Kim J.J., Wehner J.M., Tonegawa S. PKC gamma mutant mice exhibit mild deficits in spatial and contextual learning. Cell. 75:1993;1263-1271. b.
3. Akimoto K., Takahashi R., Moriya S., Nishioka N., Takayanagi J., Kimura K., Fukui Y., Osada S., Mizuno K., Hirai S., Kazlauskas A., Ohno S. EGF or PDGF receptors activate atypical PKClambda through phosphatidylinositol 3-kinase. EMBO J. 15:1996;788-798.
4. Areces L.B., Kazanietz G., Blumberg P.M. Close similarity of baculovirus-expressed n-chimaerin and protein kinase Cα as phorbol ester receptors. J. Biol. Chem. 269:1994;19553-19558.
5. Bornancin F., Parker P. Phosphorylation of threonine-638 critically controls the dephosphorylation and inactivation of protein-kinase C-alpha. Curr. Biol. 6:1996;1114-1123.
6. Bornancin F., Parker P.J. Phosphorylation of protein kinase C-α on serine 657 controls the accumulation of active enzyme and contributes to its phosphatase-resistant state. J. Biol. Chem. 272:1997;3544-3549.
7. Cazaubon S., Bornancin F., Parker P.J. Threonine-497 is a critical site for permissive activation of protein kinase Cα Biochem. J. 301:1994;443-448.
8. Conrad R., Keranen L.M., Ellington A.D., Newton A.C. Isozyme-specific inhibition of protein-kinase-C by RNA aptamers. J. Biol. Chem. 269:1994;32051-32054.
9. Dekker L.V., Parker P.J. Protein kinase C - a question of specificity. Trends Biochem. Sci. 19:1994;73-77.
10. Exton J. Signalling through phosphatidylcholine breakdown. J. Biol. Chem. 265:1990;1-4.
11. Faux M.C., Scott J.D. Regulation of the AKAP79-protein kinase C interaction by Ca2+/calmodulin. J. Biol. Chem. 272:1997;17038-17044.
12. Gschwendt M., Dieterich S., Rennecke J., Kittstein W., Mueller H.J., Johannes F.J. Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase C isoenzymes. FEBS Lett. 392:1996;77-80.
13. Hannun Y., Loomis C., Merrill A., Bell R. Sphingosine inhibition of protein kinase C activity and of phorbol dibutyrate binding in vitro and in human-platelets. J. Biol. Chem. 261:1986;12604-12609.
14. Hu H. Recent discovery and development of selective protein kinase C inhibitors. Drug Discov. Today. 1:1996;438-447.
15. Hug H., Sarre T.F. Protein kinase C isoenzymes - divergence in signal transduction. Biochem. J. 291:1993;329-343.
16. Hyatt S.L., Liao L., Chapline C., Jaken S. Identification and characterization of alpha-protein kinase-C binding-proteins in normal and transformed ref52 cells. Biochemistry. 33:1994;1223-1228.
17. Ishii H., Jirousek M.R., Koya D., Tagaki C., Xia P., Clermont A., Bursell S.E., Kern T.S., Ballas L.M., Heath W.F., Stramm L.E., Feener E.P., King G.L. Amelioration of vascular dysfunctions in diabetic rats by an oral PKC beta inhibitor. Science. 272:1996;728-731.
18. Keranen L.M., Dutil E.M., Newton A.C. Protein kinase C is regulated in vivo by three functionally distinct phosphorylations. Curr. Biol. 5:1995;1394-1403.
19. 2+, phospholipid-dependent protein kinase associated with plasma membrane. Nature. 302:1983;621-623.
20. Le Good J.A., Ziegler W.H., Parekh D.B., Alessi D.R., Cohen P., Parker P.J. Protein kinase C isotypes controled by phosphoinositide 3-kinase through the protein kinase PDK1. Science. 281:1998;2042-2045.
21. Leitges M., Schmedt C., Guinamard R., Davoust J., Schaal S., Stabel S., Tarakhovsky A. Immunodeficiency in protein kinase Cbeta-deficient mice. Science. 273:1996;788-791.
22. Martiny-Baron G., Kazanietz M.G., Mischak H., Blumberg P.M., Kochs G., Hug H., Marme D., Schachtele C. Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976. J. Biol. Chem. 268:1993;9194-9197.
23. Mochly-Rosen D., Khaner H., Lopez J. Identification of intracellular receptor proteins for activated protein-kinase-C. Proc. Natl. Acad. Sci. USA. 88:1991;3997-4000.
24. Mori T., Takai Y., Minakuchi R., Yu B., Nishizuka Y. Inhibitory action of chlorpromazine, dibucaine and other phospholipid-interacting drugs on calcium-activated, phospholipid-dependent protein kinase. J. Biol. Chem. 255:1980;8378-8380.
25. Moriya S., Kazlauskas A., Akimoto K., Hirai S., Mizuno K., Takenawa T., Fukui Y., Watanabe Y., Ozaki S., Ohno S. Platelet-derived growth factor activates protein kinase C epsilon through redundant and independent signaling pathways involving phospholipase C gamma or phosphatidylinositol 3-kinase. Proc. Natl. Acad. Sci. USA. 93:1996;151-155.
26. Nishizuka Y. Intracellular signalling by hydrolysis of phospholipids and activation of protein kinase C. Science. 258:1992;607-614.
27. Noh D.Y., Shin S.H., Rhee S.G. Phosphoinositide-specific phospholipase-C and mitogenic signaling. Biochim. Biophys. Acta [Rev. Cancer]. 1242:1995;99-113.
28. Pears C., Stabel S., Cazaubon S., Parker P.J. Studies on the phosphorylation of protein kinase C-α Biochem. J. 283:1992;515-518.
29. s6k inactivation is a novel phosphorylation site within a conserved hydrophobic domain. EMBO J. 14:1995;5279-5287.
30. Schwartz G.K., Haimovitz F.A., Dhupar S.K., Ehleiter D., Maslak P., Lai L., Loganzo F.J., Kelsen D.P., Fuks Z., Albino A.P. Potentiation of apoptosis by treatment with the protein kinase C-specific inhibitor safingol in mitomycin C-treated gastric cancer cells. J. Natl. Cancer Inst. 87:1995;1394-1399.
31. Staudinger J., Lu J., Olson E.N. Specific interaction of the PDZ domain protein PICK1 with the COOH terminus of protein kinase C-alpha. J. Biol. Chem. 272:1997;32019-32024.
32. Stempka L., Girod A., Muller H.J., Rincke G., Marks F., Gschwendt M., Bossemeyer D. Phosphorylation of protein kinase Cdelta (PKCdelta) at threonine 505 is not a prerequisite for enzymatic activity. J. Biol. Chem. 272:1997;6805-6811.
33. Stephens L., Anderson K., Stokoe D., Erdjument-Bromage H., Painter G.F., Holmes A.B., Gaffney P.R., Reese C.B., McCormick F., Tempst P., Coadwell J., Hawkins P.T. Protein kinase B kinases that mediate phosphatidylinositol 3,4,5-trisphosphate-dependent activation of protein kinase B. Science. 279:1998;710-714.
34. Tamaoki T., Nakano H. Potent and specific inhibitors of protein kinase-C of microbial origin. Biotechnology. 8:1990;732-735.
35. Tamaoki T., Nomoto H., Takahashi I., Kato Y., Morimoto M., Tomita F. Staurosporine, a potent inhibitor of phospholipid/Ca++ dependent protein kinase. Biochem. Biophys. Res. Commun. 135:1986;397-402.
36. Tsutakawa S.E., Medzihradszky K.F., Flint A.J., Burlingame A.L., Koshland D.E. Jr. Determination of in vivo phosphorylation sites in protein kinase C. J. Biol. Chem. 270:1995;26807-26812.
37. Yedovitzky M., Mochly-Rosen D., Johnson J.A., Gray M.O., Ron D., Abramovitch E., Cerasi E., Nesher R. Translocation inhibitors define specificity of protein kinase C isoenzymes in pancreatic beta-cells. J. Biol. Chem. 272:1997;1417-1420.