Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent

Pharmacology and Therapeutics

Volumn 82, Issue 2-3, 1999, Pages 293-301

  Fabbro, Doriano ^a   Buchdunger, Elisabeth ^a   Wood, Jeannette ^a   Mestan, Jürgen ^a   Hofmann, Francesco ^a   Ferrari, Stefano ^a   Mett, Helmut ^a   O'Reilly, Terence ^a   Meyer, Thomas ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

In vitro antiproliferation; In vivo antitumor; Platelet derived growth factor (PDGF) receptor; Protein kinase C (PKC) subtypes; Vascular endothelial growth factor (VEGF) receptor

Indexed keywords

ANTIMITOTIC AGENT; ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR; FLUOROURACIL; GLYCOPROTEIN P; INSULIN RECEPTOR; ISOENZYME; MIDOSTAURIN; MITOGEN ACTIVATED PROTEIN KINASE; PLATELET DERIVED GROWTH FACTOR RECEPTOR; PROTEIN KINASE C; PROTEIN KINASE C INHIBITOR; PROTEIN KINASE INHIBITOR; SOMATOMEDIN C RECEPTOR; STAUROSPORINE; STEM CELL FACTOR RECEPTOR; VASCULOTROPIN RECEPTOR;

ANGIOGENESIS; ANIMAL CELL; ANTINEOPLASTIC ACTIVITY; AUTOPHOSPHORYLATION; CELL PROLIFERATION; CONFERENCE PAPER; DRUG MECHANISM; ENZYME INHIBITION; HUMAN; HUMAN CELL; MULTIDRUG RESISTANCE; NONHUMAN; PLASMA PROTEIN BINDING; PRIORITY JOURNAL;

ANTINEOPLASTIC AGENTS; ENDOTHELIAL GROWTH FACTORS; ENZYME INHIBITORS; FORECASTING; HUMANS; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTEIN KINASES; RECEPTORS, GROWTH FACTOR; RECEPTORS, PLATELET-DERIVED GROWTH FACTOR; STAUROSPORINE;

EID: 0033036759     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0163-7258(99)00005-4     Document Type: Conference Paper

References (52)

1. Alkan S., Rutschmann S., Grogg D., Erb P. Effect of a new protein kinase C inhibitor CGP 41251 on T cell functions. inhibition of growth and target cell killing Cell. Immunol. 150:1993;137-148.
2. Andrejauskas-Buchdunger E., Regenass U. Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C mediated signal transduction pathways by the staurosporine derivative CGP 41251. Cancer Res. 52:1992;5353-5358.
3. Asaoka Y., Nakamura S., Yoshida K., Nishizuka Y. Protein kinase C, calcium and phospho-lipid degradation. Trends Biochem. Sci. 17:1992;414-418.
4. Begemann M., Kashimawo S.A., Choi Y.A., Kim S., Christiansen K.M., Duigou G., Müller M., Schieren I., Ghosh S., Fabbro D., Lampen N.M., Schiff P.B., Bruce J.N., Weinstein I.B. Inhibition of the growth of glioblastoma by CGP 41251, an inhibitor of protein kinase C and by a phorbol ester tumor promoter. Clin. Cancer Res. 2:1996;1017-1030.
5. Begemann M., Kashimawo S.A., Heitjan D.F., Schiff P.B., Bruce J.N., Weinstein B. Treatment of human glioblastoma cells with the staurosporine derivative CGP 41251 inhibits cdc2 and ckd2 kinase activity and increases radiation sensitivity. Anticancer Res. 18:1998;2275-2282.
6. Beltram J.P., Fan D., Fidler I.J., O'Brian A.C. Chemosensitization of cancer cells by the staurosporine derivative CGP 41251 in association with decreased P-glycoprotein phosphorylation. Biochem. Pharmacol. 53:1997;245-247.
7. Blobe G.C., Sachs C.W., Khan W.A., Fabbro D., Stabel S., Wetsel W., Obeid L.M., Fine R.L., Hannun Y.A. Selective regulation of protein kinase C (PKC) isoenzymes in multidrug-resistant MCF-7 cells. J. Biol. Chem. 268:1993;658-664.
8. Blobe G.C., Obeid L.M., Hannun Y.A. Regulation of protein kinase C and role in cancer biology. Cancer Metastasis Rev. 13:1994;411-431.
9. Borner C., Fabbro D. Protein kinase C and cellular transformation. Lester D., Epand R. Protein Kinase C. Current Concepts and Future Perspectives, the Ellis Horwood Series in Biochemistry and Biotechnology:1992;297-354 Chichester, West Sussex.
10. Caravatti G., Meyer T., Fredenhagen A., Trinks U., Kump W., Mett H., Fabbro D. Inhibitory activity and selectivity of staurosporine derivatives towards protein kinase C. Bioorg. Med. Chem. Lett. 4:1994;399-404.
11. Chung D.L., Brandt-Rauf P.W., Weinstein I.B., Nishimura S., Yamaizumi Z., Murphy R.B., Pincus M.R. Evidence that the ras oncogene-encoded p21 protein induces maturation via activation of protein kinase C. Proc. Natl. Acad. Sci. USA. 89:1992;1993-1996.
12. Dekker L.V., Parker P.J. Protein kinase C. a question of specificity Trends Biochem. Sci. 19:1994;73-77.
13. Detmar M., Brown L.F., Claffey K.P., Yeo K.T., Kocher O., Jackman R.W., Berse B., Dvorak H.F. Overexpression of vascular permeability factor/vascular endothelial growth factor and its receptors in psoriasis. J. Exp. Med. 180:1994;1141-1146.
14. Dietel M. Meeting report. second international symposium on cytostatic drug resistance Cancer Res. 53:1993;2683-2688.
15. Erikson R.L. Structure, expression, and regulation of protein kinases involved in the phosphorylation of ribosomal protein S6. J. Biol. Chem. 266:1991;6007-6010.
16. Fava R.A., Olsen N.J., Spencer-Green G., Yeo K.T., Yeo T.K., Berse B., Jackman R.W., Senger D.R., Dvorak H.F., Brown L.F. Vascular permeability factor/endothelial growth factor (VPF/VEGF). accumulation and expression in human synovial fluids and rheumatoid synovial tissue J. Exp. Med. 180:1994;341-346.
17. Ferrara N., Chen H., Davis-Smith T., Gerber H.P., Nguyen T.H., Peers D., Chisholm V., Hillan K.J., Schwall R.H. Vascular endothelial growth factor is essential for corpus luteum angiogenesis. Nature Med. 4:1998;336-340.
18. Fredericks W.J., Chen Y.F., Baker R.M. Immunoblot detection of P-glycoprotein in human tumours and cell lines. Ozols R.F. Molecular and Clinical Advances in Anticancer Drug Resistance. 1991;121-149 Kluwer Academic Publishers, Boston.
19. Fuse E., Tanii H., Kurata N., Kobayashi H., Shimada Y., Yamura T., Sasaki Y., Tanigawara Y., Kuwabara T., Kobayashi S. Unpredicted clinical pharmacokinetics of UCN-01 caused by the specific binding to human alpha-acid glycoprotein. Proc. Am. Assoc. Cancer Res. 39:1998;364.
20. Geiges D., Meyer T., Marte B., Vanek M., Weissgerber G., Stabel S., Pfeilschifter J., Fabbro D., Huwiler A. Activation of protein kinase C subtypes α, γ, δ, ε, ζ, η, by tumor-promoting and nontumor-promoting agents. Biochem. Pharmacol. 53:1996;865-875.
21. Gottesman M.M. How cancer cells evade chemotherapy. Sixteenth Richard and Linda Rosenthal Foundation Award Lecture Cancer Res. 53:1993;747-754.
22. Hammes H.P., Lin J., Bretzel R.G., Brownlee M., Breier G. Upregulation of the vascular endothelial growth factor/vascular endothelial growth factor receptor system in experimental background diabetic retinopathy of the rat. Diabetes. 47:1998;401-406.
23. Hill D.L., Lin T.-H., Duncan K.L.K., Smith A.C. Binding of UCN-01 to plasma proteins of human, rats and dogs. Proc. Am. Assoc. Cancer Res. 39:1998;364.
24. Houslay M.D. "Crosstalk" a pivotal role for protein kinase C in mediating relationship between signal transduction pathways Eur. J. Biochem. 195:1991;9-27.
25. Ikegami Y., Yano S., Nakao K. Antitumor effect of CGP 41251, a new selective protein kinase C inhibitor, on human non-small cell lung cancer cells. Jpn. J. Pharmacol. 70:1996;65-72. a.
26. Ikegami Y., Yano S., Nakao K. Effects of the new selective protein kinase C inhibitor 4′-N-benzoyl staurosporine on cell cycle distribution and growth inhibition in human small cell lung cancer cells. Arzneimittelforschung/Drug Res. 46:1996;201-204. b.
27. Killion J.J., Beltran P., O'Brian C.A., Yoon S.-S., Fan D., Wilson M.R., Fidler I.J. The antitumor activity of doxorubicin against drug-resistant murine carcinoma is enhanced by oral administration of a synthetic staurosporine analogue, CGP 41251. Oncol. Res. 7:1995;453-459.
28. Ludescher C., Eisterer W., Hilbe W., Hofmann J., Thaler J. Decreased potency of MDR-modulators under serum conditions determined by functional assay. Br. J. Haematol. 91:1995;652-657.
29. Marte B.M., Meyer T., Stabel S., Jaken S., Fabbro D., Hynes N.E. Protein kinase C and mammary cell differentiation. an essential role for PKC-α in the induction of μ-casein expression Cell Growth Differ. 5:1994;239-247.
30. Marte B.M., Graus-Porta D., Jeschke M., Fabbro D., Hynes N.E., Taverna D. NDF/heregulin activates MAP kinase and p70/85 S6 kinase during proliferation and differentiation of mammary epithelial cells. Oncogene. 10:1995;167-175.
31. Matter A., Meyer T., Caravatti C., Fabbro D., Mett H., Koizumi S., Geissler J., Lydon N., Traxler P., Regenass U. A pharmacological approach to growth regulation of breast cancer cells. Lippman M.E., Mihich E. The Therapeutic Implications of the Molecular Biology of Breast Cancer, Pezcoller Foundation Symposia. 1990;227-246 John Libbey CIC, Trento, Italy.
32. Matthews W., Jordan C.T., Gavin M., Jenkins N.A., Copeland N.G., Lemischka I.R. A receptor tyrosine kinase cDNA isolated from a population of enriched primitive hematopoietic cells and exhibiting close genetic linkage to c-kit. Proc. Natl. Acad. Sci. USA. 88:1991;9026-9030.
33. McDonald A.C., Propper D., Champain K., Graf P., Man A., Caponigro F., Thavasu P., Balkwill F., Twelves C., Kaye S.B., Harris A.L., King D. Phase I and pharmacokinetic study of CGP 41251, an inhibitor of protein kinase C. Proc. Am. Soc. Clin. Oncol. 16:1997;212a.
34. Meggio F., Donella Deana A., Ruzzene M., Brunati A.M., Cesaro L., Guerra B., Meyer T., Mett H., Fabbro D., Furet P., Dobrowolska A., Pinna L.A. Different susceptibility of protein kinases to staurosporine inhibition. Kinetic studies and molecular bases for the resistance of protein kinase CK2. Eur. J. Biochem. 234:1995;317-322.
35. Meyer T., Regenass U., Fabbro D., Alteri E., Rösel J., Müller M., Caravatti G., Matter A. A derivative of staurosporine (CGP 41251) shows selectivity for protein kinase C inhibition and in vitro antiproliferative as well as in vivo antitumour activity. Int. J. Cancer. 43:1989;851-856.
36. Miyamoto K., Inoko K., Wakusawa S., Kajita J., Hasegawa T., Takagi A., Koyama M. Inhibition of multidrug resistance by a staurosporine derivative, NA-382, in vitro and in vivo. Cancer Res. 53:1993;1555-1559.
37. Parker P.J., Dekker L. Protein Kinase C. 1997;Landes, Austin.
38. Pastan I., Gottesman M.M. Multidrug resistance. Annu. Rev. Med. 41:1991;277-286.
39. Perletti G.P., Monti E. PKCs. transducers of critical signals in cancer cells (review) Int. J. Oncol. 9:1996;171-177.
40. Plate K.H., Breier G., Millauer B., Ullrich A., Risau W. Up-regulation of vascular endothelial growth factor and its cognate receptors in a rat glioma model of tumor angiogenesis. Cancer Res. 53:1993;5822-5827.
41. Sampson E., Wolff C.L., Abraham I. Staurosporine reduces P-glycoprotein expression and modulates MDR. Cancer Lett. 68:1993;7-14.
42. Sanford M.S., Schindler M. Cell biological mechanisms of multidrug resistance in tumours. Proc. Natl. Acad. Sci. USA. 91:1994;3497-3504.
43. Sato W., Yusa K., Naito M., Tsuruo T. Staurosporine, a potent inhibitor of C-kinase, enhances drug accumulation in multidrug-resistant cells. Biochem. Biophys. Res. Commun. 173:1990;1252-1257.
44. Schwartz G.K. Oncologic, endocrine and metabolic. Protein kinase C inhibitors as inducers of apoptosis for cancer therapy. Expert Opin. Invest. Drugs. 5:1996;1601-1615.
45. Sedlak J., Hunakova L., Dutaj J., Chorvath B., Novotny L. Effects of protein kinase C inhibitor, staurosporine derivative CGP 41251, on cell cycle, DNA synthesis and drug uptake in neoplastic cell lines. Anticancer Drugs. 6:1995;70-76.
46. Shibuya M., Yamaguchi S., Yamane A., Ikeda T., Tojo A., Matsushime H., Sato M. Nucleotide sequence and expression of a novel human receptor-type tyrosine kinase gene (flt) closely related to the fms family. Oncogene. 5:1990;519-524.
47. Shustik C., Dalton W., Gros P. P-glycoprotein-mediated multidrug resistance in tumour cells. biochemistry, clinical relevance and modulation Mol. Aspects Med. 16:1995;1-78.
48. Susa M., Vulevic D., Lane H.A., Thomas G. Inhibition or down regulation of protein kinase C attenuates late phase p70s6k activation induced by epidermal growth factor but not by platelet-derived growth factor or insulin. J. Biol. Chem. 267:1992;6905-6909.
49. Terman B.I., Carrion M.E., Kovacs E., Rasmussen B.A., Eddy R.L., Shows T.B. Identification of a new endothelial cell growth factor receptor tyrosine kinase. Oncogene. 6:1991;1677-1683.
50. Utz I., Hofer S., Regenass U., Hilbe W., Thaler J., Grunicke H., Hofmann J. The protein kinase C inhibitor CGP 41251. a staurosporine derivative with antitumour activity, reverses multidrug resistance Int. J. Cancer. 57:1994;104-110.
51. Utz I., Spitaler M., Rybczynska M., Ludescher C., Hilbe W., Regenass U., Grunicke H., Hofmann J. Reversal of multidrug resistance by staurosporine derivatives CGP 41251 and CGP 42700. Int. J. Cancer. 77:1998;64-69.
52. Van Kalken C.K., Pinedo H.M., Giaccone G. Multidrug resistance from the clinical point of view. Eur. J. Cancer. 27:1991;1481-1486.