Protein kinase C as a therapeutic target

Clinical Cancer Research

Volumn 12, Issue 18, 2006, Pages 5336-5345

  Teicher, Beverly A ^a  

^a GENZYME CORPORATION   (United States)

Author keywords

[No Author keywords available]

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 AMIDINOTHIOPROPYL) 1H INDOL 3 YL] 3 (1 METHYL 1H INDOL 3 YL)MALEIMIDE; 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; 4 [N (2 HYDROXYETHYL) N [2 (3 INDOLYL)ETHYL]AMINOMETHYL]CINNAMOHYDROXAMIC ACID; 7 HYDROXYSTAUROSPORINE; BISINDOLYLMALEIMIDE; CAFFEINE; CAPECITABINE; CARBOPLATIN; CARMUSTINE; CISPLATIN; ENZASTAURIN; ETOPOSIDE; FLUOROURACIL; GEMCITABINE; IMATINIB; ISIS 3521; LOMUSTINE; MIDOSTAURIN; PACLITAXEL; PEMETREXED; PROTEIN KINASE C; PROTEIN KINASE C INHIBITOR; RAPAMYCIN; ROTTLERIN; UNCLASSIFIED DRUG;

ACUTE GRANULOCYTIC LEUKEMIA; B CELL LYMPHOMA; BRAIN TUMOR; BREAST CANCER; CANCER RECURRENCE; CANCER SURVIVAL; CLINICAL TRIAL; COLON CANCER; DOSE RESPONSE; DRUG INHIBITION; ENDOMETRIUM CANCER; GASTROINTESTINAL STROMAL TUMOR; GLIOBLASTOMA; GLIOMA; HUMAN; LEUKEMIA; LUNG CANCER; LUNG NON SMALL CELL CANCER; LYMPHOMA; MULTIPLE MYELOMA; NONHODGKIN LYMPHOMA; NONHUMAN; OVARY CANCER; PRIORITY JOURNAL; PROSTATE CANCER; PROTEIN TARGETING; REVIEW; SKIN CANCER; SOLID TUMOR; STOMACH CANCER;

ANIMALS; BRAIN NEOPLASMS; DRUG DELIVERY SYSTEMS; FEMALE; HUMANS; MALE; MODELS, BIOLOGICAL; NEOPLASMS; PROTEIN KINASE C; PROTEIN KINASE INHIBITORS;

EID: 33749358558     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-06-0945     Document Type: Review

References (92)

1. Nishizuka Y. Intracellular signaling by hydrolysis of phospholipids and activation of PKC. Science 1992;258:607-14.
2. Way KJ, Chou E, King GL. Identification of PKC-isoform-specific biological actions using pharmacological approaches. Trends Pharmacol Sci 2000;21:181-7.
3. Carter CA, Kane CJ. Therapeutic potential of natural compounds that regulate the activity of protein kinase C. Curr Med Chem 2004;11:2883-902.
4. Hofmann J. Protein kinase C (PKC) isozymes as potential targets for anticancer therapy. Curr Cancer Drug Targets 2004;4:125-46.
5. Violin JD, Zhang J, Tsien RY, Newton AC. A genetically encoded fluorescent reporter reveals oscillatory phosphorylation by protein kinase C. J Cell Biol 2003;161:899-909.
6. Bhalla US, Iyengar R. Emergent properties of networks of biological signaling pathways. Science 1999;283:381-7.
7. Chu F, O'Brian CA. PKC sulfhydryl targeting by disulfiram produces divergent isozymic regulatory responses that accord with the cancer preventive activity of the thiuram disulfide. Antioxid Redox Signal 2005;7:855-62.
8. Chu F, Chen LH, O'Brian CA. Cellular protein kinase C isozyme regulation by exogenously delivered physiological disulfides-implications of oxidative protein kinase C regulation to cancer prevention. Carcinogenesis 2004;25:585-96.
9. Santiago-Walker AE, Fikaris AJ, Kao GD, Brown EJ, Kazanietz MG, Meinkoth JL. Protein kinase Cδ stimulates apoptosis by initiating G1 phase cell cycle progression and S phase arrest. J Biol Chem 2005;280:32107-114.
10. Gustafson WC, Ray S, Jamieson L, Thompson EA, Brasier AR, Fields AP. Bcr-Abl regulates protein kinase Cι (PKCι) transcription via an Elk1 site in the PKCι promoter. J Biol Chem 2004;279:9400-8.
11. Murray NR, Jamieson L, Yu W, et al. Protein kinase Cι is required for Ras transformation and colon carcinogenesis in vivo. J Cell Biol 2004;164:797-802.
12. Denning MF. Epidermal keratinocytes: regulation of multiple cell phenotypes by multiple protein kinase C isoforms. Int J Biochem Cell Biol 2004;36:1141-6.
13. Sitailo LA, Tibudan SS, Denning MF. Bax activation and induction of apoptosis in human keratinocytes by the protein kinase Cδ catalytic domain. J Invest Dermatol 2004;123:434-43.
14. D'Costa AM, Denning MF. A caspase-resistant mutant of PKC-δ protects keratinocytes from UV-induced apoptosis. Cell Death Differ 2005;12:224-32.
15. Aziz MH, Wheeler DL, Bhamb B, Verma AK. Protein kinase Cδ overexpressing transgenic mice are resistant to chemically but not to UV radiation-induced development of squamous cell carcinomas: a possible link to specific cytokines and cyclooxygenase-2. Cancer Res 2006;66:713-22.
16. Wheeler DL, Martin KE, Ness KJ, et al. Protein kinase Cε is an endogenous photosensitizer that enhances ultraviolet radiation-induced cutaneous damage and development of squamous cell carcinomas. Cancer Res 2004;64:7756-65.
17. Wheeler DL, Reddig PJ, Ness KJ, Leith CP, Oberley TD, Verma AK. Overexpression of protein kinase Cε in the mouse epidermis leads to a spontaneous myeloproliferative-like disease. Am J Pathol 2005;166:117-26.
18. Wheeler DL, Li Y, Verma AK. Protein kinase Cε ultraviolet light-induced cutaneous damage and development of squamous cell carcinoma possibly through induction of specific cytokines in a paracrine mechanism. Photochem Pholobiol 2005;81:9-18
19. Cerda SR, Bissonnette M, Scaglione-Sewell B, et al. PKC-δ inhibits anchorage-dependent and -independent growth, enhances differentiation and increases apoptosis in CaCo-2 cells. Gastroenterology 2001;120:1868-72.
20. Yu W, Murray NR, Weems C, et al. Role of cyclooxygenase 2 in protein kinase CβII-mediated colon carcinogenesis. J Biol Chem 2003;278:11167-74.
21. Liu Y, Su W, Thompson EA, Leitges M, Murria NR, Fields AP. Protein kinase CβII regulates its own expression in rat intestinal epithelial cells and the colonic epithelium in vivo. J Biol Chem 2004;279:45556-63.
22. Liou JS, Chen JS, Faller DV. Characterization of p21 Ras-mediated apoptosis induced by protein kinase C inhibition and application to human tumor cell lines. J Cell Physiol 2004;198:277-94.
23. Zhang J, Anastasiadis PZ, Liu Y, Thompson EA, Fields AP. Protein Kinase C (PKC) βII induces cell invasion through a Ras/Mek-, PKCι/Rac 1-dependent signaling pathway. J Biol Chem 2004;279:22118-23.
24. Bivona TG, Quatela SE, Bodemann BO, et al. PKC regulates a farnesyl-electrostatic switch on K-Ras that promotes its association with Bcl-XL on mitochondria and induces apoptosis. Mol Cell 2006;21:481-93.
25. Atten MJ, Godoy-Romero E, Attar BM, Milson T, Zopel M, Holian O. Resveratrol regulates cellular PKCα and δ to inhibit growth and induce apoptosis in gastric cancer cells. Invest New Drugs 2005;23:111-9.
26. Gavrielides MV, Frijhoff AF, Conti CJ, Kazanietz MG. Protein kinase C and prostate carcinogenesis: targeting the cell cycle and apoptotic mechanisms. Curr Drug Targets 2004;5:431-43.
27. Stewart JR, O'Brian CA. Protein kinase C-{α} mediates epidermal growth factor transactivation in human prostate cancer cells. Mol Cancer Ther 2005;4:726-32.
28. McJilton MA, Van Sikes C, Wescott GG, et al. Protein kinase Cε interacts with Bax and promotes survival of human prostate cancer cells. Oncogene 2003;22:7958-68.
29. Wu D, Thakore CU, Wescott GG, McCubrey JA, Terrien DM. Integrin signaling links protein kinase Cε to the protein kinase B/Akt survival pathway in recurrent prostate cancer cells. Oncogene 2004;23:8659-72.
30. Eder AM, Sui X, Rosen DG, et al. Atypical PKCι contributes to poor prognosis through loss of apical-basal polarity and cyclin E overexpression in ovarian cancer. Proc Natl Acad Sci U S A 2005;102:12519-24.
31. Lahn M, Kohler G, Sundell K, et al. Protein kinase Cα expression in breast and ovarian cancer. Oncology 2004;67:1-10.
32. Lee SI, Brown MK, Eastman A. Comparison of the efficacy of 7-hydroxystaurosporine (UCN-01) am other staurosporine analogs to abrogate cisplatin-induced cell cycle arrest in human breast cancer cell lines. Biochem Pharmacol 1999;58:1713-21.
33. Sun R, Gao P, Chen L, et al. Protein kinase C ζ is required for epidermal growth factor-induced chemotaxis of human breast cancer cells. Cancer Res 2005;65:1433-41.
34. Regala RP, Weems C, Jamieson L, Copland JA, Thompson EA, Fields AP. Atypical protein kinase Cι plays a critical role in human lung cancer cell growth and tumorigenicity. J Biol Chem 2005;280:31109-15.
35. Regala RP, Weems C, Jamieson L, et al. Atypical protein kinase Cι is an oncogene in human non-small lung cancer. Cancer Res 2005;65:8905-11.
36. Jin Z, Xin M, Deng X. Survival function of protein kinase C{iota} as a novel nitrosamine 4- (methylnitrosamine)-1-(3-pyridyl)-1-butanone-activated bad kinase. J Biol Chem 2005;280:16045-52.
37. Stallings-Mann M, Jamieson L, Regala RP, Weems C, Murray NR, Fields AP. A novel small-molecule inhibitor of protein kinase Cι blocks transformed growth of non-small cell lung cancer cells. Cancer Res 2006;66:1767-74.
38. Clark AS, West KA, Blumberg PM, Dennis PA. Altered protein kinase C (PKC) isoforms in non-small cell lung cancer cells: PKCδ promotes cellular survival and chemotherapeutic resistance. Cancer Res 2003;63:780-6.
39. Ding L, Wang H, Lang W, Xiao L. Protein kinase C-ε promotes survival of lung cancer cells by suppressing apoptosis through dysregulation of the mitochondrial caspase pathway. J Biol Chem 2002;277:35305-13.
40. Lang W, Wang H, Ding L, Xiao L. Cooperation between PKC-α and PKC-ε in the regulation of JNK activation in human lung cancer cells. Cell Signal 2004;16:457-67.
41. Louis K, Guerineau N, Fromigue O, et al. Tumor cell-mediated induction of the stromal factor stromelysin-3 requires heterotypic cell contact-dependent activation of specific protein kinase C isoforms. J Biol Chem 2005;280:1272-83.
42. Villalona-Calero MA, Ritch P, Figueroa JA, et al. A phase I/II study of LY900003, an antisense inhibitor of protein kinase C-α, in combination with cisplatin and gemcitabine in patients with advanced non-small cell lung cancer. Clin Cancer Res 2004;10:6086-93.
43. Corbit KC, Soh JW, Yoshida K, Eves EM, Weinstein IB, Rosner MR. Different protein kinase C isoforms determine growth factor specificity in neuronal cells. Mol Cell Biol 2000;20:5392-403.
44. Corbit KC, Trakul N, Eves EM, Diaz B, Marshall M, Rosner MR. Activation of Raf-1 signaling by protein kinase C through a mechanism involving Raf kinase inhibitory protein. J Biol Chem 2003;278:13061-8.
45. Aeder SE, Martin PM, Soh JW, Hussaini IM. PKC-η mediates glioblastoma cell proliferation through the Akt and mTOR signaling pathways. Oncogene 2004;23:9062-9.
46. Amos S, Martin PM, Polar GA, Parsons SJ, Hussaini IM. Phorbol 12-myristate 13-acetate induces epidermal growth factor receptor transactivation via protein kinase Cδ/c-Src pathways in glioblastoma cells. J Biol Chem 2005;280:7729-38.
47. Ni H, Ergin M, Tibudan SS, Denning MF, Izban KF, Alkan S. Protein kinase C-δ is commonly expressed in multiple myeloma cells and its downregulation by rottlerin causes apoptosis. Br J Haematol 2003;121:849-56.
48. Alkan S, Huang Q, Ergin M, et al. Survival role of protein kinase C (PKC) in chronic lymphocytic leukemia and determination of isoform expression pattern and genes altered by PKC inhibition. Am J Hematol 2005;79:97-106.
49. Michie AM, Nakagawa R. The link between PKCα regulation and cellular transformation. Immunol Lett 2005;96:155-62.
50. Tamamura H, Signano DM, Lewin NE, et al. Conformationally constrained analogs of diacylglycerol (DAG). 23. hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PKC). J Med Chem 2004;47:4858-64.
51. Lampe JW, Biggers CK, Defauw JM, et al. Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits. J Med Chem 2002;45:2624-43.
52. Dieter P, Fitzke E. RO 31-8220 and RO 31-7549 show improved selectivity for protein kinase C over staurosporine in macrophages. Biochem Biophys Res Commun 1991;181:396-401.
53. Newton RC, Decicco CP. Therapeutic potential and strategies for inhibiting tumor necrosis factor-α. J Med Chem 1999;42:2295-314.
54. Sausville EA, Arbuck SG, Messmann R, et al. Phase I trial of 72-hour continuous infusion UCN-01 in patients with refractory neoplasms. J Clin Oncol 2001;19:2319-33.
55. Mack PC, Lara PN, Longmate J, et al. Phase I and correlative science trial of UCN-01 plus cisplatin (CDDP) in advanced solid tumors: a California Cancer Consortium Study [abstract 9591]. Proc Am Soc Clin Oncol 2004.
56. Hirte HW. A phase II study of UCN-01 in combination with topotecan in patients with advanced recurrent ovarian cancer: a Princess Margaret Phase II Consortium Trial [abstract 3127]. Proc Am Soc Clin Oncol 2005.
57. Si MS, Reitz BA, Borie DC. Effects of the kinase inhibitor CGP41251 (PKC 412) on lymphocyte activation and TNF-α production. Int Immunopharmacol 2005;5:1141-9.
58. Tenzer A, Zingg D, Rocha S, et al. The phosphatidylinositide 3′-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C Cancer Res 2001;61:8203-10.
59. Nakamura K, Yoshikawa N, Yamaguchi Y, Kagota S, Shinozuka K, Kunitomo M. Effect of PKC412, an inhibitor of protein kinase C, on spontaneous metastatic model mice. Anticancer Res 2003;23:1395-9.
60. Ganeshaguru K, Wickremasinghe RG, Jones DT, et al. Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica 2002;87:167-76.
61. Hemstrom TH, Joseph B, Schulte G, Lewensohn R. Zhivotovsky B. PKC 412 sensitizes U1810 non-small cell lung cancer cells to DNA damage. Exp Cell Res 2005;305:200-13.
62. Bahlis NJ, Miao Y, Koc ON, Gerson S. N-Benzoylstaurosporine (PKC412) inhibits AKT kinase inducing apoptosis in multiple myeloma cells [abstract 6503]. Proc Am Soc Clin Oncol 2005.
63. Growney JD, Clark JJ, Adelsperger J, et al. Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412. Blood 2005;106:721-4.
64. Gotlib J, Beruhe C, Growney JD, et al. Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation. Blood 2005;106:2865-70.
65. Cools J, Mentens N, Furet P, et al. Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia. Cancer Res 2004;64:6385-9.
66. George P, Bali P, Cohen P, et al. Cotreatment with 17-allylamino- demethoxygeldaamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3. Cancer Res 2004;64:3645-52.
67. Bali P, George P, Cohen P, et al. Superior activity of the combination of histone deacetylase inhibitor LAQ824 and the FLT-3 kinase inhibitor PKC412 against human acute myelogenous leukemia cells with mutant FLT-3. Clin Cancer Res 2004;10:4991-7.
68. Eder JP, Garcia-Carbonero R, Clark JW, et al. A phase I trial of daily oral 4′-N-benzoyl-staurosporine in combination with protracted continuous infusion 5-fluorouracil in patients with advanced solid malignancies. Invest New Drugs 2004;22:139-50.
69. Monnerat C, Henriksson R, Le Chevalier T, et al. Phase I study of PKC412 (N-benzoyl-staurosporine), a novel oral protein kinase C inhibitor, combined with gemcitabine and cisplatin in patients with non-small cell lung cancer. Ann Oncol 2004;15:316-23.
70. Heidel F, Solem FK, Breitenbuecher F, et al. Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain. Blood 2006;107:293-300.
71. Teicher BA, Alvarez E, Menon K, et al. Antiangtogenic effects of a protein kinase Cβ-selective small molecule. Cancer Chemother Pharmacol 2002;49:69-77.
72. Liu Y, Su W, Thompson EA, Leitges M, Murray NR, Fields AP. Protein kinase CβII regulates its own expression in rat intestinal epithelial cells and the colonic epithelium in vivo. J Biol Chem 2004;279:45556-63.
73. Rizvi MA, Ghias K, Davies KM, Ma C, Krett NL, Rosen ST. Enzastaurin (LY317615), an oral protein kinase C b inhibitor, induces apoptosis in multiple myeloma cell lines [abstract 1577]. Amer Soc Hematol 2005.
74. Podar K, Raab MS, Abtahi D, et al. The PKC-inhibitor enzastaurin inhibits MM cell growth, survival and migration in the bone marrow microenvironment [abstract 1584]. Amer Soc Hematol 2005.
75. Rossi RM, Henn AD, Conkling R, et al. The PKCβ selective inhibitor, enzastaurin (LY317615), inhibits growth of human lymphoma cells [abstract 1483]. Amer Soc Hematol 2005.
76. Rieken M, Weigert O, Pastore A, et al. Inhibition of protein kinase Cβ by enzastaurin (LY317615) induces alterations of key regulators of cell cycle and apoptosis in mantle cell lymphoma and synergizes with chemotherapeutic agents in a sequence dependent manner [abstract 2416]. Amer Soc Hematol 2005.
77. Teicher BA, Menon K, Alvarez E, Galbreath E, Shih C, Faul MM. Antiangiogenic and antitumor effects of a protein kinase Cβ inhibitor in human HT-29 colon carcinoma and human Caki-1 renal cell carcinoma xenografts. Anticancer Res 2001;21:3175-84.
78. Teicher BA, Menon K, Alvarez E, Galbreath E, Shih C, Faul MM. Antiangiogenic and antitumor effects of a protein kinase Cβ inhibitor in murine Lewis lung carcinoma and human Calu-6 non-small cell lung carcinoma xenografts. Cancer Chemother Pharmacol 2001;48:473-80.
79. Teicher BA, Menon K, Alvarez E, Liu P, Shih C, Faul MM. Antiangiogenic and antitumor effects of a protein kinase Cβ inhibitor in human hepatocellular and gastric cancer xenografts. In Vivo 2001;15:185-93.
80. Teicher BA, Menon K, Alvarez E, Galbreath E, Shih C, Faul MM. Antiangiogenic and antitumor effects of a protein kinase Cβ inhibitor in human T98G glioblastoma multiforme xenografts. Clin Cancer Res 2001;7:634-40.
81. Keyes K, Cox K, Treadway P, et al. An In vitro tumor model: analysis of angiogenic factor expression after chemotherapy. Cancer Res 2002;62:5597-602.
82. Keyes K, Mann L, Cox K, et al. Circulating angiogenic growth factor levels in mice bearing human tumors using Luminex multiplex technology. Cancer Chemother Pharmacol 2003;51:321-7.
83. Keyes KA, Mann L, Sherman M, et al. LY317615 decreases plasma VEGF levels in human tumor xenograft-bearing mice. Cancer Chemother Pharmacol 2004;53:133-40.
84. Herbst RS, Thornton DE, Kies MS, et al. Phase 1 study of LY317615, a protein kinase Cβ inhibitor [abstract 326]. Amer Soc Clin Oncol 2002.
85. Watkins V, Hong S, Lin B. Enzastaurin safety review: data from phase I and phase II trials [abstract 13077]. Amer Soc Clin Oncol 2006.
86. Green LJ, Marder P, Ray C, et al. Development and validation of a drug activity biomarker that shows target inhibition in cancer patients receiving enzastaurin, a novel protein kinase C-β inhibitor. Clin Cancer Res 2006;12:3408-15.
87. Robertson M, Kahl B, Vose J, et al. A phase II study of enzastaurin, a protein kinase C-β (PKCβ) inhibitor, in the treatment of relapsed diffuse large B-cell lymphoma (DLBCL) [abstract 934]. Amer Soc Hematol 2005.
88. Fine HA, Kim L, Royce C, et al. A phase II trial of LY317615 in patients with recurrent high grade gliomas [abstract 1511]. Amer Soc Clin Oncol 2004.
89. Fine HA, Kim L, Royce C, et al. Results from phase II trial of enzastaurin (LY317615) in patients with recurrent high grade gliomas [abstract 1504]. Amer Soc Clin Oncol 2004.
90. Leong S, Camidge G, Eckhardt G, et al. A phase I dose-escalation and pharmacokinetic study of enzastaurin combined with capecitabine in patients with advanced cancer [abstract 2048]. Amer Soc Clin Oncol 2006.
91. Hanauske A, Weigang Koehler K, Yilmaz E, et al. Pharmacokinetic interaction and safety of enzastaurin and premetrexed in patients with advanced or metastatic cancer [abstract 2047]. Amer Soc Clin Oncol 2006.
92. Beerepoot L, Rademaker-Lakhai J, Witteveen E, et al. Phase I and pharmacokinetic evaluation of enzastaurin with gemcitabine and cisplatin in advanced cancer [abstract 2046]. Amer Soc Clin Oncol 2006.