Oral small-molecule tyrosine kinase inhibitor midostaurin (PKC412) inhibits growth and induces megakaryocytic differentiation in human leukemia cells

Toxicology in Vitro

Volumn 23, Issue 6, 2009, Pages 979-985

  Huang, Yu Chuen ^a,b,c,d   Chao, David K ^a   Clifford Chao, K S ^e   Chen, Yu Jen ^a,f  

^a MACKAY MEMORIAL HOSPITAL   (Taiwan)

^b INSTITUTE OF PHYSICS   (Taiwan)

^c CHINA MEDICAL UNIVERSITY HOSPITAL   (Taiwan)

^d CHINA MEDICAL UNIVERSITY   (Taiwan)

^e Columbia University College of Physicians and Surgeons ^*  (United States)

^f CHINESE CULTURE UNIVERSITY   (Taiwan)

Author keywords

Apoptosis; Differentiation; Megakaryocyte; Midostaurin; PKC412

Indexed keywords

CD61 ANTIGEN; DNA; GLYCOPHORIN A; MIDOSTAURIN; THROMBOPOIETIN RECEPTOR;

ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; CANCER GROWTH; CANCER INHIBITION; CELL DIFFERENTIATION; CELL STRAIN K 562; CELL STRUCTURE; CHRONIC MYELOID LEUKEMIA; CONTROLLED STUDY; ERYTHROLEUKEMIA; HUMAN; HUMAN CELL; LEUKEMIA CELL LINE; MEGAKARYOCYTE; MITOSIS SPINDLE; POLYPLOIDY; PROTEIN EXPRESSION; SIGNAL TRANSDUCTION;

ANTINEOPLASTIC AGENTS; APOPTOSIS; CELL DIFFERENTIATION; CELL LINE, TUMOR; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; K562 CELLS; LEUKEMIA; MEGAKARYOCYTES; PROTEIN KINASE INHIBITORS; RECEPTORS, THROMBOPOIETIN; SIGNAL TRANSDUCTION; STAUROSPORINE; TIME FACTORS; UP-REGULATION;

EID: 68049104046     PISSN: 08872333     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tiv.2009.06.027     Document Type: Article

References (37)

1. Debiec-Rychter M., Cools J., Dumez H., Sciot R., Stul M., Mentens N., Vranckx H., Wasag B., Prenen H., Roesel J., Hagemeijer A., Van O.A., and Marynen P. Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants. Gastroenterology 128 (2005) 270-279
2. Deininger M.W., Goldman J.M., Lydon N., and Melo J.V. The tyrosine kinase inhibitor CGP57148B selectively inhibits the growth of BCR-ABL-positive cells. Blood 90 (1997) 3691-3698
3. Dekker L.V., and Parker P.J. Protein kinase C - a question of specificity. Trends in Biochemistry Sciences 19 (1994) 73-77
4. Drachman J.G., Griffin J.D., and Kaushansky K. The c-Mpl ligand (thrombopoietin) stimulates tyrosine phosphorylation of Jak2, Shc, and c-Mpl. Journal of Biological Chemistry 270 (1995) 4979-4982
5. Druker B.J., Tamura S., Buchdunger E., Ohno S., Segal G.M., Fanning S., Zimmermann J., and Lydon N.B. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nature Medicine 2 (1996) 561-566
6. Fabbro D., Ruetz S., Bodis S., Pruschy M., Csermak K., Man A., Campochiaro P., Wood J., O'Reilly T., and Meyer T. PKC412 - a protein kinase inhibitor with a broad therapeutic potential. Anti-cancer Drug Design 15 (2000) 17-28
7. Furukawa Y., Vu H.A., Akutsu M., Odgerel T., Izumi T., Tsunoda S., Matsuo Y., Kirito K., Sato Y., Mano H., and Kano Y. Divergent cytotoxic effects of PKC412 in combination with conventional antileukemic agents in FLT3 mutation-positive versus-negative leukemia cell lines. Leukemia 21 (2007) 1005-1014
8. Gambacorti-Passerini C., Le C.P., Mologni L., Fanelli M., Bertazzoli C., Marchesi E., Di N.M., Biondi A., Corneo G.M., Belotti D., Pogliani E., and Lydon N.B. Inhibition of the ABL kinase activity blocks the proliferation of BCR/ABL+ leukemic cells and induces apoptosis. Blood Cells, Moleculars and Diseases 23 (1997) 380-394
9. George J.N., Nurden A.T., and Phillips D.R. Molecular defects in interactions of platelets with the vessel wall. New England Journal of Medicine 311 (1984) 1084-1098
10. Goekjian P.G., and Jirousek M.R. Protein kinase C inhibitors as novel anticancer drugs. Expert Opinion on Investigational Drugs 10 (2001) 2117-2140
11. Gorre M.E., Mohammed M., Ellwood K., Hsu N., Paquette R., Rao P.N., and Sawyers C.L. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science 293 (2001) 876-880
12. Growney J.D., Clark J.J., Adelsperger J., Stone R., Fabbro D., Griffin J.D., and Gilliland D.G. Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412. Blood 106 (2005) 721-724
13. Hong Y., Martin J.F., Vainchenker W., and Erusalimsky J.D. Inhibition of protein kinase C suppresses megakaryocytic differentiation and stimulates erythroid differentiation in HEL cells. Blood 87 (1996) 123-131
14. Hunakova L., Sedlak J., Klobusicka M., Sulikova M., and Chorvath B. Phorbol ester (TPA)-induced differential modulation of cell surface antigens in human pluripotential leukemia (K-562) cell line: effects of protein kinase inhibitors with broad- and PKC selective inhibitory activity. Neoplasma 42 (1995) 249-253
15. Kantarjian H., Sawyers C., Hochhaus A., Guilhot F., Schiffer C., Gambacorti-Passerini C., Niederwieser D., Resta D., Capdeville R., Zoellner U., Talpaz M., Druker B., Goldman J., O'Brien S.G., Russell N., Fischer T., Ottmann O., Cony-Makhoul P., Facon T., Stone R., Miller C., Tallman M., Brown R., Schuster M., Loughran T., Gratwohl A., Mandelli F., Saglio G., Lazzarino M., Russo D., Baccarani M., and Morra E. Hematologic and cytogenetic responses to imatinib mesylate in chronic myelogenous leukemia. New England Journal of Medicine 346 (2002) 645-652
16. Kaushansky K. The thrombocytopenia of cancer. Prospects for effective cytokine therapy. Hematology/Oncology Clinics of North America 10 (1996) 431-455
17. Knapper S. FLT3 inhibition in acute myeloid leukaemia. British Journal of Haematology 138 (2007) 687-699
18. Koeffler H.P., and Golde D.W. Human myeloid leukemia cell lines: a review. Blood 56 (1980) 344-350
19. Lazarus A.H., Ellis J., Semple J.W., Mody M., Crow A.R., and Freedman J. Comparison of platelet immunity in patients with SLE and with ITP. Transfusion Science 22 (2000) 19-27
20. Leszczyniecka M., Roberts T., Dent P., Grant S., and Fisher P.B. Differentiation therapy of human cancer: basic science and clinical applications. Pharmacology and Therapeutics 90 (2001) 105-156
21. Long M.W., Heffner C.H., Williams J.L., Peters C., and Prochownik E.V. Regulation of megakaryocyte phenotype in human erythroleukemia cells. Journal of Clinical Investigation 85 (1990) 1072-1084
22. Lozzio B.B., and Lozzio C.B. Properties of the K562 cell line derived from a patient with chronic myeloid leukemia. International Journal of Cancer 19 (1977) 136
23. Martin P., and Papayannopoulou T. HEL cells: a new human erythroleukemia cell line with spontaneous and induced globin expression. Science 216 (1982) 1233-1235
24. Nemunaitis J., Holmlund J.T., Kraynak M., Richards D., Bruce J., Ognoskie N., Kwoh T.J., Geary R., Dorr A., Von H.D., and Eckhardt S.G. Phase I evaluation of ISIS 3521, an antisense oligodeoxynucleotide to protein kinase C-alpha, in patients with advanced cancer. Journal of Clinical Oncology 17 (1999) 3586-3595
25. Nowell P., and Hungerford D. A minute chromosome in human chronic granulocytic leukemia. Science 132 (1960) 1497
26. Odgerel T., Kikuchi J., Wada T., Shimizu R., Futaki K., Kano Y., and Furukawa Y. The FLT3 inhibitor PKC412 exerts differential cell cycle effects on leukemic cells depending on the presence of FLT3 mutations. Oncogene 27 (2008) 3102-3110
27. O'Dwyer M.E., and Druker B.J. STI571: an inhibitor of the BCR-ABL tyrosine kinase for the treatment of chronic myelogenous leukaemia. The Lancet Oncology 1 (2000) 207-211
28. Propper D.J., McDonald A.C., Man A., Thavasu P., Balkwill F., Braybrooke J.P., Caponigro F., Graf P., Dutreix C., Blackie R., Kaye S.B., Ganesan T.S., Talbot D.C., Harris A.L., and Twelves C. Phase I and pharmacokinetic study of PKC412, an inhibitor of protein kinase C. Journal of Clinical Oncology 19 (2001) 1485-1492
29. Quentmeier H., MacLeod R.A., Zaborski M., and Drexler H.G. JAK2 V617F tyrosine kinase mutation in cell lines derived from myeloproliferative disorders. Leukemia 20 (2006) 471-476
30. Rouyez M.C., Boucheron C., Gisselbrecht S., Dusanter-Fourt I., and Porteu F. Control of thrombopoietin-induced megakaryocytic differentiation by the mitogen-activated protein kinase pathway. Molecular and Cellular Biology 17 (1997) 4991-5000
31. Rowley J.D. Letter: A new consistent chromosomal abnormality in chronic myelogenous leukaemia identified by quinacrine fluorescence and Giemsa staining. Nature 243 (1973) 290-293
32. Sausville E.A., Arbuck S.G., Messmann R., Headlee D., Bauer K.S., Lush R.M., Murgo A., Figg W.D., Lahusen T., Jaken S., Jing X., Roberge M., Fuse E., Kuwabara T., and Senderowicz A.M. Phase I trial of 72-hour continuous infusion UCN-01 in patients with refractory neoplasms. Journal of Clinical Oncology 19 (2001) 2319-2333
33. Sedlak J., Hunakova L., Duraj J., Chorvath B., and Novotny L. Effects of protein kinase C inhibitor, staurosporine derivative CGP 41 251, on cell cycle, DNA synthesis and drug uptake in neoplastic cell lines. Anti-cancer Drugs 6 (1995) 70-76
34. Sell S. Leukemia: stem cells, maturation arrest, and differentiation therapy. Stem Cell Reviews 1 (2005) 197-205
35. Stone R.M. Optimizing treatment of chronic myeloid leukemia: a rational approach. Oncologist 9 (2004) 259-270
36. Stone R.M., DeAngelo D.J., Klimek V., Galinsky I., Estey E., Nimer S.D., Grandin W., Lebwohl D., Wang Y., Cohen P., Fox E.A., Neuberg D., Clark J., Gilliland D.G., and Griffin J.D. Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412. Blood 105 (2005) 54-60
37. Tabilio A., Pelicci P.G., Vinci G., Mannoni P., Civin C.I., Vainchenker W., Testa U., Lipinski M., Rochant H., and Breton-Gorius J. Myeloid and megakaryocytic properties of K-562 cell lines. Cancer Research 43 (1983) 4569-4574