Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571)

Cancer Research

Volumn 62, Issue 24, 2002, Pages 7149-7153

  La Rosée, Paul ^a,b   Corbin, Amie S ^a   Stoffregen, Eric P ^a   Deininger, Michael W ^a   Druker, Brian J ^a  

^a OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

^b UNIVERSITY OF HEIDELBERG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

6 (2,6 DICHLOROPHENYL) 2 (4 FLUORO 3 METHYLANILINO) 8 METHYL 8H PYRIDO[2,3 D]PYRIMIDIN 7 ONE; BCR ABL PROTEIN; IMATINIB; ISOPROTEIN; PROTEIN KINASE INHIBITOR; PYRIDO[2,3 D]PYRIMIDINE DERIVATIVE;

ADVANCED CANCER; ANIMAL CELL; APOPTOSIS; ARTICLE; CHRONIC MYELOID LEUKEMIA; CONTROLLED STUDY; DRUG MECHANISM; DRUG TARGETING; ENZYME INHIBITION; GENE MUTATION; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; SITE DIRECTED MUTAGENESIS; TUMOR CELL LINE;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE; DRUG RESISTANCE, NEOPLASM; ENZYME INHIBITORS; HEMATOPOIETIC STEM CELLS; HUMANS; LEUKEMIA, MYELOID, CHRONIC; MICE; MUTAGENESIS, SITE-DIRECTED; PIPERAZINES; PROTEIN ISOFORMS; PROTEIN STRUCTURE, TERTIARY; PROTEIN-TYROSINE KINASES; PYRIDONES; PYRIMIDINES; TRANSFECTION;

EID: 0037115644     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (36)

1. Deininger, M. W., Goldman, J. M., and Melo, J. V. The molecular biology of chronic myeloid leukemia. Blood, 96: 3343-3356, 2000.
2. Druker, B. J., Talpaz, M., Resta, D. J., Peng, B., Buchdunger, E., Ford, J. M., Lydon, N. B., Kantarjian, H., Capdeville, R., Ohno-Jones, S., and Sawyers, C. L. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia, N. Engl. J. Med., 344: 1031-1037, 2001.
3. Druker, B. J., Sawyers, C. L., Kantarjian, H., Resta, D. J., Reese, S. F., Ford, J. M., Capdeville, R., and Talpaz, M. Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome. N. Engl. J. Med., 344: 1038-1042, 2001.
4. Druker, B. J., for the IRIS (International Randomized IFN versus STI571) Study Group. STI571 (Gleevec/Glivec, imatinib) versus interferon (IFN) + cytarabine as initial therapy for patients with CML: Results of a randomized study. Proc. Am. Soc. Clin. Oncol. 21: 1a, 2002.
5. Kantarjian, H., Sawyers, C., Hochhaus, A., Guilhot, F., Schiffer, C., Gambacorti-Passerini, C., Niederwieser, D., Resta, D., Capdeville, R., Zoellner, U., Talpaz, M., and Druker, B. Hematologic and cytogenetic responses to imatinib mesylate in chronic myelogenous leukemia. N. Engl. J Med., 346: 645-652, 2002.
6. Sawyers, C. L., Hochhaus, A., Feldman, E., Goldman, J. M., Miller, C. B., Ottmann, O. G., Schiffer, C. A., Talpaz, M., Guilhot, F., Deininger, M. W., Fischer, T., O'Brien, S. G., Stone, R. M., Gambacorti-Passerini, C. B., Russell, N. H., Reiffers, J. J., Shea, T. C., Chapuis, B., Coutre, S., Tura, S., Morra, E., Larson, R. A., Saven, A., Peschel, C., Gratwohl, A., Mandelli, F., Ben Am. M., Gathmann, I., Capdeville, R., Paquette, R. L., and Druker, B. J. Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: Results of a Phase II study. Blood, 99: 3530-3539, 2002.
7. Corbin, A. S., Toledo, L. M., Lydon, N. B., Buchdunger, E., Kuriyan, J., and Druker, B. J. Analysis of the structural basis of specificity of inhibition of the Abl kinase by STI571. Blood 96: 470a, 2000.
8. Corbin, A. S., Buchdunger, E., Pascal, F., and Druker, B. J. Analysis of the structural basis of specificity of inhibition of the Abl kinase by STI571. J. Biol. Chem., 277: 32214-32219, 2002.
9. Nagar, B., Bornmann, W. G., Pellicena, P., Schindler, T., Veach, D. R., Miller, W. T., Clarkson, B., and Kuriyan, J. Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571). Cancer Res., 62: 4236-4243, 2002.
10. Schindler, T., Bornmann, W., Pellicena, P., Miller, W. T., Clarkson, B., and Kuriyan, J. Structural mechanism for STI-571 inhibition of abelson tyrosine kinase. Science (Wash. DC), 289: 1938-1942, 2000.
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 (Wash. DC), 293: 876-880, 2001.
12. Kreil, S., Muller, M. C., Lahaye, T., La Rosée, P., Corbin, A. S., Schoch, C., Cross, N. C. P., Berger, U., Rieder, H., Druker, B. J., Gschaidmeier, H., Hehlmann, R., and Hochhaus, A. Molecular and chromosomal mechanisms of resistance in CML patients after STI571 (Glivec) therapy. Blood, 98: 435a, 2001.
13. Hochhaus, A., Kreil, S., Corbin, A., La Rosee, P., Lahaye, T., Berger, U., Cross, N. C., Linkesch, W., Druker, B. J., and Hehlmann, R. Roots of clinical resistance to STI-571 cancer therapy. Science (Wash. DC), 293: 2163, 2001.
14. Barthe, C., Cony-Makhoul, P., Melo, J. V., and Mahon, J. R. Roots of clinical resistance to STI-571 cancer therapy, Science (Wash. DC), 293: 2163, 2001.
15. von Bubnoff, N., Schneller, F., Peschel, C., and Duyster, J. BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: A prospective study. Lancet, 359: 487-491, 2002.
16. Branford, S., Rudzki, Z., Walsh, S., Grigg, A., Arthur, C., Taylor, K., Herrmann, R., Lynch, K. P., and Hughes, T. P. High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (ST1571) resistance. Blood, 99: 3472-3475, 2002.
17. Roche-Lestienne, C., Soenen-Comu, V., Grardel-Duflos, N., Lai, J. L., Philippe, N., Facon, T., Fenaux, P., and Preudhomme, C. Several types of mutations of the Abl gene can be found in chronic myeloid leukemia patients resistant to STI571, and they can pre-exist to the onset of treatment. Blood, 100: 1014-1018, 2002.
18. Hofmann, W. K., Jones, L. C., Lemp, N. A., de Vos, S., Gschaidmeier, H., Hoelzer, D., Ottmann, O. G., and Koeffler, H. P. Ph(+) acute lymphoblastic leukemia resistant to the tyrosine kinase inhibitor STI571 has a unique BCR-ABL gene mutation. Blood, 99: 1860-1862, 2002.
19. Roumiantsev, S., Shah, N. P., Gorre, M. E., Nicoll, J., Brasher, B. B., Sawyers, C. L., and van Etten, R. A. Clinical resistance to the kinase inhibitor STI-571 in chronic myeloid leukemia by mutation of Tyr-253 in the Abl kinase domain P-loop. Proc. Natl. Acad. Sci. USA, 99: 10700-10705, 2002.
20. Shah, N., Nicoll, J., Nagar, B., Gorre, M., Paquette, R., Kuriyan, J., and Sawyers, C. Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell. 2: 117-125, 2002.
21. Kraker, A. J., Hartl, B. G., Amar, A. M., Barvian, M. R., Showalter, H. D., and Moore, C. W. Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. Biochem. Pharmacol., 60: 885-898, 2000.
22. Dorsey, J. F., Jove, R., Kraker, A. J., and Wu, J. The pyrido[2, 3-d] pyrimidine derivative PD180970 inhibits p210Bcr-Abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res., 60: 3127-3131, 2000.
23. Wisniewski, D., Lambek, C. L., Liu, C., Strife, A., Veach, D. R., Nagar, B., Young, M. A., Schindler, T., Bommann, W. G., Bertino, J. R., Kuriyan, J., and Clarkson, B. Characterization of potent inhibitors of the Bcr-Abl and the c-kit receptor tyrosine kinases. Cancer Res., 62: 4244-4255, 2002.
24. Pear, W. S., Nolan, G. P., Scott, M. L., and Baltimore, D. Production of high-titer helper-free retroviruses by transient transfection. Proc. Natl. Acad. Sci. USA, 90: 8392-8396, 1993.
25. Mosmann, T. Rapid colorimetric assay for cellular growth and survival: Application to proliferation and cytotoxicity assays. J. Immunol. Methods, 65: 55-63, 1983.
26. Dorey, K., Engen, J. R., Kretzschmar, J., Wilm, M., Neubauer, G., Schindler, T., and Superti-Furga, G. Phosphorylation and structure-based functional studies reveal a positive and a negative role for the activation loop of the c-Abl tyrosine kinase. Oncogene, 20: 8075-8084, 2001.
27. Gorre, M. E., Ellwood-Yen, K., Chiosis, G., Rosen, N., and Sawyers, C. L. BCR-ABL point mutants isolated from patients with imatinib mesylate-resistant chronic myeloid leukemia remain sensitive to inhibitors of the BCR-ABL chaperone heat shock protein 90. Blood. 100: 3041-3044, 2002.
28. Nimmanapalli, R., O'Bryan, E., and Bhalla, K. Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts. Cancer Res., 61: 1799-1804, 2001.
29. Hoover, R. R., Mahon, F. X., Melo, J. V., and Daley, G. Q. Overcoming STI571 resistance with the farnesyl transferase inhibitor SCH66336. Blood, 100: 1068-1071, 2002.
30. Yu, C., Krystal, G., Varticovksi, L., McKinstry, R., Rahmani, M., Dent, P., and Grant, S. Pharmacologic mitogen-activated protein/extracellu]ar signal-regulated kinase kinase/mitogen-activated protein kinase inhibitors interact synergistically with STI571 to induce apoptosis in Bcr/Abl-expressing human leukemia cells. Cancer Res., 62: 188-199, 2002.
31. Klejman, A., Rushen, L., Morrione, A., Slupianek, A., and Skorski, T. Phosphatidylinositol-3 kinase inhibitors enhance the anti-leukemia effect of STI571. Oncogene, 21: 5868-5876, 2002.
32. Ma, Y., Zeng, S., Metcalfe, D. D., Akin, C., Dimitrijevic, S., Butterfield, J. H., McMahon, G., and Longley, B. J. The c-KIT mutation causing human mastocytosis is resistant to STI571 and other KIT kinase inhibitors; kinases with enzymatic site mutations show different inhibitor sensitivity profiles than wild-type kinases and those with regulatory-type mutations. Blood, 99: 1741-1744, 2002.
33. Heinrich, M. C., Blanke, C. D., Druker, B. J., and Corless, C. L. Inhibition of KIT tyrosine kinase activity: A novel molecular approach to the treatment of KIT-positive malignancies. J. Clin. Oncol., 20: 1692-1703, 2002.
34. Demetri, G. D., von Mehren, M., Blanke, C. D., Van den Abbeele, A. D., Eisenberg, B., Roberts, P. J., Heinrich, M. C., Tuveson, D. A., Singer, S., Janicek, M., Fletcher, J. A., Silverman, S. G., Silberman, S. L., Capdeville, R., Kiese, B., Peng, B., Dimitrijevic, S., Druker, B. J., Corless, C., Fletcher, C. D., and Joensuu, H. Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. N. Engl. J Med., 347: 472-480, 2002.
35. Danhauser-Riedl, S., Warmuth, M., Druker, B. J., Emmerich, B., and Hallek, M. Activation of Src kinases p53/56lyn and p59hck by p210bcr/abl in myeloid cells. Cancer Res., 56: 3589-3596, 1996.
36. Kraker, A. J., Roberts, B. J., Vincent, P. W., Patmore, S. J., and Elliott, W. L. In vivo antitumor activity of selective c-src tyrosine kinase (TK) inhibitors. Proc. Am. Assoc. Cancer Res., 40: 808, 1999.