Overcoming resistance to imatinib by combining targeted agents

Molecular Cancer Therapeutics

Volumn 2, Issue 3, 2003, Pages 225-226

  Druker, Brian J ^a  

^a HOWARD HUGHES MEDICAL INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; BCR ABL PROTEIN; ENZYME INHIBITOR; FARNESYL TRANS TRANSFERASE; IMATINIB; LONAFARNIB; PIPERAZINE DERIVATIVE; PIPERIDINE DERIVATIVE; PYRIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; TRANSFERASE;

ACUTE GRANULOCYTIC LEUKEMIA; APOPTOSIS; CELL DIVISION; DRUG ANTAGONISM; DRUG EFFECT; DRUG RESISTANCE; GENETICS; HUMAN; METABOLISM; NOTE; PATHOLOGY;

ALKYL AND ARYL TRANSFERASES; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; APOPTOSIS; CELL DIVISION; DRUG RESISTANCE, NEOPLASM; ENZYME INHIBITORS; FARNESYLTRANSTRANSFERASE; FUSION PROTEINS, BCR-ABL; HUMANS; LEUKEMIA, MYELOCYTIC, ACUTE; PIPERAZINES; PIPERIDINES; PYRIDINES; PYRIMIDINES;

EID: 0642333844     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: None     Document Type: Note

References (19)

1. Deininger, M. W., Goldman, J. M., and Melo, J. V. The molecular biology of chronic myeloid leukemia. Blood, 96: 3343-3356, 2000.
2. Mauro, M. J., O'Dwyer, M., Heinrich, M. C., and Druker, B. J. STI571: a paradigm of new agents for cancer therapeutics. J. Clin. Oncol., 20: 325-334, 2002.
3. Druker, B. J., Sawyers, C. L., Kantarjian, H., Resta, D. J., Fernandes Reese, S., 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. 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. N., 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 myeloid leukemia in myeloid blast crisis: results of a phase II study. Blood, 99: 3530-3539, 2002.
5. Reichert, A., Heisterkamp, N., Daley, G. Q., and Groffen, J. Treatment of Bcr/Abl-positive acute lymphoblastic leukemia in P190 transgenic mice with the farnesyl transferase inhibitor SCH66336. Blood, 97: 1399-1403, 2001.
6. Peters, D. G., Hoover, R. R., Gerlach, M. J., Koh, E. Y., Zhang, H., Choe, K., Kirschmeier, P., Bishop, W. R., and Daley, G. Q. Activity of the farnesyl protein transferase inhibitor SCH66336 against BCR/ABL-induced murine leukemia and primary cells from patients with chronic myeloid leukemia. Blood, 97: 1404-1412, 2001.
7. Karp, J. E., Lancet, J. E., Kaufmann, S. H., End, D. W., Wright, J. J., Bol, K., Horak, I., Tidwell, M. L., Liesveld, J., Kottke, T. J., Ange, D., Buddharaju, L., Gojo, I., Highsmith, W. E., Belly, R. T., Hohl, R. J., Rybak, M. E., Thibault, A., and Rosenblatt, J. Clinical and biologic activity of the farnesyltransferase inhibitor R115777 in adults with refractory and relapsed acute leukemias: a phase 1 clinical-laboratory correlative trial. Blood, 97: 3361-3369, 2001.
8. Cortes, J. E., Albitar, M., Thomas, D., Giles, F., Kurzrock, R., Thibault, A., Rackoff, W., Koller, C., O'Brien, S., Garcia-Manero, G., Talpaz, M., and Kantarjian, H. Efficacy of the farnesyl transferase inhibitor, ZARNES-TRATM (R115777), in chronic myeloid leukemia and other other hematological malignancies. Blood, 101: 1692-1697, 2003.
9. Nakajima, A., Tauchi, T., Sumi, M., Bishop, W. R., and Ohyashiki, K. Efficacy of SCH66336, a farnesyl transferase inhibitor, in conjuction with imatinib against Bcr-Abl-positive cells. Mol. Cancer Ther., 2: 219-224, 2003.
10. 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.
11. Hochhaus, A., Kreil, S., Corbin, A. S., La Rosée, P., Müller, M. C., Lahaye, T., Hanfstein, B., Schoch, C., Cross, N. C. P., Berger, U., Gschaidmeier, H., Druker, B. J., and Hehlmann, R. Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy. Leukemia (Baltimore), 16: 2190-2196, 2002.
12. Shah, N. P., Nicoll, J. M., Nagar, B., Gorre, M. E., Paquette, R. L., Kuriyan, J., and Sawyers, C. L. 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 Cells (Cold Spring Harbor), 2: 117-125, 2002.
13. 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.
14. Corbin, A. S., La Rosée, P., Stoffregen, E., Druker, B. J., and Deininger, M. W. Several Bcr-Abl kinase domain mutants associated with imatinib mesylate resistance remain sensitive to imatinib. Blood, in press, 2003.
15. Larson, R. A. for the IRIS (International Randomized IFN vs STI571) Study Group. Imatinib (STI571, Gleevec) as initial therapy for patients with newly diagnosed Ph+ chronic myeloid leukemia (CML): results of a randomized Phase III study vs interferon-α + cytarabine. Blood, 100: 4a, 2002.
16. Hughes, T., Kaeda, J., Branford, S., Rudzki, Z., Hochhaus, A., Capdeville, R., Gathmann, I., Bolton, A. E., Goldman, J. M., and Radich, J. Molecular responses to imatinib (STI571) or interferon + Ara-C as initial therapy for CML: results in the IRIS study. Blood, 100: 93a, 2002.
17. Graham, S. M., Jorgensen, H. G., Allan, E., Pearson, C., Alcorn, M. J., Richmond, L., and Holyoake, T. L. Primitive, quiescent. Philadelphia-positive stem cells from patients with chronic myeloid leukemia are insensitive to STI571 in vitro. Blood, 99: 319-325, 2002.
18. Prendergast, G. C., and Du, W. Targeting farnesyltransferase: is Ras relevant? Drug Resist. Update, 2: 81-84, 1999.
19. Du, W., Lebowitz, P. F., and Prendergast, G. C. Cell growth inhibition by farnesyltransferase inhibitors is mediated by gain of geranylgeranylated RhoB. Mol. Cell. Biol., 19: 1831-1840, 1999.