Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl

Cancer Cell

Volumn 7, Issue 2, 2005, Pages 129-141

  Weisberg, Ellen ^a   Manley, Paul W ^b   Breitenstein, Werner ^b   Brüggen, Josef ^b   Cowan Jacob, Sandra W ^b   Ray, Arghya ^a   Huntly, Brian ^c   Fabbro, Doriano ^b   Fendrich, Gabriele ^b   Hall Meyers, Elizabeth ^a   Kung, Andrew L ^a,d   Mestan, Jürgen ^b   Daley, George Q ^d   Callahan, Linda ^a   Catley, Laurie ^a   Cavazza, Cara ^a   Mohammed, Azam ^d   Neuberg, Donna ^a   Wright, Renee D ^c   Gilliland, D Gary ^c   Griffin, James D ^a   more..

^a DANA FARBER CANCER INSTITUTE   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

^c BRIGHAM AND WOMEN S HOSPITAL   (United States)

^d BOSTON CHILDREN S HOSPITAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BCR ABL PROTEIN; IMATINIB; NILOTINIB; PROTEIN TYROSINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ACUTE LYMPHOBLASTIC LEUKEMIA; ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER SURVIVAL; CHRONIC MYELOID LEUKEMIA; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DETERMINATION; DRUG POTENCY; DRUG STRUCTURE; FEMALE; HEMATOPOIETIC CELL; IC 50; LEUKEMOGENESIS; MOUSE; NONHUMAN; PHILADELPHIA CHROMOSOME POSITIVE CELL; PRIORITY JOURNAL; SCID MOUSE; SURVIVAL RATE;

ANIMALIA;

EID: 13844251975     PISSN: 15356108     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ccr.2005.01.007     Document Type: Article

References (64)

1. S.A. Armstrong, A.L. Kung, M.E. Mabon, L.B. Silverman, R.W. Stam, M.L. Den Boer, R. Pieters, J.H. Kersey, S.E. Sallan, and J.A. Fletcher Validation of a therapeutic target identified by gene expression based classification Cancer Cell 3 2003 173 183
2. M. Azam, R.R. Latek, and G.Q. Daley Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL Cell 112 2003 831 843
3. C. Barthe, P. Cony-Makhoul, J.V. Melo, and J.R. Mahon Roots of clinical resistance to STI-571 cancer therapy Science 293 2001 2163
4. C. Barthe, M.J. Gharbi, V. Lagarde, C. Chollet, P. Cony-Makhoul, J. Reiffers, J.M. Goldman, J.V. Melo, and F.X. Mahon Mutation in the ATP-binding site of BCR-ABL in a patient with chronic myeloid leukaemia with increasing resistance to STI571 Br. J. Haematol. 119 2002 109 111
5. A. Bedi, B.A. Zehnbauer, J.P. Barber, S.J. Sharkis, and R.J. Jones Inhibition of apoptosis by BCR-ABL in chronic myeloid leukemia Blood 83 1994 2038 2044
6. S. Branford, T.P. Hughes, and Z. Rudzki Monitoring chronic myeloid leukaemia therapy by real-time quantitative PCR in blood is a reliable alternative to bone marrow cytogenetics Br. J. Haematol. 107 1999 587 599
7. S. Branford, Z. Rudzki, S. Walsh, A. Grigg, C. Arthur, K. Taylor, R. Herrmann, K.P. Lynch, and T.P. Hughes 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 (STI571) resistance Blood 99 2002 3472 3475
8. E. Buchdunger, J. Zimmermann, H. Mett, T. Meyer, M. Muller, B.J. Druker, and N.B. Lydon Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative Cancer Res. 56 1996 100 104
9. E. Buchdunger, C.L. Cioffi, N. Law, D. Stover, S. Ohno-Jones, B.J. Druker, and N.B. Lydon Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors J. Pharmacol. Exp. Ther. 295 2000 139 145
10. E. Buchdunger, A. Matter, and B.J. Druker Bcr-Abl inhibition as a modality of CML therapeutics Biochim. Biophys. Acta 1551 2001 M11 M18
11. L.J. Campbell, C. Patsouris, K.C. Rayeroux, K. Somana, E.H. Januszewicz, and J. Szer BCR-ABL amplification in chronic myelocytic leukemia blast crisis following imatinib mesylate administration Cancer Genet. Cytogenet. 139 2002 30 33
12. M. Carroll, M.H. Tomasson, G.F. Barker, T.R. Golub, and D.G. Gilliland The Tel platelet-derived growth factor receptor (PDGF-beta-R) fusion in chronic myelomonocytic leukemia is a transforming protein that self-associates and activates PDGF-beta-R kinase-dependent signaling pathways Proc. Natl. Acad. Sci. USA 93 1996 14845 14850
13. J. Cools, E.H. Stover, C.L. Boulton, J. Gotlib, R.D. Legare, S.M. Amaral, D.P. Curley, N. Duclos, R. Rowan, and J.L. Kutok PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRalpha-induced myeloproliferative disease Cancer Cell 3 2003 459 469
14. A.S. Corbin, P. La Rosee, E.P. Stoffregen, B.J. Druker, and M.W. Deininger Several Bcr-Abl kinase domain mutants associated with imatinib mesylate resistance remain sensitive to imatinib Blood 101 2003 4611 4614
15. S.W. Cowan-Jacob, V. Guez, J.D. Griffin, D. Fabbro, G. Fendrich, P. Furet, J. Liebetanz, J. Mestan, and P.W. Manley Bcr-Abl kinase mutations and drug resistance to imatinib (STI571) in chronic myelogenous leukemia Mini Rev. Med. Chem. 4 2004 285 299
16. S. Danhauser-Riedl, M. Warmuth, B.J. Druker, B. Emmerich, and M. Hallek Activation of Src kinases p53/56lyn and p59hck by p210bcr/abl in myeloid cells Cancer Res. 56 1996 3589 3596
17. M.W.N. Deininger, J.M. Goldman, and J.V. Melo The molecular biology of chronic myeloid leukemia Blood 96 2000 3343 3356
18. G.D. Demetri, M. von Mehren, C.D. Blanke, A.D. Van den Abbeele, B. Eisenberg, P.J. Roberts, M.C. Heinrich, D.A. Tuveson, S. Singer, and M. Janicek Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors N. Engl. J. Med. 347 2002 472 480
19. B.J. Druker, S. Tamura, E. Buchdunger, S. Ohno, G.M. Segal, S. Fanning, J. Zimmermann, and N.B. Lydon Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells Nat. Med. 2 1996 561 566
20. M.Y. Gordon, C.R. Dowding, G.P. Riley, J.M. Goldman, and M.F. Greaves Altered adhesive interactions with marrow stroma of heamotopoietic progenitor cells in chronic myeloid leukaemia Nature 328 1987 342 344
21. M.E. Gorre, M. Mohammed, K. Ellwood, N. Hsu, R. Paquette, P.N. Rao, and C.L. Sawyers Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification Science 293 2001 876 880
22. M.E. Gorre, K. Ellwood-Yen, G. Chiosis, N. Rosen, and C.L. Sawyers 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 2002 3041 3044
23. A. Hochhaus, and P. La Rosee Imatinib therapy in chronic myelogenous leukemia: Strategies to avoid and overcome resistance Leukemia 18 2004 1321 1331
24. A. Hochhaus, S. Kreil, A. Corbin, P. La Rosee, T. Lahaye, U. Berger, N.C. Cross, W. Linkesch, B.J. Druker, and R. Hehlmann Roots of clinical resistance to STI-571 cancer therapy Science 293 2001 2163
25. A. Hochhaus, S. Kreil, A.S. Corbin, P. La Rosee, M.C. Muller, T. Lahaye, B. Hanfstein, C. Schoch, N.C. Cross, and U. Berger Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy Leukemia 16 2002 2190 2196
26. W.K. Hofmann, L.C. Jones, N.A. Lemp, S. de Vos, H. Gschaidmeier, D. Hoelzer, O.G. Ottmann, and H.P. Koeffler Ph(+) acute lymphoblastic leukemia resistant to the tyrosine kinase inhibitor STI571 has a unique BCR-ABL gene mutation Blood 99 2002 1860 1862
27. R.R. Hoover, F.X. Mahon, J.V. Melo, and G.Q. Daley Overcoming STI571 resistance with the farnesyl transferase inhibitor SCH66336 Blood 100 2002 1068 1071
28. Y. Hu, Y. Liu, S. Pelletier, E. Buchdunger, M. Warmuth, D. Fabbro, M. Hallek, R.A. Van Etten, and S. Li Requirement of Src kinases Lyn, Hck and Fgr for BCR-ABL1-induced B-lymphoblastic leukemia but not chronic myeloid leukemia Nat. Genet. 36 2004 453 461
29. H.M. Kantarjian, and M. Talpaz Definition of the accelerated phase of chronic myelogenous leukemia J. Clin. Oncol. 6 1988 180 182
30. L.M. Kelly, J.C. Yu, C.L. Boulton, M. Apatira, J. Li, C.M. Sullivan, I. Williams, S.M. Amaral, D.P. Curley, and N. Duclos CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML) Cancer Cell 1 2002 421 432
31. G.W. Krystal Mechanisms of resistance to imatinib (STI571) and prospects for combination with conventional chmeotherapeutic agents Drug Resist. Updat. 4 2001 16 21
32. A. Klejman, L. Rushen, A. Morrione, A. Slupianek, and T. Skorski Phosphatidylinositol-3-kinase inhibitors enhance the anti-leukemia effect of STI571 Oncogene 21 2002 5868 5876
33. P. La Rosee, K. Johnson, M.E. O'Dwyer, and B.J. Druker In vitro studies of the combination of imatinib mesylate (Gleevec) and arsenic trioxide (Trisenox) in chronic myelogenous leukemia Exp. Hematol. 30 2002 729 737
34. P. le Coutre, E. Tassi, M. Varella-Garcia, R. Barni, L. Mologni, G. Cabrita, E. Marchesi, R. Supino, and C. Gambacorti-Passerini Induction of resistance to the Abelson inhibitor STI571 in human leukemic cells through gene amplification Blood 95 2000 1758 1766
35. Q. Liu, J. Schwaller, J. Kutok, D. Cain, J.C. Aster, I.R. Williams, and D.G. Gilliland Signal transduction and transforming properties of the TEL-TRKC fusions associated with t(12;15)(p13;q25) in congenital fibrosarcoma and acute myelogenous leukemia EMBO J. 19 2000 1827 1838
36. T.G. Lugo, A.M. Pendergast, A.J. Muller, and O.N. Witte Tyrosine kinase activitiy and transformation potency of BCR-ABL oncogene products Science 247 1990 1079 1082
37. F.X. Mahon, M.V. Deininger, B. Schultheis, J. Chabrol Reiffers, J.M. Goldman, and J.V. Melo Selection and characterization of BCR-ABL positive cell lines with differential sensitivity to the tyrosine kinase inhibitor STI571: Diverse mechanisms of resistance Blood 96 2000 1070 1079
38. P.W. Manley, W. Breitenstein, J. Bruggen, S.W. Cowan-Jacob, P. Furet, J. Mestan, and T. Meyer Urea-derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases Bioorg. Med. Chem. Lett. 14 2004 5793 5797
39. J.V. Melo, H. Myint, D.A. Galton, and J.M. Goldman P190BCR-ABL chronic myeloid leukaemia: The missing link with chronic myelomonocytic leukaemia? Leukemia 8 1994 208 211
40. M.G. Mohi, C. Boulton, T.L. Gu, D.W. Sternberg, D. Neuberg, J.D. Griffin, D.G. Gilliland, and B.G. Neel Combination of rapamycin and protein tyrosine kinase (PTK) inhibitors for the treatment of leukemias caused by oncogenic PTKs Proc. Natl. Acad. Sci. USA 101 2004 3130 3135
41. F. Morel, M.J. Bris, A. Herry, G.L. Calvez, V. Marion, J.F. Abgrall, C. Berthou, and M.D. Braekeleer Double minutes containing amplified bcr-abl fusion gene in a case of chronic myeloid leukemia treated by imatinib Eur. J. Haematol. 70 2003 235 239
42. B.M. Mow, J. Chandra, P.A. Svingen, C.G. Hallgren, E. Weisberg, T.J. Kottke, V.L. Narayanan, M.R. Litzow, J.D. Griffin, and E.A. Sausville Effects of the Bcr-Abl kinase inhibitors STI571 and adaphostin (NSC 680410) on chronic myelogenous leukemia cells in vitro Blood 99 2002 664 671
43. B. Nagar, O. Hantschel, M. Young, K. Scheffzek, D. Veach, W. Bornmann, B. Clarkson, G. Superti-Furga, and J. Kuriyan Structural basis for the autoinhibition of c-Abl tyrosine kinase Cell 112 2003 859 871
44. A. Nakajima, T. Tauchi, M. Sumi, W.R. Bishop, and K. Ohyashiki Efficacy of SCH66336, farnesyl transferase inhibitor, in conjuction with imatinib against BCR-ABL-positive cells Mol. Cancer Ther. 2 2003 219 224
45. R. Nimmanapalli, E. O'Bryan, M. Huang, P. Bali, P.K. Burnette, T. Loughran, J. Tepperberg, R. Jove, and K. Bhalla Molecular characterization and sensitivity of STI-571 (imatinib mesylate, Gleevec)-resistant, Bcr-Abl-positive, human acute leukemia cells to SRC kinase inhibitor PD180970 and 17-allylamino-17-demethoxygeldanamycin Cancer Res. 62 2002 5761 5769
46. S.G. O'Brien, F. Guilhot, R.A. Larson, I. Gathmann, M. Baccarani, F. Cervantes, J.J. Cornelissen, T. Fischer, A. Hochhaus, and T. Hughes Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia N. Engl. J. Med. 348 2003 994 1004
47. M.E. O'Dwyer, M.J. Mauro, G. Kurilik, M. Mori, S. Balleisen, S. Olson, E. Magenis, R. Capdeville, and B.J. Druker The impact of clonal evolution on response to imatinib mesylate (STI571) in accelerated phase CML Blood 100 2002 1628 1633
48. T. O'Hare, R. Pollock, E.P. Stoffregan, J.A. Keats, O.M. Abdullah, E.M. Moseson, V.M. Rivera, H. Tang, C.A. Metcalf III, and R.S. Bohacek Inhibition of native and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: Implications for CML Blood 104 2004 2532 2539
49. O.G. Ottmann, B.J. Druker, C.L. Sawyers, J.M. Goldman, J. Reiffers, R.T. Silver, S. Tura, T. Fischer, M.W. Deininger, and C.A. Schiffer A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias Blood 100 2002 1965 1971
50. L. Puil, J. Liu, G. Gish, G. Mbamalu, D. Bowtell, P.G. Pelicci, R. Arlinghaus, and T. Pawson Bcr-Abl oncoproteins bind directly to activators of the Ras signaling pathway EMBO J. 13 1994 746 773
51. F. Ravandi, J. Cortes, M. Albitar, R. Arlinghaus, J. Qiang Guo, M. Talpaz, and H.M. Kantarjian Chronic myelogenous leukaemia with p185BCR-ABL expression: Characteristics and clinical significance Br. J. Haematol. 107 1999 581 586
52. C. Ricci, B. Scappini, V. Divoky, S. Gatto, F. Onida, S. Verstovsek, H.M. Kantarjian, and M. Beran Mutation in the ATP-binding pocket of the ABL kinase domain in an STI571-resistant BCR-ABL-positive cell line Cancer Res. 62 2002 5995 5998
53. C. Roche-Lestienne, V. Soenen-Cornu, N. Grardel-Duflos, J.L. Lai, N. Philippe, T. Facon, P. Fenaux, and C. Preudhomme 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 2002 1014 1018
54. C.L. Sawyers, A. Hochhaus, E. Feldman, J.M. Goldman, C.B. Miller, O.G. Ottmann, C.A. Schiffer, M. Talpaz, F. Guilhot, and M.W. Deininger Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: Results of a phase II study Blood 99 2002 3530 3539
55. T. Schindler, W. Bornmann, P. Pellicena, T.W. Miller, B. Clarkson, and J. Kuriyan Structural mechanism of STI-571 inhibition of abelson tyrosine kinase Science 289 2000 1938 1942
56. J. Schwaller, J. Frantsve, J. Aster, I.R. Williams, M.H. Tomasson, T.S. Ross, P. Peeters, L. Van Rompaey, R.A. Van Etten, and R. Ilaria Jr. Transformation of hematopoietic cell lines to growth-factor independence and induction of a fatal myelo- and lymphoproliferative disease in mice by retrovirally transduced TEL/JAK2 fusion genes EMBO J. 17 1998 5321 5333
57. N.P. Shah, J.M. Nicoll, B. Nagar, M.E. Gorre, R.L. Paquette, J. Kuriyan, and C.L. Sawyers 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 2002 117 125
58. N.P. Shah, C. Tran, F.Y. Lee, P. Chen, D. Norris, and C.L. Sawyers Overriding imatinib resistance with a novel ABL kinase inhibitor Science 305 2004 399 401
59. X. Sun, J.E. Layton, A. Elefanty, and G.J. Lieschke Comparison of effects of the tyrosine kinase inhibitors AG957, AG490, and STI571 on BCR-ABL-expressing cells, demonstrating synergy between AG490 and STI571 Blood 97 2001 2008 2015
60. J.T. Thiesing, S. Ohno-Jones, K.S. Kolibaba, and B.J. Druker Efficacy of STI571, an abl tyrosine kinase inhibitor, in conjunction with other antileukemic agents against bcr-abl-positive cells Blood 96 2000 3195 3199
61. A.J. Tipping, F.X. Mahon, G. Zafirides, V. Lagarde, J.M. Goldman, and J.V. Melo Drug responses of imatinib mesylate-resistant cells: Synergism of imatinib with other chemotherapeutic drugs Leukemia 16 2002 2349 2357
62. N. von Bubnoff, F. Schneller, C. Peschel, and J. Duyster BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: A prospective study Lancet 359 2002 487 491
63. M. Warmuth, N. Simon, O. Mitina, R. Mathes, D. Fabbro, P.W. Manley, E. Buchdunger, K. Forster, I. Moarefi, and M. Hallek Dual-specific Src and Abl kinase inhibitors, PP1 and CGP76030, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Abl kinases Blood 101 2003 664 672
64. E. Weisberg, and J.D. Griffin Mechanism of resistance to the ABL tyrosine kinase inhibitor STI571 in BCR-ABL-transformed hematopoietic cell lines Blood 95 2000 3498 3505