New resistance mechanisms for small molecule kinase inhibitors of Abl kinase

Drug Discovery Today: Technologies

Volumn 11, Issue 1, 2014, Pages 5-10

  Modugno, Michele ^a  

^a NERVIANO MEDICAL SCIENCES   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

ABELSON KINASE INHIBITOR; BOSUTINIB; DANUSERTIB; DASATINIB; IMATINIB; NILOTINIB; PONATINIB; PROTEIN TYROSINE KINASE INHIBITOR; REBASTINIB; TOZASERTIB; UNCLASSIFIED DRUG; ABELSON KINASE; PROTEIN KINASE INHIBITOR;

ARTICLE; BINDING AFFINITY; CANCER RESISTANCE; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL (TOPIC); CRYSTAL STRUCTURE; DRUG DESIGN; DRUG SAFETY; DRUG STRUCTURE; ENZYME ACTIVE SITE; GENE MUTATION; HUMAN; PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); RANDOMIZED CONTROLLED TRIAL (TOPIC); WILD TYPE; ANTAGONISTS AND INHIBITORS; DRUG DEVELOPMENT; DRUG RESISTANCE; GENETICS;

DRUG DISCOVERY; DRUG RESISTANCE, NEOPLASM; HUMANS; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-ABL;

EID: 84899967194     PISSN: None     EISSN: 17406749     Source Type: Journal    
DOI: 10.1016/j.ddtec.2013.12.001     Document Type: Review

References (38)

1. M.W. Deininger, J.M. Goldman, and J.V. Melo The molecular biology of chronic myeloid leukemia Blood 96 2000 3343 3356
2. D. Cilloni, and G. Saglio Molecular pathways: BCR-ABL Clin Cancer Res 18 2012 930 937
3. A. Hochhaus, S.G. O'Brien, F. Guilhot, B.J. Druker, S. Branford, and L. Foroni et al. Six-year follow-up of patients receiving imatinib for the first-line treatment of chronic myeloid leukemia Leukemia 23 2009 1054 1061
4. J.F. Apperley Part I: mechanisms of resistance to imatinib in chronic myeloid leukaemia Lancet Oncol 8 2007 1018 1029
5. S. Soverini Philadelphia-positive patients who already harbor imatinib-resistant Bcr-Abl kinase domain mutations have a higher likelihood of developing additional mutations associated with resistance to second- or third-line tyrosine kinase inhibitors Blood 114 2009 2168 2171
6. J. Eswaran, and S. Knapp Insights into protein kinase regulation and inhibition by large scale structural comparison Biochim Biophys Acta 1804 2010 429 432
7. Y. Liu, and N.S. Gray Rational design of inhibitors that bind to inactive kinase conformations Nat Chem Biol 2 2006 358 364
8. E. Weisberg, P.W. Manley, W. Breitenstein, J. Brüggen, S.W. Cowan-Jacob, and A. Ray et al. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl Cancer Cell 7 2005 129 141
9. J.Y. Blay, and M. von Mehren Nilotinib: a novel, selective tyrosine kinase inhibitor Semin Oncol 38 Suppl 1 2011 S3 S9
10. N.P. Shah, C. Tran, F.Y. Lee, P. Chen, D. Norris, and C.L. Sawyers et al. Overriding imatinib resistance with a novel ABL kinase inhibitor Science 305 2004 399 401
11. H. Kantarjian, N.P. Shah, A. Hochhaus, J. Cortes, S. Shah, and M. Ayala et al. Dasatinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia N Engl J Med 362 2010 2260 2270
12. F.P. Santos, and J. Cortes Dasatinib for the treatment of Philadelphia chromosome-positive leukemias Expert Opin Pharmacother 13 2012 2381 2395
13. G. Saglio, D.W. Kim, S. Issaragrisil, P. le Coutre, G. Etienne, and C. Lobo et al. Nilotinib versus imatinib for newly diagnosed chronic myeloid leukemia N Engl J Med 362 2010 2251 2259
14. J. Cortes Bosutinib in the treatment of chronic myelogenous leukemia Clin Adv Hematol Oncol 10 2012 736 737
15. F. Zuccotto, E. Ardini, E. Casale, and M. Angiolini Through the 'gatekeeper door': exploiting the active kinase conformation J Med Chem 53 2010 2681 2694
16. X.Y. Lu, Q. Cai, and K. Ding Recent developments in the third generation inhibitors of Bcr-Abl for overriding T315I mutation Curr Med Chem 18 2011 2146 2157
17. F.J. Giles, J. Cortes, D. Jones, D. Bergstrom, H. Kantarjian, and S.J. Freedman MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation Blood 109 2007 500 502
18. M. Modugno, E. Casale, C. Soncini, P. Rosettani, R. Colombo, and R. Lupi et al. Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358 Cancer Res 67 2007 7987 7990
19. A. Gontarewicz, and T.H. Brümmendorf Danusertib (formerly PHA-739358) - a novel combined pan-Aurora kinases and third generation Bcr-Abl tyrosine kinase inhibitor Recent Results Cancer Res 184 2010 199 214
20. A. Gontarewicz, S. Balabanov, G. Keller, R. Colombo, A. Graziano, and E. Pesenti et al. Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I Blood 111 2008 4355 4364
21. M. Kollareddy, D. Zheleva, P. Dzubak, P.S. Brahmkshatriya, M. Lepsik, and M. Hajduch Aurora kinase inhibitors: progress towards the clinic Invest New Drugs 30 2012 2411 2432
22. N.J. Donato, D. Fang, H. Sun, D. Giannola, L.F. Peterson, and M. Talpaz Targets and effectors of the cellular response to aurora kinase inhibitor MK-0457 (VX-680) in imatinib sensitive and resistant chronic myelogenous leukemia Biochem Pharmacol 79 2010 688 697
23. T. O'Hare, W.C. Shakespeare, X. Zhu, C.A. Eide, V.M. Rivera, and F. Wang et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance Cancer Cell 16 2009 401 412
24. T. Zhou, L. Commodore, W.S. Huang, Y. Wang, M. Thomas, and J. Keats et al. Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance Chem Biol Drug Des 77 2011 1 11
25. X. Deng, S.M. Lim, J. Zhang, and N.S. Gray Broad spectrum alkynyl inhibitors of T315I Bcr-Abl Bioorg Med Chem Lett 20 2010 4196 4200
26. J.E. Cortes, H. Kantarjian, N.P. Shah, D. Bixby, M.J. Mauro, and I. Flinn et al. Ponatinib in refractory philadelphia chromosome-positive leukemias N Engl J Med 367 2012 2075 2088
27. V. De Falco, P. Buonocore, M. Muthu, L. Torregrossa, F. Basolo, and M. Billaud et al. Ponatinib (AP24534) is a novel potent inhibitor of oncogenic ret mutants associated with thyroid cancer J Clin Endocrinol Metab 98 2013 E811 E819
28. J.M. Gozgit, M.J. Wong, S. Wardwell, J.W. Tyner, M.M. Loriaux, and Q.K. Mohemmad et al. Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies Mol Cancer Ther 10 2011 1028 1035
29. E. Zirm et al. Ponatinib may overcome resistance of FLT3-ITD harbouring additional point mutations, notably the previously refractory F691I mutation Br J Haematol 157 2012 483 492
30. C.C. Smith et al. Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD Blood 121 2013 3165 3171
31. K.V. Gleixner et al. Synergistic growth-inhibitory effects of ponatinib and midostaurin (PKC412) on neoplastic mast cells carrying KIT D816V Haematologica 98 2013 1450 1457
32. E. Lierman, S. Smits, J. Cools, B. Dewaele, M. Debiec-Rychter, and P. Vandenberghe Ponatinib is active against imatinib-resistant mutants of FIP1L1-PDGFRA and KIT, and against FGFR1-derived fusion kinases Leukemia 26 2012 1693 1695
33. J.M. Gozgit Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models Mol Cancer Ther 11 2012 690 699
34. M. Ren, M. Hong, G. Liu, H. Wang, V. Patel, and P. Biddinger et al. Novel FGFR inhibitor ponatinib suppresses the growth of non-small cell lung cancer cells overexpressing FGFR1 Oncol Rep 29 2013 2181 2190
35. N.P. Shah Ponatinib in patients with refractory acute myeloid leukaemia: findings from a phase 1 study Br J Haematol 162 2013 548 552
36. W.W. Chan Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036 Cancer Cell 19 2011 556 568
37. N.P. Shah, B.J. Skaggs, S. Branford, T.P. Hughes, J.M. Nicoll, and R.L. Paquette et al. Sequential ABL kinase inhibitor therapy selects for compound drug-resistant BCR-ABL mutations with altered oncogenic potency J Clin Invest 117 2007 2562 2569
38. C.A. Eide, L.T. Adrian, J.W. Tyner, M. Mac Partlin, D.J. Anderson, and S.C. Wise et al. The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile Cancer Res 71 2011 3189 3195