Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases

Proceedings of the National Academy of Sciences of the United States of America

Volumn 102, Issue 31, 2005, Pages 11011-11016

  Carter, Todd A ^a   Wodicka, Lisa M ^a   Shah, Neil P ^b   Velasco, Anne Marie ^a   Fabian, Miles A ^a   Treiber, Daniel K ^a   Milanov, Zdravko V ^a   Atteridge, Corey E ^a   Biggs III, William H ^a   Edeen, Philip T ^a   Floyd, Mark ^a   Ford, Julia M ^a   Grotzfeld, Robert M ^a   Herrgard, Sanna ^a   Insko, Darren E ^a   Mehta, Shamal A ^a   Patel, Hitesh K ^a   Pao, William ^c   Sawyers, Charles L ^b   Varmus, Harold ^c   Zarrinkar, Patrick P ^a   Lockhart, David J ^a   more..

^a Ambit Biosciences   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c MEMORIAL SLOAN KETTERING CANCER CENTER   (United States)

Author keywords

Drug resistance; Gatekeeper mutation; Kinase inhibitor

Indexed keywords

4 [6 METHOXY 7 [3 (1 PIPERIDINYL)PROPOXY] 4 QUINAZOLINYL] 1 PIPERAZINECARBOXYLIC ACID (4 ISOPROPOXYPHENYL)AMIDE; ABELSON KINASE; BCR ABL PROTEIN; CANERTINIB; CYCLOPROPANECARBOXYLIC ACID [4 [4 (4 METHYL 1 PIPERAZINYL) 6 (5 METHYL 2H PYRAZOL 3 YLAMINO) 2 PYRIMIDINYLTHIO]PHENYL]AMIDE; DASATINIB; DORAMAPIMOD; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; IMATINIB; LAPATINIB; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; MUTANT PROTEIN; PELITINIB; PROTEIN KINASE INHIBITOR; STEM CELL FACTOR; SUNITINIB; THREONINE; UNCLASSIFIED DRUG; VANDETANIB;

AMINO ACID SEQUENCE; ARTICLE; CANCER CHEMOTHERAPY; CANCER RESISTANCE; CONTROLLED STUDY; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG TARGETING; EMBRYO; ENZYME ACTIVE SITE; ENZYME INHIBITION; HUMAN; HUMAN CELL; LUNG NON SMALL CELL CANCER; PRIORITY JOURNAL; PROTEIN TARGETING;

CELL LINE; DRUG RESISTANCE, NEOPLASM; HUMANS; INDOLES; KINETICS; MORPHOLINES; MUTATION; NAPHTHALENES; NEOPLASMS; ONCOGENE PROTEINS V-ABL; ORGANIC CHEMICALS; PIPERAZINES; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-KIT; PYRAZOLES; PYRROLES; RECEPTOR, EPIDERMAL GROWTH FACTOR;

PYRONIA TITHONUS;

EID: 23344440655     PISSN: 00278424     EISSN: None     Source Type: Journal    
DOI: 10.1073/pnas.0504952102     Document Type: Article

References (52)

1. Sawyers, C. (2004) Nature 432, 294-297.
2. Druker, B. J. (2004) Oncologist 9, 357-360.
3. Wadleigh, M., DeAngelo, D. J., Griffin, J. D. & Stone, R. M. (2005) Blood 105, 22-30.
4. Gorre, M. E., Mohammed, M., Ellwood, K., Hsu, N., Paquette, R., Rao, P. N. & Sawyers, C. L. (2001) Science 293, 876-880.
5. Deininger, M., Buchdunger, E. & Druker, B. J. (2005) Blood 105, 2640-2653.
6. Chen, L. L., Trent, J. C., Wu, E. F., Fuller, G. N., Ramdas, L., Zhang, W., Raymond, A. K., Prieto, V. G., Oyedeji, C. O., Hunt, K. K., et al. (2004) Cancer Res. 64, 5913-5919.
7. Tamborini, E., Bonadiman, L., Greco, A., Albertini, V., Negri, T., Gronchi, A., Bertulli, R., Colecchia, M., Casali, P. G., Pierotti, M. A., et al. (2004) Gastroenterology 127, 294-299.
8. Debiec-Rychter, M., Cools, J., Dumez, H., Sciot, R., Stul, M., Mentens, N., Vranckx, H., Wasag, B., Prenen, H., Roesel, J., et al. (2005) Gastroenterology 128, 270-279.
9. Cools, J., DeAngelo, D. J., Gotlib, J., Stover, E. H., Legare, R. D., Cortes, J., Kutok, J., Clark, J., Galinsky, I., Griffin, J. D., et al. (2003) N. Engl. J. Med. 348, 1201-1214.
10. Kobayashi, S., Boggon, T. J., Dayaram, T., Janne, P. A., Kocher, O., Meyerson, M., Johnson, B. E., Eck, M. J., Tenen, D. G. & Halmos, B. (2005) N. Engl. J. Med. 352, 786-792.
11. Pao, W., Miller, V. A., Politi, K. A., Riely, G. J., Somwar, R., Zakowski, M. F., Kris, M. G. & Varmus, H. (2005) PLoS Med. 2, e73.
12. Deininger, M. W. & Druker, B. J. (2004) Cancer Cell 6, 108-110.
13. Daub, H., Specht, K. & Ullrich, A. (2004) Nat. Rev. Drug Discov. 3, 1001-1010.
14. Fabian, M. A., Biggs, W. H., Treiber, D. K., Atteridge, C. E., Azimioara, M. D., Benedetti, M. G., Carter, T. A., Ciceri, P., Edeen, P. T., Floyd, M., et al. (2005) Nat. Biotechnol. 23, 329-336.
15. Buchdunger, E., Cioffi, C. L., Law, N., Stover, D., Ohno-Jones, S., Druker, B. J. & Lydon, N. B. (2000) J. Pharmacol. Exp. Ther. 295, 139-145.
16. Heinrich, M. C., Griffith, D. J., Druker, B. J., Wait, C. L., Ott, K. A. & Zigler, A. J. (2000) Blood 96, 925-932.
17. Joensuu, H., Roberts, P. J., Sarlomo-Rikala, M., Andersson, L. C., Tervahartiala, P., Tuveson, D., Silberman, S., Capdeville, R., Dimitrijevic, S., Druker, B., et al. (2001) N. Engl. J. Med. 344, 1052-1056.
18. Blencke, S., Zech, B., Engkvist, O., Greff, Z., Orfi, L., Horvath, Z., Keri, G., Ullrich, A. & Daub, H. (2004) Chem. Biol. 11, 691-701.
19. Shah, N. P., Tran, C., Lee, F. Y., Chen, P., Norris, D. & Sawyers, C. L. (2004) Science 305, 399-401.
20. Weisberg, E., Manley, P. W., Breitenstein, W., Bruggen, J., Cowan-Jacob, S. W., Ray, A., Huntly, B., Fabbro, D., Fendrich, G., Hall-Meyers, E., et al. (2005) Cancer Cell 7, 129-141.
21. La Rosee, P., Corbin, A. S., Stoffregen, E. P., Deininger, M. W. & Druker, B. J. (2002) Cancer Res. 62, 7149-7153.
22. O'Hare, T., Pollock, R., Stoffregen, E. P., Keats, J. A., Abdullah, O. M., Moseson, E. M., Rivera, V. M., Tang, H., Metcalf, C. A., III, Bohacek, R. S., et al. (2004) Blood 104, 2532-2539.
23. Pargellis, C., Tong, L., Churchill, L., Cirillo, P. F., Gilmore, T., Graham, A. G., Grob, P. M., Hickey, E. R., Moss, N., Pav, S., et al. (2002) Nat. Struct. Biol. 9, 268-272.
24. Harrington, E. A., Bebbington, D., Moore, J., Rasmussen, R. K., Ajose-Adeogun, A. O., Nakayama, T., Graham, J. A., Demur, C., Hercend, T., Diu-Hercend, A., et al. (2004) Nat. Med. 10, 262-267.
25. Fiedler, W., Serve, H., Dohner, H., Schwittay, M., Ottmann, O. G., O'Farrell, A. M., Bello, C. L., Allred, R., Manning, W. C., Cherrington, J. M., et al. (2005) Blood 105, 986-993.
26. Calvo, E., Tolcher, A. W., Hammond, L. A., Patnaik, A., de Bono, J. S., Eiseman, I. A., Olson, S. C., Lenehan, P. F., McCreery, H., Lorusso, P., et al. (2004) Clin. Cancer Res. 10, 7112-7120.
27. Tsou, H. R., Overbeek-Klumpers, E. G., Hallett, W. A., Reich, M. F., Floyd, M. B., Johnson, B. D., Michalak, R. S., Nilakantan, R., Discafani, C., Golas, J., et al. (2005) J. Med. Chem. 48, 1107-1131.
28. Shah, N. P., Nicoll, J. M., Nagar, B., Gone, M. E., Paquette, R. L., Kuriyan, J. & Sawyers, C. L. (2002) Cancer Cell 2, 117-125.
29. Hirota, S., Isozaki, K., Moriyama, Y., Hashimoto, K., Nishida, T., Ishiguro, S., Kawano, K., Hanada, M., Kurata, A., Takeda, M., et al. (1998) Science 279, 577-580.
30. Rubin, B. P., Singer, S., Tsao, C., Duensing, A., Lux, M. L., Ruiz, R., Hibbard, M. K., Chen, C. J., Xiao, S., Tuveson, D. A., et al. (2001) Cancer Res. 61, 8118-8121.
31. Lombardo, L. J., Lee, F. Y., Chen, P., Norris, D., Barrish, J. C., Behnia, K., Castaneda, S., Cornelius, L. A., Das, J., Doweyko, A. M., et al. (2004) J. Med. Chem. 47, 6658-6661.
32. Burgess, M. R., Skaggs, B. J., Shah, N. P., Lee, F. Y. & Sawyers, C. L. (2005) Proc. Natl. Acad. Sci. USA 102, 3395-3400.
33. Corbin, A. S., Griswold, I. J., La Rosee, P., Yee, K. W., Heinrich, M. C., Reimer, C. L., Druker, B. J. & Deininger, M. W. (2004) Blood 104, 3754-3757.
34. O'Farrell, A. M., Abrams, T. J., Yuen, H. A., Ngai, T. J., Louie, S. G., Yee, K. W., Wong, L. M., Hong, W., Lee, L. B., Town, A., et al. (2003) Blood 101, 3597-3605.
35. Abrams, T. J., Lee, L. B., Murray, L. J., Fryer, N. K. & Cherrington, J. M. (2003) Mol. Cancer Ther. 2, 471-478.
36. Kelly, L. M., Yu, J. C., Boulton, C. L., Apatira, M., Li, J., Sullivan, C. M., Williams, I., Amaral, S. M., Curley, D. P., Duclos, N., et al. (2002) Cancer Cell 1, 421-432.
37. Griswold, I. J., Shen, L. J., La Rosee, P., Demehri, S., Heinrich, M. C., Braziel, R. M., McGreevey, L., Haley, A. D., Giese, N., Druker, B. J., et al. (2004) Blood 104, 2912-2918.
38. Schindler, T., Bornmann, W., Pellicena, P., Miller, W. T., Clarkson, B. & Kuriyan, J. (2000) Science 289, 1938-1942.
39. Lynch, T. J., Bell, D. W., Sordella, R., Gurubhagavatula, S., Okimoto, R. A., Brannigan, B. W., Harris, P. L., Haserlat, S. M., Supko, J. G., Haluska, F. G., et al. (2004) N. Engl. J. Med. 350, 2129-2139.
40. Paez, J. G., Janne, P. A., Lee, J. C., Tracy, S., Greulich, H., Gabriel, S., Herman, P., Kaye, F. J., Lindeman, N., Boggon, T. J., et al. (2004) Science 304, 1497-1500.
41. Pao, W., Miller, V., Zakowski, M., Doherty, J., Politi, K., Sarkaria, I., Singh, B., Heelan, R., Rusch, V., Fulton, L., et al. (2004) Proc. Natl. Acad. Sci. USA 101, 13306-13311.
42. Eyers, P. A., Craxton, M., Morrice, N., Cohen, P. & Goedert, M. (1998) Chem. Biol. 5, 321-328.
43. Fox, T., Coll, J. T., Xie, X., Ford, P. J., Germann, U. A., Porter, M. D., Pazhanisamy, S., Fleming, M. A., Galullo, V., Su, M. S., et al. (1998) Protein Sci. 7, 2249-2255.
44. Gorre, M. E., Ellwood-Yen, K., Chiosis, G., Rosen, N. & Sawyers, C. L. (2002) Blood 100, 3041-3044.
45. Gumireddy, K., Baker, S. J., Cosenza, S. C., John, P., Kang, A. D., Robell, K. A., Reddy, M. V. & Reddy, E. P. (2005) Proc. Natl. Acad. Sci. USA 102, 1992-1997.
46. 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., et al. (2001) N. Engl. J. Med. 344, 1031-1037.
47. Smaill, J. B., Rewcastle, G. W., Loo, J. A., Greis, K. D., Chan, O. H., Reyner, E. L., Lipka, E., Showalter, H. D., Vincent, P. W., Elliott, W. L., et al. (2000) J. Med. Chem. 43, 1380-1397.
48. Wissner, A., Overbeek, E., Reich, M. F., Floyd, M. B., Johnson, B. D., Mamuya, N., Rosfjord, E. C., Discafani, C., Davis, R., Shi, X., et al. (2003) J. Med. Chem. 46, 49-63.
49. Discafani, C. M., Carroll, M. L., Floyd, M. B., Jr., Hollander, I. J., Husain, Z., Johnson, B. D., Kitchen, D., May, M. K., Malo, M. S., Minnick, A. A., Jr., et al. (1999) Biochem. Pharmacol. 57, 917-925.
50. Rabindran, S. K., Discafani, C. M., Rosfjord, E. C., Baxter, M., Floyd, M. B., Golas, J., Hallett, W. A., Johnson, B. D., Nilakantan, R., Overbeek, E., et al. (2004) Cancer Res. 64, 3958-3965.
51. Kwak, E. L., Sordella, R., Bell, D. W., Godin-Heymann, N., Okimoto, R. A., Brannigan, B. W., Harris, P. L., Driscoll, D. R., Fidias, P., Lynch, T. J., et al. (2005) Proc. Natl. Acad. Sci. USA 102, 7665-7670.
52. Manning, G., Whyte, D. B., Martinez, R., Hunter, T. & Sudarsanam, S. (2002) Science 298, 1912-1934.