Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase

Journal of Biological Chemistry

Volumn 279, Issue 30, 2004, Pages 31655-31663

  Mol, Clifford D ^a   Dougan, Douglas R ^a   Schneider, Thomas R ^b   Skene, Robert J ^a   Kraus, Michelle L ^a   Scheibe, Daniel N ^a   Snell, Gyorgy P ^a   Zou, Hua ^a   Sang, Bi Ching ^a   Wilson, Keith P ^a  

^a Takeda San Diego Inc   (United States)

^b FIRC INSTITUTE OF MOLECULAR ONCOLOGY   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATION ANALYSIS; BIOLOGICAL MEMBRANES; CONFORMATIONS; CRYSTAL STRUCTURE; ENZYME KINETICS; TUMORS;

AUTOINHIBITION; PATHOGENESIS; PROTEIN-TYROSINE KINASE; STRUCTURE-GUIDED DESIGN;

ENZYME INHIBITION;

C KIT TYROSINE KINASE; IMATINIB; PROTEIN TYROSINE KINASE; STEM CELL FACTOR RECEPTOR; UNCLASSIFIED DRUG;

ARTICLE; CANCER; CARCINOGENESIS; CRYSTAL STRUCTURE; DRUG MECHANISM; ENZYME INHIBITION; HUMAN; NUCLEOTIDE SEQUENCE; PATHOGENESIS; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN TARGETING;

EID: 2942542387     PISSN: 00219258     EISSN: None     Source Type: Journal    
DOI: 10.1074/jbc.M403319200     Document Type: Article

References (52)

1. Linnekin, D. (1999) Int. J. of Biochem. Cell Biol. 31, 1053-1074
2. Besmer, P., Murphy, J. E., George, P. C., Qiu, F. H., Bergold, P. J., Lederman, L., Snyder, H. W., Jr., Broudeur, D., Zuckerman, E. E., and Hardy, W. D. (1986) Nature 320, 415-421
3. Coussens, L., Van Beveren, C., Smith, D., Chen, E., Mitchell, R. L., Isacke, C. M., Verma, I. M., and Ullrich, A. (1986) Nature 320, 277-280
4. Rosnet, O., Schiff, C., Pebusque, M.-J., Marchetto, S., Tonnelle, C., Toiron, Y., Birg, F., and Birnbaum, D. (1993) Blood 82, 1110-1119
5. Claesson-Welsh, L., Eriksson, A., Westermark, B., and Heldin, C.-H. (1989) Proc. Natl. Acad. Sci. U. S. A. 86, 4917-4921
6. Yarden, Y., Escobedo, J. A., Kuang, W.-J., Yang-Feng, T. L., Daniel, T. O., Tremble, P. M., Chen, E. Y., Ando, M. E., Harkins, R. N., Francke, U., Fried, V. A., Ullrich, A., and Williams, L. T. (1986) Nature 323, 226-232
7. Yarden, Y., Kuang, W.-J., Yang-Feng, T., Coussens, L., Munemitsu, S., Dull, T. J., Chen, E., Schlessinger, J., Francke, U., and Ullrich, A. (1987) EMBO J. 6, 3341-3351
8. Ullrich, A., and Schlessinger, J. (1990) Cell 61, 203-212
9. Heldin, C.-H. (1995) Cell 80, 213-223
10. Hubbard, S. R., Mohammadi, M., and Schlessinger, J. (1998) J. Biol. Chem. 273, 11987-11990
11. Weiss, A., and Schlessinger, J. (1998) Cell 94, 277-280
12. Blume-Jensen, P., and Hunter, T. (2001) Nature 411, 355-365
13. Hirota, S., Isozaki, K., Moriyama, Y., Hashimoto, K., Nishida, T., Ishiguro, S., Kawano, K., Hanada, M., Kurata, A., Takeda, M., Tunio, G. M., Matsuzawa, Y., Kanakura, Y., Sinomura, Y., and Kitamura, Y. (1998) Science 279, 577-580
14. Nishida, T., Hirota, S., Taniguchi, M., Hashimoto, K., Isozaki, K. Nakamura, H., Kanakura, Y., Tanaka, T., Takabayashi, A., Matsuda, H., and Kitamura, Y. (1998) Nat. Genet. 19, 323-324
15. Tian, Q., Frierson, H. F., Jr., Krystal, G. W., and Moskaluk, C. A. (1999) Am. J. Pathol. 154, 1643-1647
16. Kitamura, Y., Hirota, S., and Nishida, T. (2001) Mutat. Res. 477, 165-171
17. Longley, B. J., Jr., Metcalfe, D. D., Tharp, M., Wang, X., Tyrrell, L., Lu, S.-Z., Heitjan, D., and Ma, Y. (1999) Proc. Natl. Acad. Sci. U. S. A. 96, 1609-1614
18. Frost, M. J., Ferrao, P. T., Hughes, T. P., and Ashman, L. K. (2002) Mol. Cancer Ther. 12, 1115-1124
19. Ma, Y., Zeng, S., Metcalfe, D. D., Akin, C., Dimitrijevic, S., Butterfield, J. H., McMahon, G., and Longley, B. J. (2002) Blood 99, 1741-1744
20. Ueda, S., Ikeda, H., Mizuki, M., Ishiko, J., Matsumura, I., Tanaka, H., Shibayama, H., Sugahara, H., Takai, E., Zhang, X., Machii, T., and Kanakura, Y. (2002) Int. J. Hematol. 76, 427-435
21. Zermati, Y., De Sepulveda, P., Feger, F., Letard, S., Kersual, J., Casteran, N., Gorochev, G., Dy, M., Ribadeau Dumas, A., Dorgham, K., Parizot, C., Bieche, Y., Vidaud, M., Lortholary, O., Arock, M., Hermine, O., and Dubreuil, P. (2003) Oncogene 22, 660-664
22. Kozlowski, M., Larose, L., Lee, F., Le, D. M., Rottapel, R., and Siminovitch, K. A. (1998) Mol. Cell. Biol. 18, 2089-2099
23. Ma, Y., Cunningham, M. E., Wang, X., Ghosh, I., Regan, L., and Longley, B. J. (1999) J. Biol. Chem. 274, 13399-13402
24. Irusta, P. M., and DiMaio, D. (1998) EMBO J. 17, 6912-6923
25. Irusta, P. M., Luo, Y., Bakht, O., Lai, C.-C., Smith, S. O., and DiMaio, D. (2002) J. Biol. Chem. 277, 38627-38634
26. Ilsley, J. L., Sudol, M., and Winder, S. J. (2002) Cell. Signal. 14, 183-189
27. Macias, M. J., Wiesner, S., and Sudol, M. (2002) FEBS Lett. 513, 30-37
28. Sudol, M., and Hunter, T. (2000) Cell 103, 1001-1004
29. Chan, P. M., Ilangumaran, S., La Rose, J., Chakrabartty, A., and Rottapel, R. (2003) Mol. Cell. Biol. 23, 3067-3078
30. Hubbard, S. R., and Hill, J. H. (2000) Annu. Rev. Biochem. 69, 373-398
31. Hubbard, S. R. (2002) Curr. Opin. Struct. Biol. 12, 735-741
32. Wybenga-Groot, L. E., Baskin, B., Ong, S. H., Tong, J., Pawson, T., and Sicheri, F. (2001) Cell 106, 745-757
33. Till, J. H., Becerra, M., Watty, A., Lu, Y., Ma, Y., Neubert, T. A., Burden, S. J., and Hubbard, S. R. (2002) Structure 10, 1187-1196
34. Li, S., Covino, N. D., Stein, E. G., Till, J. H., and Hubbard, S. R. (2003) J. Biol. Chem. 278, 26007-26014
35. O'Dwyer, M. E., Mauro, M. J. and Druker, B. J. (2003) Cancer Investig. 3, 429-438
36. Buchdunger, E., Cioffi, C. L., Law, N., Stover, D., Ohno Jones, S., Druker, B. J., and Lydon, N. B. (2000) J. Pharmacol. Exp. Ther. 295, 139-145
37. Mol, C. D., Lim, K. B., Sridhar, V., Zou, H., Chien, E. Y., Sang, B.-C., Nowakowski, J., Kassel, D. B., Cronin, C. N., and Mcree, D. E. (2003) J. Biol. Chem. 278, 31461-31464
38. Hosfield, D., Palan, J., Hilgers, M., Scheibe, D., McRee, D. E., and Stevens, R. C. (2003) J. Struct. Biol. 142, 207-217
39. Otwinowski, Z., and Minor, W. (1997) Methods Enzymol. 276, 307-326
40. Navaza, J. (2001) Acta Crystallogr. Sect. D 57, 1367-1372
41. Murshudov, G. N., Vagin, A. A., and E. J. Dodson. (1997) Acta Crystallogr. Sect. D 53, 240-255
42. McRee, D. E. (1999) J. Struct. Biol. 125, 156-165
43. Cruickshank, D. W. (1999) Acta Crystallogr. Sect. D 55, 583-601
44. Schneider, T. R. (2002) Acta Crystallogr. Sect. D 58, 195-208
45. Kemp, B. E., and Pearson, R. B. (1991) Biochim. Biophys. Acta 1094, 67-76
46. Huse, M., and Kuriyan, J. (2002) Cell 109, 275-282
47. Nagar, B., Hantschel, O., Young, M. A., Scheffzek, K., Veach, D., Bornmann, W., Clarkson, B., Superti-Furga, G., and Kuriyan, J. (2003) Cell 112, 859-871
48. Piao, X., Paulson, R., van der Greer, P., Pawson, T., and Bernstein, A. (1996) Proc. Natl. Acad. Sci. U. S. A. 93, 14665-14669
49. Hubbard, S. R., Wei, L., Ellis, L., and Hendrickson, W. A. (1994) Nature 372, 746-754
50. Schindler, T., Bornmann, W. G., Pellicena, P., Miller, W. T., Clarkson, B., and Kuriyan, J. (2000) Science 289, 1938-1942
51. Nagar, B., Bornmann, W. G., Pellicena, P., Schindler, T., Veach, D. R., Miller, W. T., Clarkson, B., and Kuriyan, J. (2002) Cancer Res. 62, 4236-4243
52. Griffith, J., Black, J., Faerman, C., Swenson, L., Wynn, M., Lu, F., Lippke, J., and Saxena, K. (2004) Mol. Cell 13, 169-178