Characterization of the two-step pathway for inhibition of thrombin by α-ketoamide transition state analogs

Journal of Biological Chemistry

Volumn 273, Issue 9, 1998, Pages 4843-4854

  Lewis, Sidney D ^a   Lucas, Bobby J ^a   Brady, Stephen F ^a   Sisko, John T ^a   Cutrona, Kellie J ^a   Sanderson, Philip E J ^a   Freidinger, Roger M ^a   Mao, Shi Shan ^a   Gardell, Stephen J ^a   Shafer, Jules A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

L 370518; L 372011; L 372051; L 372228; L 372912; THROMBIN; THROMBIN INHIBITOR; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; AMINO TERMINAL SEQUENCE; ARTICLE; ENZYME ACTIVITY; ENZYME BINDING; GENE REARRANGEMENT; PRIORITY JOURNAL; PROTEIN FOLDING; THROMBIN TIME; THROMBOGENESIS;

BINDING SITES; BINDING, COMPETITIVE; CATALYSIS; FLOW INJECTION ANALYSIS; FLUORESCENT DYES; KINETICS; MODELS, CHEMICAL; OLIGOPEPTIDES; SERINE PROTEINASE INHIBITORS; THROMBIN;

EID: 18744427103     PISSN: 00219258     EISSN: None     Source Type: Journal    
DOI: 10.1074/jbc.273.9.4843     Document Type: Article

References (24)

1. Mehdi, S. (1993) Bioorg. Chem. 21, 249-259
2. Fusetani, N., Matsunaga, S., Matsumoto, H., and Takebayashi, Y. (1990) J. Am. Chem. Soc. 112, 7053-7054
3. Hagihara, M., and Schreiber, S. L. (1992) J. Am. Chem. Soc. 114, 6570-6571
4. Wipf, P., and Kim, H. (1993) J. Org. Chem. 58, 5592-5594
5. Lewis, S. D., Ng, A. S., Baldwin, J. J., Fusetani, N., Naylor, A. M., and Shafer, J. A. (1993) Thromb. Res. 70, 173-190
6. Marynoff, B. E., Greco, M. N., Zhang, H.-C., Andrade-Gordon, P., Kauffman, J. A., Nicolaou, K. C., Liu, A., and Brungs, P. H. (1995) J. Am. Chem. Soc. 117, 1225-1239
7. Maryanoff, B. E., Qiu, X., Padmanabhan, K. P., Tulinsky, A., Almond, H. R., Jr., Andrade-Gordon, P., Greco, M. N., Kauffman, J. A., Nicolaou, K. C., Liu, A., Brungs, P. H., and Fusetani, N. (1993) Proc. Natl. Acad. Sci. U. S. A. 90, 8048-8052
8. Lewis, S. D., Ng, A. S., Lyle, E. A., Mellott, M. J., Appleby, S. D., Brady, S. F., Stauffor, K. J., Sisko, J. T., Mao, S.-S., Veber, D. F., Nutt, R. F., Lynch, J. J., Cook, J. J., Gardell, S. J., and Shafer, J. A. (1995) Thromb. Haemostasis 74, 1107-1113
9. Brady, S. F., Sisko, J. T., Stauffer, K. J., Colton, C. D., Qiu, H., Lewis, S. D., Ng, A. S., Shafer, J. A., Bogusky, M. J., Veber, D. F., Nutt, R. F. (1995) Bioorg. & Med. Chem. Lett. 3 1063-1078
10. Brady, S. F., Lewis, S. D., Colton, C. D., Stauffer, K. J., Sisko, J. T., Ng, A. S., Homnick, C. F., Bogusky, M. J., Shafer, J. A., Veber, D. F., and Nutt, R. F. (1995) in Peptides: Chemistry, Structure and Biology (Kaumaya, P. T. P., and Hodges, R. S. eds) pp. 331-333, Mayflower Scientific, Ltd., London
11. Cutrona, K. J., and Sanderson, P. E. J. (1996) Tetrahedron Lett. 37, 5045-5048
12. Lyle, T. A., Chen, Z., Appleby, S. D., Freidinger, R. M., Gardell, S. J., Lewis, S. D., Li, Y., Lyle, E. A., Lynch, J. J., Jr., Mulichak, A. M., Ng, A. S., Naylor-Olsen, A. M., and Sanders, W. M. (1997) Bioorg. & Med. Chem. Lett. 7, 67-72
13. Bode, W., Turk, D., and Karshikov, A. (1992) Protein Sci. 1, 426-471
14. Chen, Z., Li, Y., Mulichak, A. M., Lewis, S. D., and Shafer, J. A. (1995) Arch. Biochem. Biophys. 322, 198-203
15. Morrison, J. F. (1982) Trends Biochem. Sci. 7, 102-105
16. Sculley, M. J., Morrison, J. F., and Cleland, W. W. (1996) Biochim. Biophys. Acta 1298, 78-86
17. Nesheim, M. E., Prendergast, F. G., Mann, K. G. (1979) Biochemistry 18, 996-1003
18. Williams, J. W., and Morrison, J. F. (1979) Methods Enzymol. 63, 437-467
19. Henderson, P. J. F. (1972) Biochem. J. 127, 321-333
20. Cha, S. (1975) Biochem. Pharmacol. 24, 2177-2185
21. Nesheim, M. E. (1983) J. Biol. Chem. 258, 14708-14717
22. Stone, S. R., and Hermans, J. M. (1995) Biochemistry 34, 5164-5172
23. Schechter, I., and Berger, A. (1967) Biochem. Biophys. Res. Commun. 27, 157-162
24. Bode, W., Magr, I., Baumann, U., Huber, R., Stone, S. R., and Hofsteenge, J. (1989) EMBO J. 8, 3467-3475