Molecular design and characterization of an α-thrombin inhibitor containing a novel P1 moiety

Biochemistry

Volumn 36, Issue 5, 1997, Pages 1034-1040

  Malikayil, J A ^a   Burkhart, Joseph P ^a   Schreuder, Herman A ^a   Broersma Jr , Robert J ^a   Tardif, Chantal ^a   Kutcher III, Louis W ^a   Mehdi, Shujaath ^a   Schatzman, Gerald L ^a   Neises, Bernhard ^a   Peet, Norton P ^a  

^a SANOFI   (France)

Author keywords

[No Author keywords available]

Indexed keywords

ALANINE; SERINE; THROMBIN; THROMBIN INHIBITOR; TRYPSIN; TRYPTOPHAN;

AMINO ACID SUBSTITUTION; ARTICLE; BINDING AFFINITY; CRYSTAL STRUCTURE; MOLECULAR MODEL; PRIORITY JOURNAL;

ALANINE; ANIMALS; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HIRUDINS; MODELS, MOLECULAR; OLIGOPEPTIDES; PARTIAL THROMBOPLASTIN TIME; PEPTIDE FRAGMENTS; PROTEIN CONFORMATION; RATS; SERINE PROTEINASE INHIBITORS; SOFTWARE; THROMBIN; TRYPSIN; TRYPSIN INHIBITORS; TRYPTOPHAN;

EID: 0031050773     PISSN: 00062960     EISSN: None     Source Type: Journal    
DOI: 10.1021/bi9622231     Document Type: Article

References (33)

1. Bailey, K., Bettelheim, Lorand, L., & Middlebrook, W. R. (1951) Nature 167, 233-234.
2. Berliner, L. J., & Shen, Y. Y. L. (1977) Biochemistry 16, 4622-4626.
3. Bode, W., Bauman, M. I., Huber, R., Stone, S. R., & Hofsteenge, J. (1989) EMBO J. 8, 3467-3475.
4. Bode, W., Turk, D., & Karshikov, A. (1992) Protein Sci. 86, 426-471.
5. Brooks, C. L., III, Karplus, M., & Pettitt, B. M. (1988) in Proteins: A Theoretical Perspective of Dynamics, Structure, and Thermodynamics, pp 95-116, Wiley-Interscience, New York.
6. Bruner-Lorand, J., Pilkington, T. R. E., & Lorand, L. (1966) Nature 210, 1273-1274.
7. Brünger, A. T. (1992) X-PLOR v3.1 Manual, Yale University Press, New Haven, CT.
8. Burley, S. K., & Petsko, G. A. (1988) Adv. Protein Chem. 39, 125-189.
9. Claeson, G. (1994) Blood Coagulation Fibrinolysis 5, 411-436.
10. Clore, M. G., Gronenborn, A. M., Carlson, G., & Meyer, E. F. (1986) J. Mol. Biol. 190, 259-267.
11. Fenton, J. W., II, Ofosu, F. A., Moon, D. G., & Maraganore, J. M. (1991) Blood Coagulation Fibrinolysis 2, 69-75.
12. Franzen, H., Grehn, L., & Ragnarsson, U. (1984) J. Chem. Soc., 1699-1700.
13. Grassman, P. G., & O'Reilly, N. J. (1987) J. Org. Chem. 52, 2481-2490.
14. Hansen, S. R., & Harker, L. A. (1988) Proc. Natl. Acad. Sci. U.S.A. 85, 3184-3188.
15. Jones, T. A. (1985) Methods Enzymol. 115, 157-171.
16. Kabsch, W. (1988) J. Appl. Crystallogr. 21, 916-924.
17. Kaiser, B., & Hauptmann, J. (1992) Cardiovasc. Drug Rev. 10, 71-87.
18. Lorand, L. (1951) Nature 167, 992-993.
19. Lorand, L. (1952) Biochem. J. 52, 200-203.
20. Lorand, L. (1961) Thromb. Diath. Haemorrh., Suppl. 7, 238-248.
21. Lorand, L., & Middlebrook, W. R. (1952) Biochem. J. 52, 196-199.
22. Lorand, L., & Konishi, K. (1964) Arch. Biochem. Biophys. 105, 58-67.
23. Mockros, L. F., Roberts, W. W., & Lorand, L. (1974) Biophys. Chem. 2, 164-169.
24. Perutz, M. F., Fermi, G., Abraham, D. J., Feyart, C., & Bursaus, E. (1986) J. Am. Chem. Soc. 108, 1064-1078.
25. Powers, J. C., & Kam, C.-M. (1992) in Thrombin: Structure and Function (Berliner, L., Ed.) pp 117-158, Plenum Press, New York.
26. Roberts, W. W., Lorand, L., & Mockros, L. F. (1973) Biorheology 10, 29-42.
27. Rydel, T. J., Tulinsky, A., Bode, W., & Huber, R. (1991) J. Mol. Biol. 221, 583-601.
28. Schechter, I., & Berger, A. (1967) Biochem. Biophys. Res. Commun. 27, 157-162.
29. Shen, L., & Lorand, L. (1983) J. Clin. Invest. 71, 1336-1341.
30. Still, W. C., Kahn, M., & Mitra, A. (1978) J. Org. Chem. 43, 2923-2925.
31. Tuppy, H., Wiesbauer, W., & Wintersberger, E. (1962) Hoppe-Seyler's Z. Physiol. Chem. 329, 278.
32. Veber, D. F., Lewis, S. D., Shafer, J. A., Feng, D.-M., Nutt, R. F., & Brady, S. F. (1994) WO945051.
33. Weitz, J. L., Hudoba, M., Massel, D., Maraganore, J., & Hirsch, J. (1990) J. Clin. Invest. 86, 385-391.