Analysis of human cytochrome P450 3A4 cooperativity: Construction and characterization of a site-directed mutant that displays hyperbolic steroid hydroxylation kinetics

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

Volumn 95, Issue 12, 1998, Pages 6636-6641

  Harlow, Greg R ^a   Halpert, James R ^a  

^a UNIVERSITY OF ARIZONA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALPHA NAPHTHOFLAVONE; CYTOCHROME; PROGESTERONE; TESTOSTERONE;

ARTICLE; BINDING KINETICS; BINDING SITE; COMPETITIVE INHIBITION; COMPUTER MODEL; ENZYME ACTIVE SITE; ENZYME ANALYSIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; HUMAN TISSUE; HYDROXYLATION; PRIORITY JOURNAL; SITE DIRECTED MUTAGENESIS; STEROID METABOLISM;

BINDING SITES; CYTOCHROME P-450 ENZYME SYSTEM; HUMANS; HYDROXYLATION; MIXED FUNCTION OXYGENASES; MUTAGENESIS, SITE-DIRECTED; MUTATION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0032499691     PISSN: 00278424     EISSN: None     Source Type: Journal    
DOI: 10.1073/pnas.95.12.6636     Document Type: Article

References (29)

1. Guengerich, F. P. (1990) Chem. Res. Toxicol. 3, 363-371.
2. McKinnon, R. A., Burgess, W. M., Hall, P. M., Roberts-Thomson, S. J., Gonzalez, F. J. & McManus, M. E. (1995) Gut 36, 259-267.
3. Kolars, J. C., Lown, K. S., Schmiedlin-Ren, P., Ghosh, M., Fang, C., Wrighton, S. A., Merion, R. M. & Watkins, P. B. (1994) Pharmacogenetics 4, 247-259.
4. Guengerich, F. P. (1995) Cytochrome P450: Structure, Mechanism, and Biochemistry, ed. Ortiz de Montellano, P. R. (Plenum, New York).
5. Schwab, G. E., Raucy, J. L. & Johnson, E. F. (1988) Mol. Phamacol. 33, 493-499.
6. He, Y. A., He, Y. Q., Szklarz, G. D. & Halpert, J. R. (1997) Biochemistry 36, 8831-8839.
7. Harlow, G. R. & Halpert, J. R. (1997) J. Biol. Chem. 272, 5396-5402.
8. Ueng, Y.-F., Kuwabara, T., Chun, Y.-J. & Guengerich, F. P. (1997) Biochemistry 36, 370-381.
9. Kerlan, V., Dreano, Y., Bercovici, J. P., Beaune, P. H., Floch, H. H. & Berthou, F. (1992) Biochem. Pharmacol. 44, 1745-1756.
10. Ueng, Y., Shimada, T., Yamazaki, H. & Guengerich, F. P. (1995) Chem. Res. Toxicol. 8, 218-225.
11. Shimada, T. & Guengerich, F. P. (1989) Proc. Natl. Acad. Sci. USA 86, 462-465.
12. Koley, A. P., Buters, J. T. M., Robinson, R. C., Markowitz, A. & Friedman, F. K. (1997) J. Biol. Chem. 272, 3149-3152.
13. Shou, M., Grogan, J., Mancewicz, J. A., Krausz, K. W., Gonzalez, F. J., Gelboin, H. V. & Korzekwa, K. R. (1994) Biochemistry 33, 6450-6455.
14. Kerr, B. M., Thummel, K. E., Wurden, C. J., Klein, S. M., Kroetz, D. L., Gonzalez, F. J. & Levy, R. H. (1994) Biochem. Pharmacol. 47, 1969-1979.
15. Li, Y., Wang, E., Patten, C. J., Chen, L. & Yang, C. (1994) Drug. Metab. Dispos. 22, 566-571.
16. Perutz, M. (1970) Nature (London) 228, 726-739.
17. Szklarz, G. D. & Halpert, J. R. (1997) J. Comput. Aided Mol. Des. 11, 265-272.
18. Wang, R. W., Newton, D. J., Scheri, T. D. & Lu, A. Y. H. (1997) Drug Metab. Dispos. 25, 502-507.
19. Domanski, T. L., Liu, J., Harlow, G. R. & Halpert, J. R. (1998) Arch. Biochem. Biophys. 350, 223-232.
20. John, G. H., Hasler, J. A., He, Y. & Halpert, J. R. (1994) Arch. Biochem. Biophys. 314, 367-375.
21. Lowry, O. H., Rosebrough, N. J., Farr, A. L. & Randall, R. J. (1951) J. Biol. Chem. 193, 265-275.
22. Harlow, G. R., He, Y. A. & Halpert, J. R. (1997) Biochim. Biophys. Acta 1338, 258-266.
23. Harlow, G. R. & Halpert, J. R. (1996) Arch. Biochem. Biophys. 326, 85-92.
24. Gibson, G., Cinti, D., Sligar, S. & Schenkman, J. (1980) J. Biol. Chem. 255, 1867-1873.
25. Dixon, M. (1953) Biochem. J. 55, 170-171.
26. Hasemann, C. A., Kurumbail, R. G., Boddupalli, S. S., Peterson, J. A. & Deisenhofer, J. (1995) Curr. Biol. 2, 41-62.
27. Gotoh, O. (1992) J. Biol. Chem. 267, 83-90.
28. Luo, Z., He, Y. & Halpert, J. R. (1994) Arch. Biochem. Biophys. 309, 52-57.
29. Johnson, E. F., Schwab, G. E. & Vickery, L. E. (1988) J. Biol. Chem. 263, 17672-17677.