Design of potent and selective human cathepsin K inhibitors that span the active site

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

Volumn 94, Issue 26, 1997, Pages 14249-14254

  Thompson, Scott K ^a   Halbert, Stacie M ^a   Bossard, Mary J ^a   Tomaszek, Thaddeus A ^a   Levy, Mark A ^a   Zhao, Baoguang ^a   Smith, Ward W ^a   Abdel Meguid, Sherin S ^a   Janson, Cheryl A ^a   D'Alessio, Karla J ^a   Mcqueney, Michael S ^a   Amegadzie, Bernard Y ^a   Hanning, Charles R ^a   Desjarlais, Renee L ^a   Briand, Jacques ^a   Sarkar, Susanta K ^a   Huddleston, Michael J ^a   Ijames, Carl F ^a   Carr, Steven A ^a   Garnes, Keith T ^a   Shu, Art ^a   Heys, J Richard ^a   Bradbeer, Jeremy ^a   Zembryki, Denise ^a   Lee Rykaczewski, Liz ^a   James, Ian E ^a   Lark, Michael W ^a   Drake, Fred H ^a   Gowen, Maxine ^a   Gleason, John G ^a   Veber, Daniel F ^a,b   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b SmithKline Beecham Pharmaceutical ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CATHEPSIN; CYSTEINE PROTEINASE; LEUPEPTIN;

ARTICLE; ENZYME ACTIVE SITE; ENZYME INHIBITION; HUMAN; HUMAN CELL; OSTEOCLAST; OSTEOPOROSIS; PRIORITY JOURNAL;

BINDING SITES; CATHEPSINS; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; PROTEIN CONFORMATION;

EID: 0000263910     PISSN: 00278424     EISSN: None     Source Type: Journal    
DOI: 10.1073/pnas.94.26.14249     Document Type: Article

References (26)

1. Drake, F. H., Dodds, R. A., James, I. E., Connor, J. R., Debouck, C., Richardson, S., Lee-Rykaczewski, E., Coleman, L., Rieman, D., Barthlow, R., Hastings, G. & Gowen, M. (1996) J. Biol. Chem. 271, 12511-12516.
2. Bossard, M. J., Tomaszek, T. A., Thompson, S. K., Amegadzie, B. Y., Hanning, C. R., Jones, C., Kurdyla, J. T., McNulty, D. E., Drake, F. H., Gowen, M. & Levy, M. A. (1996) J. Biol. Chem. 271, 12517-12524.
3. McQueney, M. S., Amegadzie, B. Y., D'Alessio, K. D., Hanning, C. R., McLaughlin, M. M., McNulty, D., Carr, S. A., Ijames, C., Kurdyla, J. & Jones, C. S. (1997) J. Biol. Chem. 272, 13955-13960.
4. McKerrow, J. H. & James, M. N. G., eds. (1996) Perspect. Drug Dis. Des. 6, 1-125.
5. Demuth, H.-U. (1990) J. Enzyme Inhibition 3, 249-278.
6. Schechter, I. & Berger, A. (1967) Biochem. Biophys. Res. Commun. 27, 157-162.
7. Baggio, R., Shi, Y.-Q., Wu, Y.-Q. & Abeles, R. H. (1996) Biochemistry 35, 3351-3353.
8. Amos, H. E. & Park, B. K. (1985) in Immunotoxicology and Immunopharmacology, eds., Dean, J. H., Luster, M. I., Munson, A. E. & Amos, H. E. (Raven, New York), pp. 207-228.
9. Ondetti, M. A., Rubin, B. & Cushman, D. W. (1977) Science 196, 441-444.
10. Roberts, N. A., Martin, J. A., Kinchington, D., Broakhurst, A. V., Craig, J. C., Duncan, I. B., Galpin, S. A., Handa, B. K., Kay, V., Krohn, A., Lambert, R. W., Merrett, J. H., Mills, J. S., Parkes, K. E. B., Redshaw, S., Ritchie, A. J., Taylor, D. L., Thomas, G. J. & Machin, P. J. (1990) Science 248, 358-361.
11. Schroeder, E., Phillips, C., Garman, E., Harlos, K. & Crawford, C. (1993) FEBS Lett. 315, 38-42.
12. Yamashita, D. S., Smith, W. W., Zhao, B., Janson, C. A., Tomaszek, T. A., et al. (1997) J. Am. Chem. Soc. 119, 11351-11352.
13. Nowick, J. S., Holmes, D. L., Noranha, G., Smith, E. M., Nguyen, T. M. & Huang, S.-L. (1996) J. Org. Chem. 61, 3929-3934.
14. Bromme, D., Bonneau, P. R., Lachance, P., Wiederanders, B., Kirschke, H., Peters, C., Thomas, D. Y., Storer, A. C. & Vernet, T. (1993) J. Biol. Chem. 268, 4832-4838.
15. Votta, B., Levy, M. A., Badger, A., Bradbeer, J., Dodds, R. A., James, I. E., Thompson, S., Bossard, M. J., Carr, T., Connor, J. R., Tomaszek, T. A., Szewczuk, L., Drake, F. H., Veber, D. F. & Gowen, M. (1997) J. Bone Miner. Res. 12, 1396-1406.
16. Zhao, B, Janson, C. A., Amegadzie, B. Y., D'Alessio, K., Griffin, C., Hanning, C. R., Jones, C., Kurdyla, J., McQueney, M., Qiu, X., Smith, W. W. & Abdel-Meguid, S. S. (1997) Nat. Struct. Biol. 4, 109-111.
17. Foged, N. T., Delaisse, J.-M., Hou, P., Sato, T., Winding, B. & Bonde, M. (1996) J. Bone Miner. Res. 11, 226-237.
18. Suga, T., Izumi, S. & Hirata, T. (1986) Chem. Lett. 12, 2053-2056.
19. Laskowski, M. (1986) Adv. Exp. Med. Biol. 199, 1-17.
20. Thompson, S. K., Murthy, K. H. M., Zhao, B., Winborne, E., Green, D. W., Fisher, S. M., DesJarlais, R. L., Tomaszek, T. A., Meek, T. D., Gleason, J. G. & Abdel-Meguid, S. S. (1994) J. Med. Chem. 37, 3100-3107.
21. Thompsons, K., Eppley, A. M., Frazee, J. S., Darcy, M. G., Lum, R. T., Tomaszek, T. A., Ivanoff, L. A., Morris, J. F., Sternberg, E. J., Lambert, D. M., Fernandez, A. V., Petteway, S. R., Meek, T. D., Metcalf, B. W. & Gleason, J. G. (1994) Biomed. Chem. Lett. 4, 2441-2446.
22. Li, R., Gong, B., Selzer, P. M., Li, Z., Davidson, E., Kursban, G., Miller, R. E., Nuzum, E. D., McKerrow, J. H., Fletterick, R. J., Gillmor, S. A., Craik, C. S., Kuntz, I. D., Cohen, F. E. & Kenyon, G. L. (1996) Biomed. Chem. 4, 1421-1427.
23. Li, Z., Chen, X., Davidson, E., Zwang, O., Mendis, C., Ring, C. S., Roush, W. R., Fegley, G., Li, R., Rosenthal, P. J., Lee, G. K., Kenyon, G., Kuntz, I. D. & Cohen, F. E. (1994) Chem. Biol. 1, 31-37.
24. Fink, A. L. & Petsko, G. A. (1981) Adv. Enzymol. Relat. Areas Mol. Biol. 52, 177-246.
25. Petsko, G. A. (1992) Philos. Trans. R. Soc. London, Ser. A 340, 323-334.
26. Thompson, D. D., Seedor, J. G., Fisher, J. E., Rosenblatt, M. & Rodan, G. A. (1988) Proc. Natl. Acad. Sci. USA 85, 5673-5677.