Nature Structural Biology
4, 105 - 109 (1997)
doi:10.1038/nsb0297-105
Crystal structure of human cathepsin K complexed with a potent inhibitorMary E. McGrath1, 2, Jeffrey L. Klaus1, Michael G. Barnes1
& Dieter Brömme1
1Arris Pharmaceutical, 385 Oyster Point Blvd., Suite 3, South San Francisco, California 94080, USA
2mcgrath@arris.com The high resolution structure of the new therapeutic target, cathepsin K, complexed with the potent mechanism-based inhibitor, APC3328, reveals the substrate-binding sites of this cysteine proteinase and validates the binding mode for this inhibitor class. REFERENCES
- Delaisse, J.-M. et al. Bone 8, 305−313 (1987). | Article | PubMed | ISI | ChemPort |
- Everts, V., Beertsen, W. & Schröder R Calcif. Tissue Int. 43, 172−178 (1988). | PubMed | ISI | ChemPort |
- Delaisse, J.-M. & Vaes, G. in Biology and Physiology of the Osteoclast (eds. Rifkin, B.R. & Gay, C.V.) 289−314 (CRC Press, Boca Raton, FL, 1992).
- Tezuka, K. et al. J. Biol. Chem. 269, 1106−1109 (1994). | PubMed | ISI | ChemPort |
- Drake, F.H. et al. J. Biol. Chem. 271, 12511−12516 (1996). | Article | PubMed | ISI | ChemPort |
- Brömme, D. & Okamoto, K. Biol. Chem. Hoppe-Seyler 376, 379−384 (1995). | PubMed | ISI |
- Brömme, D., Okamoto, K., Wang, B.B. & Biroc, S. J. Biol. Chem. 271, 2126−2132 (1996). | Article | PubMed | ISI |
- Bossard, M.J. et al. J. Biol. Chem. 271, 12517−12524 (1996). | Article | PubMed | ISI | ChemPort |
- Polymeropoulos, M.H. et al. Nature Genetics 10, 238−239 (1995). | PubMed | ISI | ChemPort |
- Gelb, B.D., Edelson, J.G. & Desnick, R.J. Nature Genetics 10, 235−237 (1995). | PubMed | ISI | ChemPort |
- Gelb, B.D., Shi, G.-P., Chapman, H.A. & Desnick, R.J. Science 273, 1236−1238 (1996). | PubMed | ISI | ChemPort |
- Berti, P.J. & Storer, A.C. J. Mol. Biol. 246, 273−283 (1995). | Article | PubMed | ISI | ChemPort |
- Polgar, L. FEBS Lett. 47, 15−18 (1974). | Article | PubMed | ISI | ChemPort |
- Rullmann, J.A.C., Bellido, M.N. & van Duijnen, P.T. J. Mol. Biol. 206 (1989). | ChemPort |
- Kamphuis, I.G., Kalk, K.H., Swarte, M.B.A. & Drenth, J. J. Mol. Biol. 179, 233−256 (1984). | PubMed | ISI | ChemPort |
- McGrath, M.E. et al. J. Mol. Biol. 247, 251−259 (1995). | Article | PubMed | ISI | ChemPort |
- Musil, D. et al. EMBO J. 10, 2321−2330 (1991). | PubMed | ISI | ChemPort |
- Turk, D. et al. Biochemistry 34, 4791−4797 (1995). | PubMed | ISI | ChemPort |
- Jia, Z. et al. J. Biol. Chem. 270, 5527−5533 (1995). | Article | PubMed | ISI | ChemPort |
- Palmer, J.T., Rasnick, D. & Klaus, J.L. J. Med. Chem. 38, 3193−3196 (1995). | PubMed | ISI | ChemPort |
- Yamamoto, D. et al. J. Biol. Chem. 266, 14771−14777 (1991). | PubMed | ISI | ChemPort |
- Drenth, J., Kalk, K.H. & Swen, H.M. Biochemistry 15, 3731−3738 (1976). | PubMed | ISI | ChemPort |
- Cygler, M. et al. Structure 4, 405−416 (1996). | Article | PubMed | ISI | ChemPort |
- Coulombe, R. et al. EMBO J. 15, 5492−5503 (1996). | PubMed | ISI | ChemPort |
- James, M.N.G. in Keystone Symposium on the Structural and Molecular Biology of Proteinase Function and Inhibition (Sante Fe, New Mexico, 1994).
- Kirschke, H., Wiederanders, B., Brömme, D. & Rinne, A. Biochem. J. 264, 467−473 (1989). | PubMed | ISI | ChemPort |
- Brömme, D. et al. J. Biol. Chem. 268, 4832−4838 (1993). | PubMed | ISI |
- Pickersgill, R.W., Goodenough, P.W., Sumner, I.G. & Collins, M.E. Biochem. J. 254, 235−238 (1988). | PubMed | ISI | ChemPort |
- Taylor, M.A.J. et al. Protein Engng. 7, 1267−1276 (1994). | ChemPort |
- Collaborative Computational Project, Num. 4 Acta Crystallogr. D50, 760−763 (1994). | ChemPort |
- McRee, D.E. Practical Protein Crystallography (Academic Press, New York, 1993).
- Brünger, A.T. X-PLOR Version 3.1, Manual (Yale University, 1992).
- Luthy, R., Bowie, J.U. & Eisenberg, D. Nature 356, 83−85 (1992). | Article | PubMed | ISI | ChemPort |
- Bernstein, F.C. et al. J. Mol. Biol. 112, 535−542 (1977). | PubMed | ISI | ChemPort |
|