Crystal structure of human osteoclast cathepsin K complex with E-64

The structure of human cathepsin K, a potential target for treatment of osteoporosis, reveals active site differences with homologous cysteine proteinases that should enable the design of cathepsin K selective inhibitors.

[1]  Duncan E. McRee.  4 – PROTEIN CRYSTALLOGRAPHY COOKBOOK , 1993 .

[2]  G. Bilbe,et al.  Molecular cloning of human cDNA for cathepsin K: novel cysteine proteinase predominantly expressed in bone. , 1995, Biochemical and biophysical research communications.

[3]  S. Weiss,et al.  Molecular cloning of human cathepsin O, a novel endoproteinase and homologue of rabbit OC2 , 1995, FEBS letters.

[4]  M. Kumegawa,et al.  Molecular cloning of a possible cysteine proteinase predominantly expressed in osteoclasts. , 1994, The Journal of biological chemistry.

[5]  A. Brunger.  Free R value: a novel statistical quantity for assessing the accuracy of crystal structures. , 1992 .

[6]  R. Ménard,et al.  Structure of human procathepsin L reveals the molecular basis of inhibition by the prosegment. , 1996, The EMBO journal.

[7]  C. Debouck,et al.  Cathepsin K, but Not Cathepsins B, L, or S, Is Abundantly Expressed in Human Osteoclasts (*) , 1996, The Journal of Biological Chemistry.

[8]  B. Gelb,et al.  Pycnodysostosis, a Lysosomal Disease Caused by Cathepsin K Deficiency , 1996, Science.

[9]  N. Xuong,et al.  Crystal structure of an actinidin-E-64 complex. , 1992, Biochemistry.

[10]  D. Brömme,et al.  Human cathepsin O2, a novel cysteine protease highly expressed in osteoclastomas and ovary molecular cloning, sequencing and tissue distribution. , 1995, Biological chemistry Hoppe-Seyler.

[11]  Robert Huber,et al.  The refined 2.15 A X‐ray crystal structure of human liver cathepsin B: the structural basis for its specificity. , 1991, The EMBO journal.

[12]  D. Mcnulty,et al.  Proteolytic Activity of Human Osteoclast Cathepsin K , 1996, The Journal of Biological Chemistry.

[13]  A. Berger,et al.  On the size of the active site in proteases. I. Papain. , 1967, Biochemical and biophysical research communications.

[14]  T. A. Jones,et al.  A graphics model building and refinement system for macromolecules , 1978 .

[15]  D. McRee.  Practical Protein Crystallography , 1993 .

[16]  M. Karplus,et al.  Crystallographic R Factor Refinement by Molecular Dynamics , 1987, Science.

[17]  C. P. Huber,et al.  Crystal structure of a papain-E-64 complex. , 1989, Biochemistry.

[18]  D. Brömme,et al.  Human Cathepsin O2, a Matrix Protein-degrading Cysteine Protease Expressed in Osteoclasts , 1996, The Journal of Biological Chemistry.

[19]  H. Mizuno,et al.  Refined x-ray structure of papain.E-64-c complex at 2.1-A resolution. , 1993, The Journal of biological chemistry.

[20]  K. Tanaka,et al.  Purification and properties of a new cathepsin from rat liver. , 1978, Journal of biochemistry.

[21]  P. Kraulis.  A program to produce both detailed and schematic plots of protein structures , 1991 .