Crystal structure of human cathepsin K complexed with a potent inhibitor

被引:146
作者
McGrath, ME
Klaus, JL
Barnes, MG
Bromme, D
机构
[1] Arris Pharmaceutical, South San Francisco, CA 94080
关键词
D O I
10.1038/nsb0297-105
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
收藏
页码:105 / 109
页数:5
相关论文
共 34 条
  • [1] PROTEIN DATA BANK - COMPUTER-BASED ARCHIVAL FILE FOR MACROMOLECULAR STRUCTURES
    BERNSTEIN, FC
    KOETZLE, TF
    WILLIAMS, GJB
    MEYER, EF
    BRICE, MD
    RODGERS, JR
    KENNARD, O
    SHIMANOUCHI, T
    TASUMI, M
    [J]. JOURNAL OF MOLECULAR BIOLOGY, 1977, 112 (03) : 535 - 542
  • [2] ALIGNMENT PHYLOGENY OF THE PAPAIN SUPERFAMILY OF CYSTEINE PROTEASES
    BERTI, PJ
    STORER, AC
    [J]. JOURNAL OF MOLECULAR BIOLOGY, 1995, 246 (02) : 273 - 283
  • [3] Proteolytic activity of human osteoclast cathepsin K - Expression, purification, activation, and substrate identification
    Bossard, MJ
    Tomaszek, TA
    Thompson, SK
    Amegadzie, BY
    Hanning, CR
    Jones, C
    Kurdyla, JT
    McNulty, DE
    Drake, FH
    Gowen, M
    Levy, MA
    [J]. JOURNAL OF BIOLOGICAL CHEMISTRY, 1996, 271 (21) : 12517 - 12524
  • [4] BROMME D, 1993, J BIOL CHEM, V268, P4832
  • [5] Human cathepsin O-2, a matrix protein-degrading cysteine protease expressed in osteoclasts - Functional expression of human cathepsin O-2 in Spodoptera frugiperda and characterization of the enzyme
    Bromme, D
    Okamoto, K
    Wang, BB
    Biroc, S
    [J]. JOURNAL OF BIOLOGICAL CHEMISTRY, 1996, 271 (04) : 2126 - 2132
  • [6] HUMAN CATHEPSIN O2, A NOVEL CYSTEINE PROTEASE HIGHLY EXPRESSED IN OSTEOCLASTOMAS AND OVARY MOLECULAR-CLONING, SEQUENCING AND TISSUE DISTRIBUTION
    BROMME, D
    OKAMOTO, K
    [J]. BIOLOGICAL CHEMISTRY HOPPE-SEYLER, 1995, 376 (06): : 379 - 384
  • [7] Brunger A.T., 1992, X PLOR VERSION 3 1 M
  • [8] Structure of human procathepsin L reveals the molecular basis of inhibition by the prosegment
    Coulombe, R
    Grochulski, P
    Sivaraman, J
    Menard, R
    Mort, JS
    Cygler, M
    [J]. EMBO JOURNAL, 1996, 15 (20) : 5492 - 5503
  • [9] Structure of rat procathepsin B: Model for inhibition of cysteine protease activity by the proregion
    Cygler, M
    Sivaraman, J
    Grochulski, P
    Coulombe, R
    Storer, AC
    Mort, JS
    [J]. STRUCTURE, 1996, 4 (04) : 405 - 416
  • [10] Delaisse Jean-Marie, 1992, P289