OST -5440, A Small Molecule Inhibitor of Human Cathepsin K, Inhibits Bone Resorption In Vivo as well as In Vitro

  • Kim, H.D. (Research Laboratories, Dong-A Pharmaceutical Co., Ltd.) ;
  • Park, J.H. (Yuhan Research Institut) ;
  • Lee, S.S. (Yuhan Research Institut) ;
  • H, Son-M. (Yuhan Research Institut) ;
  • Y, Kwak-W. (Yuhan Research Institut) ;
  • S, Yang-J. (Yuhan Research Institut) ;
  • I, Lim-J (Yuhan Research Institut) ;
  • Kim, S.H. (Yuhan Research Institut) ;
  • Kim, W.B. (Yuhan Research Institute)
  • Published : 2003.04.01

Abstract

Cathepsin K (CK) is a cysteine protease that plays a major and essential role in osteoclast-mediated degradation of collagen matrix of bone. Its tissue-limited distribution and pivotal contribution to bone resorption meet the requirements as the potential therapeutic target of the disease with excessive bone loss such as osteoporosis. In a search for potent CK inhibitors. we found OST-5440 that effectively inhibited bone resorption in vivo as well as in vitro. (omitted)

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