Advances in the discovery of cathepsin K inhibitors on bone resorption

Jun Lu, Maolin Wang, Ziyue Wang, Zhongqi Fu, Aiping LYU*, Ge ZHANG

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

53 Citations (Scopus)


Cathepsi. (Cat K), highly expressed in osteoclasts, i. cysteine protease member of the cathepsin lysosomal protease family and has been of increasing interest a. target of medicinal chemistry efforts for its role in bone matrix degradation. Inhibition of the Ca. enzyme reduces bone resorption and thus, has rendered the enzyme as an attractive target for anti-resorptive osteoporosis therapy. Over the past decades, considerable efforts have been made to design and develop highly potent, excellently selective and orally applicable Ca. inhibitors. These inhibitors are derived from synthetic compounds or natural products, some of which have passed preclinical studies and are presently in clinical trials at different stages of advancement. In this review, we briefly summarised the historic development of Ca. inhibitors and discussed the relationship between structures of inhibitors and active sites in Ca. for the purpose of guiding future development of inhibitors.

Original languageEnglish
Pages (from-to)890-904
Number of pages15
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Issue number1
Publication statusPublished - 1 Jan 2018

Scopus Subject Areas

  • Pharmacology
  • Drug Discovery

User-Defined Keywords

  • bone resorption
  • cathepsi. inhibitors
  • Cathepsin K
  • osteoclast
  • osteoporosis


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