Recent developments in cathepsin K inhibitor design.
Cathepsin K is abundantly and selectively expressed in osteoclasts where it plays a critical role in bone degradation. Cathepsin K inhibitors are the first antiresorptive agents that prevent bone loss while allowing bone formation to continue, thereby enhancing the quality and ultimately the strength of bone. The development of cathepsin K inhibitors requires appropriate cell-based assays and animal models. Advances in reversible cathepsin K inhibitor design from January 2004 are reviewed herein.
Grabowskal
Urszula
U
Medivir UK Ltd, Chesterford Research Park, Little Chesterford, CB10 1XL, UK. urszula.grabowska@medivir.com
Chambers
Timothy J
TJ
Shiroo
Masahiro
M
D000818:Animals; D001862:Bone Resorption / Q000188:drug therapy / Q000201:enzymology; D056657:Cathepsin K; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D015394:Molecular Structure; D010024:Osteoporosis / Q000188:drug therapy / Q000201:enzymology
D004791:Enzyme Inhibitors; D002403:Cathepsins; C534130:CTSK protein, human; D056657:Cathepsin K