Small-molecule Cathepsin K inhibitors: a medicinal chemistry perspective

Cathepsin K (Cat K) is a member of the Cathepsin family and is found in a wide range of tissues. Cat K is involved in the terminal catabolism and recycling of endocytosed proteins, as well as specific cellular processes and a wide range of diseases. It is predominantly expressed in osteoclasts and has potent collagenase activity. Based on its particular structure and biological functions, Cat K inhibitors with precise targeting and good penetration are potential therapeutic approaches for related diseases. In this paper, we introduce the structure and biological functions of Cat K and focus on Cat K inhibitors with therapeutic potential for human diseases.

Cathepsin K; drug design; molecular binding modes; small molecule inhibitors; structure-activity relationships (SAR).