Cathepsin K Inhibitors: Their Potential as Anti-Osteoporosis Agents

Abstract

Since the discovery of cathepsin K, its critical role in the resorption of the organic matrix of bone has been established by the efforts of numerous research groups. The potential use of cathepsin K inhibitors to prevent and treat osteoporosis has spurred drug discovery research at many pharmaceutical companies. Pathological roles in arthritis and atherosclerosis offer other potential therapeutic options. Many thiol reactive groups have been coupled with enzyme recognition sequences to devise potent cathepsin K inhibitors. Multiple cycles of design, synthesis, structure elucidation, and drug property profiling have proved fruitful. These efforts are paying off with cathepsin K inhibitors entering clinical studies. Early human data supports a promising future for this therapeutic class of osteoporosis drugs.