Protease Inhibitors as Chemotherapeutics

Abstract

Proteolytic enzymes (peptidases or proteases) are involved in a wide range of human pathologies. Therefore, they represent molecular targets for therapeutic intervention, and protease inhibitors are promising chemotherapeutics. These inhibitory drugs are typically developed as small-molecule compounds that block the protease active site. In this area, pharmaceutical research has achieved a number of successes over the past 30 years, and several dozen protease inhibitors are currently used in clinical practice or are in advanced clinical trials. This review focuses on the most important areas of their application, including the treatment of hypertension, diabetes, hepatitis C, AIDS, Alzheimer's disease, and cancer.