Aspartic protease inhibitors as drug candidates for treating various difficult-to-treat diseases

Aspartic proteases are important molecular targets for developing drugs to treat various difficult-to-treat diseases. The aspartic proteases, HIV protease and plasmepsins, are essential for the survival of the virus and malaria parasite, respectively, and AIDS and malaria are counted in two of three major infectious diseases. Renin and β-secretase that are also a class of aspartic proteases are the promising molecular targets for developing hypertension and Alzheimer's disease drugs, respectively. We have developed aspartic protease inhibitors with a transition-state analogue as drug candidates against these difficult-to-treat diseases, hypertension, AIDS, adult T-cell leukemia (ATL), human T-lymphotropic virus type I-associated myelopathy (HAM), malaria, and Alzheimer's disease. Here, we describe our recent drug discovery study on aspartic protease inhibitors.