Crystal structure of HIV-1 protease in complex with VX-478, a potent and orally bioavailable inhibitor of the enzyme

HIV protease is an attractive therapeutic target for the treatment of HIV infection and AIDS, due to its obligatory role in the life cycle of the virus. Of the many in vitro potent HIV protease inhibitors described so far, however, only a few have advanced into clinical trials. Here, we report the structure of HIV-1 protease in complex with VX-478, a potent, low molecular weight, orally bioavailable HIV protease inhibitor currently in advanced preclinical development.