[Structure-guided molecular-targeting approach for development of AIDS therapeutics]

The development of AIDS therapeutics from the first three dideoxynucleoside reverse transcriptase inhibitors to the most recently approved HIV integrase inhibitor and CCR5 inhibitor employed a structure-guided molecular-targeting approach, which made its swift progress and evolution possible. Indeed, the recent efforts to develop new classes of antiretroviral agents more extensively involve predictive modeling based on crystallography, which has certainly maximized our chances of success. Although we have now faced multiple major problems, which represent the challenges different than those we faced in the development of the first drugs, it is likely that further improved approaches to explore new treatment modalities will enable us to control HIV diseases more efficiently and more