Structure-based design of AIDS drugs and the development of resistance

AIDS is a major worldwide epidemic spread primarily through contact with infected blood during sexual activity, drug injection, birth, and, rarely now, blood transfusion. More than a dozen drugs for the treatment of AIDS have been introduced in the last 15 years and the process leading to their development offers an excellent example of the progress made in the field of rational drug design. The principal targets of the approved drugs are reverse transcriptase and protease enzymes encoded by the human immunodeficiency virus. In particular, introduction of protease inhibitors has led to a significant decrease of the mortality and morbidity associated with AIDS. My presentation will discuss methods utilized for the development of selected AIDS drugs, primarily protease inhibitors, and the emergence of drug resistance which is presently the greatest challenge in fighting this disease in developed countries.