Prior studies on the natural triterpene betulinic acid (1) led to our discovery and development of Bevirimat (2), a modified triterpene and the first-in-class HIV maturation inhibitor. In these studies, we also discovered that appropriately substituted triterpenes show potent HIV entry inhibition. Thus, the overall goal of this research is to further study modified triterpenes as potent HIV-1 entry inhibitors. We hypothesize that new triterpenes with a pharmacological profile superior to current leads can be identified through structural optimization of current leads or new triterpenes from natural sources. It is highly probable that the preclinical drug candidates generated from this project can be developed to enter clinical trials, and possibly succeeded later on as new anti-HIV drugs targeting viral entry. The hypothesis will be tested and the goal will be achieved through the following specific aims.
|Effective start/end date||9/12/09 → 2/11/11|
- NIH National Institute of Allergy and Infectious Diseases (NIAID)
HIV Fusion Inhibitors
Drug Delivery Systems