BETHESDA, Md--NCI research from the 1980s, in which scientists used crystallography to study the structure of the human immunodeficiency virus (HIV), paved the way for development of the current crop of HIV-specific protease inhibitors (see " Early Combination Treatment May Provide HIV Control" for a report on clinical trials of protease inhibitors).
Data from crystallization studies were used to develop 3-dimensional models of the enzyme. Researchers were then able to determine the shape a protease inhibitor must have to "fit" into the enzyme's active site and inhibit its function.
The coordinates for the 3-dimensional image were deposited in the Brook-haven National Laboratory database, making the structure available to pharmaceutical companies, who then put their drug design teams to work to develop novel inhibitors.
George VandeWoude, PhD, special advisor to the director of NCI's Division of Basic Sciences, said that the achievement "emphasizes that basic research is worth the effort."