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."