Drug for AIDS Therapy

One of the early research projects undertaken at Argonne National Laboratory’s Advanced Photon Source, was an examination of the Acquired Immune Deficiency Syndrome (AIDS) Human Immunodeficiency Virus, or HIV.

Designing an effective anti-HIV drug requires very precise design: the drug must be highly target-specific—in fact it must exactly fit the particular structure of the target molecule—the ‘lock-and-key requirements’ for drug designers. The design must also be flexible enough to accommodate changes in that structure.

Using X-ray crystallography, researchers found the points of attack of the HIV protease inhibitors – agents that block the breakdown of proteins. Protease inhibitors stop HIV from making new copies of itself by blocking the last step in the process, when the virus attempts to replicate. Out of that discovery came the drug Kaletra®, now the most-prescribed drug in its class for AIDS therapy and a product of Abbott Laboratories, which was one of the earliest users of the Advanced Photon Source.

Abbott Labs is part of the Industrial Macromolecular Crystallography Association (IMCA), which operates one of the beamlines at the Advanced Photon Source through a contract with the Center for Advanced Radiation Sources at The University of Chicago. Researchers took a close-up view of the protein called the HIV protease, revealing the atomic details of how compounds interact with the protein.

The drug Kaletra®, now the most-prescribed drug in its class for AIDS therapy

“Kaletra is a clear example of the positive impact derived from research at our DOE-sponsored facility,” said Murray Gibson, Argonne associate laboratory director for scientific user facilities. “This premier national research facility provides the brightest X-ray beams in the Western Hemisphere to more than 5,000 scientists from around the United States and the world.