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GEN’s editor in chief, John Sterling, interviews life science academic and biotech industry leaders on important research, technology, and trends. These podcasts will keep you informed with all the important details you need.

University of Florida scientists have identified a drug compound that dramatically lowers blood pressure, improves heart function and, in a remarkable finding, prevents damage to the heart and kidneys in rats with persistent hypertension.

Dr. Ostrov, an assistant professor in the department of pathology at the University of Florida College of Medicine, discusses the details of the study. Noting that it has only recently come to be appreciated that angiotensin converting enzyme or ACE and ACE2 play an important role in balancing the activity of each other to maintain normal blood pressure, Dr. Ostrov talks about the search by his team for a compound to boost the activity of ACE2, which the researchers believed would have a beneficial effect on the heart.

He goes on to explain how the use of a supercomputer to process 140,000 prospective drug compounds in a matter of weeks ultimately led to the discovery of the promising lead compound.
X-ray crystallographer David Ostrov, Ph.D., is an assistant professor in the University of Florida College of Medicine’s Department of Pathology, Immunology and Laboratory Medicine. He also is affiliated with the UF Shands Cancer Center. Ostrov and his research team are hard at work designing new drugs for an array of conditions, including many novel therapies for cancer. To do so, they harness the ability of one of the most powerful supercomputers on the planet to process as many as 300,000 potential drug compounds within two hours. Researchers can run a molecular docking program they designed that attempts to fit each prospective compound into selected structural pockets on a target protein that are most vulnerable to attack. The program rotates the compounds in a thousand different orientations to identify which is likely to work best and in what position. The winning candidate, the “lead compound,” can then be synthesized by a chemist, tested in the lab and — if it proves promising — eventually in people. The work has led to numerous grants, publications and patent applications — about 20 patents related to discoveries made using Ostrov’s method have been applied for so far — and more are on the way. And the approach isn’t just used for cancer, but also for heart disease, diabetes, Alzheimer’s and other conditions. Ostrov earned his doctorate at the University of Washington in Seattle and completed a fellowship through the Department of Microbiology and Immunology at the Albert Einstein College of Medicine before joining the UF faculty in 2002. He is a member of the American Crystallographic Association and the American Association of Immunologists.

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