Stephen W. Fesik, professor of biochemistry, pharmocology, and chemistry at the Vanderbilt School of Medicine, presented audience members with a series of proteins that bind to other proteins and may serve as viable treatments for cancer patients in the future at yesterday’s 14th Andrew H. Weinberg Memorial Lecture at Harvard Medical School.
Fesik, who is also a member of the Vanderbilt-Ingram Cancer Center, presented strategies to design potential cancer drugs that work based on protein-protein interactions.
In structure-based drug design, the three-dimensional structure of the designated biological target determines the components of the treatment while fragment-based approaches in drug discovery employ physical techniques to determine how fragments bind to protein targets.
Fesik highlighted the importance of fragment-based approaches and their advantages in the creation of new drugs.
“Fragment-based screening involves highly-focused chemistry,” he said. “It tailors molecules to bind to a protein target of interest and covers more chemical space, while identifying hits not obtained in other screens.”
Fesik said that his research had encountered some skepticism, as other scientists’ previous attempts to create treatments dependent on protein-protein interactions have failed. To combat this perception of the direction his research took, he outlined pre-clinical activities and the multiple approaches to treatment employed in their studies, which he said improved the odds of success.
“We are trying to identify useful lead molecules and compounds in clinical trials,” he said. “My lab is focused on developing improvements in fragment-based approaches and applying them to target proteins involved in protein-protein interactions.”
Fesik’s presentation is part of an annual series named for a young patient at the Harvard affiliate Dana-Farber Cancer Institute who died of a rare muscle tumor. The lectures aim to facilitate discussion between medical professionals, policy-makers, and clinicians about new approaches and theories in cancer treatment.
—Staff writer Barbara B. DePena can be reached at barbara.b.depena@college.harvard.edu.
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