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Award to help push boundaries of drug discovery

BY: MELISSA MARINO

8/12/2010 - Stephen Fesik, Ph.D., has been awarded a National Institutes of Health Director's Pioneer Award for his proposal to push the boundaries of drug discovery.

Fesik, the Orrin H. Ingram II Chair in Cancer Research, is the first investigator from Vanderbilt to receive this coveted award.

Stephen Fesik, Ph.D.

Stephen Fesik, Ph.D.

The 17 researchers honored this year join the 81 other investigators who have received these awards since the program began in 2004.

The award provides $2.5 million in direct costs over five years.

Fesik — a member of the Vanderbilt-Ingram Cancer Center, the Vanderbilt Institute of Chemical Biology, and the Center for Structural Biology and professor of Biochemistry, Pharmacology and Chemistry — plans to use these funds to develop new approaches for discovering drugs to target proteins currently considered “undruggable.”

Only about 10 percent of proteins encoded by the human genome are thought to be druggable, or able to be modulated by small-molecule drugs. The remaining “undruggable” targets include proteins involved in protein-protein interactions, which play a central role in nearly all signaling processes in a cell and, therefore, could represent important drug targets.

But targeting these challenging proteins will require a new set of tools beyond those traditionally used in drug discovery. Fesik plans to develop the needed methods by employing fragment-based methods.

This approach involves screening small chemical fragments for their ability to bind to small pockets on a protein target and linking the chemical fragments together guided by structural information on how they bind.

In addition to establishing the approaches for drugging challenging targets, Fesik also plans to examine what molecular features make a molecule “drug-like,” safe, and orally bioavailable.

The Fesik group is applying these methods first to highly validated cancer targets. If successful, the strategy could have a major impact on cancer therapies. The methods being developed could also have even more widespread importance.

“Expanding the 'druggable genome' could allow more drugs to be obtained against new targets and improve our ability to treat disease in all therapeutic areas,” Fesik said.

The research could “revolutionize our approach to drug discovery and have a dramatic impact on human health.”

The Pioneer Award is “designed to support individual scientists of exceptional creativity who propose pioneering — and possibly transforming approaches — to major challenges in biomedical and behavioral research,” according to the NIH website.

“Having served on the (selection) committee previously, I know that the competition is extraordinary,” said Jeff Balser, M.D., Ph.D., vice chancellor for Health Affairs, who chaired the Pioneer Award review committee in 2007.

“This award is a great honor for Steve and for Vanderbilt and is further evidence that our faculty are among the most innovative thinkers in the nation.”

“NIH is pleased to be supporting scientists from across the country who are taking considered risks in a wide range of areas in order to accelerate research,” said NIH Director Francis S. Collins, M.D., Ph.D. “We look forward to the results of their work.”

More information on the Pioneer Award is at http://nihroadmap.nih.gov/pioneer.

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