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Fesikís cancer research achievements honored

BY: DAGNY STUART

3/29/2012 - Stephen Fesik, Ph.D., professor of Biochemistry, Pharmacology and Chemistry at Vanderbilt, will receive the 2012 AACR Award for Outstanding Achievement in Chemistry in Cancer Research.

Stephen Fesik, Ph.D.

Stephen Fesik, Ph.D.

Fesik, who holds the Orrin H. Ingram II chair in cancer research, will receive the special recognition during the American Association for Cancer Research (AACR) Annual Meeting in Chicago March 31 - April 4.
He will deliver a special lecture, “Drugging the undruggable using fragment-based methods,” Tuesday, April 3.

“It is a great honor to be recognized by the American Association for Cancer Research, which has a history of contributing to the fight against cancer for over 100 years,” said Fesik. “I appreciate the support of my past and present colleagues who made this award possible. Using fragment-based methods, we hope to discover inhibitors against highly validated but challenging cancer targets.

"Every day, I am inspired by the possibility that our efforts in cancer drug discovery could dramatically improve the lives of millions who are affected by this horrible disease.”

Fesik is being recognized for the use of nuclear magnetic resonance (NMR) to discover novel, potent small molecules capable for use as cancer therapeutics.

He was one of the first researchers to use NMR spectroscopy for cancer drug discovery. He developed many NMR methods and determined the three-dimensional structures of several proteins, especially proteins involved in cell death (apoptosis).

Through the use of his “SAR (structure-activity relationships) by NMR” method, one of the first examples of fragment-based approaches to drug discovery, several inhibitors of protein-protein interactions were discovered.

One of these compounds, ABT-263 (navitoclax), is currently in clinical trials for its ability to inhibit the Bcl-2 family of proteins and subsequently initiate tumor cell death.

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