Events & Seminars > Event Details


4:00 pm
Room 304, Chemistry Building

Anticancer Discovery from Simple and Complex Compounds


Professor Paul J. Hergenrother
University of Illinois at Urbana-Champaign

Hosted by: Professor Mike Hilinski

 Natural products and their derivatives have long been used as medicinal agents, and they still make up a significant fraction of clinically approved drugs. Recently, the trend in drug discovery is toward compounds that are much simpler than natural products, typically synthetic compounds that have few sp3-hybridized carbons and few stereogenic centers.  While such compounds have value for certain types of targets (e.g., active sites of enzymes that accommodate flat substrates), there are certain targets and disease areas that are best modulated with complex molecules.  This lecture will describe our discovery of a “simple” compound that is entering a human clinical trial for the treatment of cancer, and the use of natural products as the starting point for the synthesis of collections of complex and diverse compounds.  The compounds created through this latter effort have value in many different disease areas.


Biographical Sketch

Paul J. Hergenrother was born in 1972 and raised in Akron, Ohio.  He attended the University of Notre Dame, where he received his B.S. in Chemistry in 1994.  From there Paul moved to the University of Texas at Austin, to conduct graduate research under the direction of Professor Stephen F. Martin.  He graduated with his PhD in Chemistry in 1999, and moved on as an American Cancer Society postdoctoral fellow to Harvard University, working in the laboratory of Professor Stuart L. Schreiber in the Department of Chemistry and Chemical Biology.  He established his own laboratory in the Department of Chemistry at the University of Illinois at Urbana-Champaign in 2001.   The Hergenrother laboratory uses small molecules to identify and validate novel targets for the treatment of intractable diseases, including cancer, degenerative disorders, and multidrug-resistant bacteria.  They discovered the first compound (called PAC-1) to directly activate procaspase-3; PAC-1 has been utilized by many laboratories as a tool for studying procaspase-3 activation, and is entering human clinical trials for the treatment of cancer.  The Hergenrother laboratory also discovered the potent anticancer activity of the natural product deoxynyboquinone (DNQ), and has demonstrated the tremendous selectivity of DNQ for cancer cells.  Recently, the Hergenrother laboratory reported a novel method for rapid construction of complex and diverse compounds starting from natural products.  The hundreds of compounds they have synthesized through this method will no doubt serve as the starting point for future biological discoveries from the Hergenrother laboratory and their many collaborators.