PPII Mimics as Probes of the Active Site Occupancy Requirements of Protein Kinases

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The focus of this research involves the synthesis of compounds that mimic the poly-L-proline type II (PPII) conformation. The strategy involves the preparation of proline templated amino acids (PTAAs) that when coupled sequentially populate the PPII conformation in solution. The PPII mimics will then serve as a general scaffold for the synthesis of inhibitors that target at least a subset of protein kinases.With this award, the Organic and Macromolecular Chemistry Program is supporting the research and educational activities of Dr. Jose S. Madalengoitia in the Department of Chemistry at the University of Vermont & State Agricultural College. Professor Madalengoitia will focus his work on developing methods for preparation of protein kinase inhibitors. These inhibitors are useful for unraveling complex signal cascades. This project should have broader impacts for medical science since aberrant protein kinase activity has been linked to many disease states. Also, the project will offer diverse training to undergraduates as well as graduate students.