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Florida Faculty and Professional Staff
Philip Lo Grasso
Professor
Sr. Scientific Director
Department of Molecular Therapeutics
TSRI - 2005
Joint Appointments Department of Metabolism and Aging, Scripps Florida
Department of Pharmacology, University of Florida
Education
B.A., Chemistry, New York University 1985
M.S., Biochemistry, Florida State University 1988
Ph.D., Pharmacology, University of Florida 1992
Research Focus
The major focus of our research effort is the study of structure function relationships of enzymes (kinases, protease, dehydrogenases) and how this relates to drug discovery of enzyme inhibitors. Of particular current interest is the MAP kinase family member c-jun-N-terminal kinase 3 (JNK3). JNK3 has been shown to play a significant role in neuronal survival and is a viable target for developing drugs to treat neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and stroke. Another kinase that we have interest in is Rho-kinase (ROCK). ROCK is involved in smooth-muscle contraction and has been shown to have therapeutic potential in conditions ranging from angina to spinal cord injury. We utilize molecular biology, protein chemistry, enzymology, cell biology, and structure-based drug design to achieve these goals. A third focus of the lab is in the area of chemical biology. Here we are interested in discovering molecular targets for molecules that have been shown to have activity in anxiety, cancer, and infectious disease.
Selected References
Kamenecka, Ted, Jiang, Rong, Song, Xinyi, Duckett, Derek, Chen, Weimin, Ling, Yuan Yuan, Habel, Jeff, Laughlin, John, D., Chambers, Jeremy, Figuera-Losada, Mariana, Cameron, Michael, D., Lin, Li, Ruiz, Claudia, and LoGrasso, Philip. 2010. Synthesis, Biological Evaluation, X-Ray Structure, and Pharmacokinetics of Aminopyrimidine c-jun-N-terminal Kinase (JNK) Inhibitors. J. Medicinal Chemistry, 53:419-431.
Kamenecka, Ted, Habel, Jeff, Duckett, Derek, Chen, Weimin, Ling, Yuan Yuan, Frackowiak, Bozena, Jiang, Rong, Shin, Youseung, Song, Xinyi, and LoGrasso, Philip. 2009. Structure Activity Relationships and X-Ray Structures Describing the Selectivity of Amino Pyrazole Inhibitors for c-jun-N-terminal Kinase 3 (JNK3) over p38. J. Biol. Chem. 284:12853-12861.
Feng, Yangbo, Yin, Yan, Weiser, Amiee, Griffin, Evelyn, Cameron, Michael, Lin, Li, Ruiz, Claudia, Schurer, Stephan, Inoue, Toshihiro, Rao, Vasanth, Schröter, Thomas, and LoGrasso, Philip. 2008. Discovery of Substituted 4-(Pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as Potent and Highly Selective Rho Kinase (ROCK-II) Inhibitors. J. Medicinal Chemistry, 51: 6642-6645.
Ember, Brian, Kamenecka, Ted, and LoGrasso, Philip. 2008 Kinetic Mechanism and Inhibitor Characterization for c-jun-N-Terminal Kinase 3α1. Biochemistry, 47:3076-3084.
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