Scripps Florida Logo

Metabolism and Aging - Faculty

Philip Lo Grasso, Ph.D.

Professor
July 2005 - Present
Department of Molecular Therapeutics
Florida Campus
Laboratory Website
lograsso@scripps.edu
(561) 228-2230

Scripps Research Joint Appointments

Professor, Department of Metabolism & Aging
Sr. Scientific Director, Discovery Biology, Translational Research Institute

Other Joint Appointments

Adjunct Professor, Department of Pharmacology, University of Florida

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.

Education

M.S., Biochemistry, The Florida State University, 1988
B.A., Chemistry, New York University, 1985
Ph.D., Pharmacology, University of Florida, 1992

Selected References

Crocker C, Khan S, Cameron M, Robertson H, Robertson G and LoGrasso P. 2011. JNK Inhibition Protects Dopamine Neurons and Provides Behavioral Improvement in a Rat 6-Hydroxydopamine Model of Parkinson's Disease. ACS Chemical Neuroscience, Feb 7; 2 (4), pp. 207-212

Chambers J, Pachori A, Howard S, Ganno M, Hansen Jr. D, Kamenecka T, Song X, Duckett D, Chen W, Ling YY, Cherry L, Cameron M, Lin L, Ruiz C and LoGrasso P. 2011. Small Molecule c-jun-N-Terminal Kinase Inhibitors Protect Dopaminergic Neurons in a Model of Parkinson's Disease. ACS Chemical Neuroscience, Feb 7; 2 (4), pp. 198-206

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, Schürer, 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.