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Wednesday, April 28
12:30 pm Registration
1:30 Chairperson's Opening Remarks
1:40 Discovery of Novel JNK Inhibitors for the Treatment of Parkinson’s Disease
Philip LoGrasso, Ph.D., Professor; Senior Director, Molecular Therapeutics, The Scripps Research Institute
c-jun-N-terminal-kinase 3 is (JNK 3) expressed primarily in the brain and is associated with Parkinson’s disease. In this study we developed highly potent, selective JNK inhibitors which had good brain penetration, good DMPK properties, and showed in vivo efficacy in animal models of Parkinson’s disease. Moreover, compounds developed had plasma:brain ratios of 2:1 or even 1:1 with good DMPK properties in rat. Furthermore, these compounds were shown to be efficacious in the 6-OHDA and MPTP animal models of Parkinson’s disease.
2:10 Talk Title to be Announced
Roderick E. Hubbard, Ph.D., Professor, Research, Vernalis, Ltd. (tentative)
2:40 Targeting the Polo-Box Domain of Polo-Like Knase 1 (Plk1)
Kyung Lee, Ph.D., Senior Investigator, Metabolism, National Cancer Institute
Although development of kinase therapeutics has long been sought, the current prevailing strategy of inhibiting the catalytic activity of the kinases has suffered from a high level of cross-reactivity with other unrelated kinases. Protein-protein interaction inhibitors are thought to be highly specific and, therefore, more amenable for combinatorial therapy with less toxicological problems. However, largely due to the difficulty of finding a right target with a small, well-defined, and unique binding cleft has hampered the development of this class of therapeutic agents. We have identified a 5 amino acid-long peptide and generated high affinity peptidomimetics that specifically bind to and specifically inhibit the non-catalytic, but functionally essential, polo-box domain of Plk1. Our current effort for the generation of a new class of anti-Plk1 PBD inhibitors will be discussed.
3:10 Sponsored Presentations (Opportunity Available)
3:40 Networking Refreshment Break, Poster and Exhibit Viewing
4:20 2-Phenylamino-Pyrimidines: Finding Novel Chemical Space and Charting the Water of Activity/Selectivity in a Mature Scaffold
Xiaolin Li, Ph.D., Research Investigator, Medicinal Chemistry, Genomics Institute of the Novartis Research Foundation
New chemical space in a mature 2-phenylamino-pyrimidine scaffold can be identified for novel cKit/PDGFR inhibitors as potential therapeutics for immunological disorders. Excellent kinase activities and exquisite selectivities were achieved by innovative design and subtle structure modifications. Multi-parameter optimizations were carried out successively to address a range of issues such as pharmacokinetics and potential drug-drug interactions, etc.
4:50 Talk Title to be Announced
Sean G. Buchanan, Ph.D., Senior Research Advisor, Lilly Research Laboratories
520 pm Break-Out Discussions
6:30 End of Day
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