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Kinase Inhibitors - Day 3

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7:00am – 6:00pm Registration Open

7:30 Continental Breakfast
Breakout Discussion Sessions

Table 1
Post “Rule of 5” Optimization Paradigms
Gerhard Mueller, Ph.D., Chief Scientific Officer, Proteros Fragments, GmbH

Table 2
The Challenge of Drug Resistance
Jeffrey E. Settleman, M.D., Lorel Schwartz Professor of Medicine, Harvard University Medical School

Table 3
Multitargeted vs Selective Kinase Inhibitors
David Simmons, Ph.D., MBA, Chief Scientific Officer, Cellzome



8:30 Chairperson’s Remarks
Ronan O’Hagan, Ph.D., Group Leader, Target Validation/Biology, AVEO Pharmaceuticals, Inc

8:40 Targeting the PI3K Pathway in Lung Disease
Matt Thomas, Ph.D., Research Investigator, Respiratory Disease Area, Novartis Institutes for Biomedical Research
An assessment of each PI3-kinase isoform as a drug discovery target for respiratory diseases. The rationale for PI3Kα inhibition in the treatment of lung cancer, and PI3Kβ inhibitors in pulmonary thrombotic processes, are balanced with a potential side effect profile affecting metabolism and/or fetal development. Roles for PI3Kδ in inflammatory lung diseases and PI3Kγ in asthma are weighed against the consequences of manipulating key immune cell populations.

9:10 Modeling Sensitivity and Resistance to Kinase Inhibitors in Human Cancer-Derived Cell Lines
Jeffrey E. Settleman, M.D., Lorel Schwartz Professor of Medicine, Harvard University Medical School

9:40 Networking Coffee Break in the Exhibit Hall 

10:40 The Discovery of Potent Selective JAK2 Inhibitors for Treatment of Myeloproliferative Disorders
Chris Burns, Ph.D., Director, Research, Cytopia Research Pty. Ltd. 
The Janus kinases (JAKs), consisting of JAK1, JAK2, JAK3 and TYK2, are an important family of cytoplasmic tyrosine kinases. The JAKs play an essential role in cytokine signal transduction through the phosphorylation of specific STAT proteins. The recent identification of an activating mutation of JAK2 (V617F) being present in >95% of Polycythemia Vera (PV) patients, and >50% of Essential Thrombocythemia (ET) and Myelofibrosis patients has initiated much interest in the discovery and development of selective JAK2 inhibitors as a potential targeted treatment for this patient population.
Using a proprietary molecular modelling capability coupled with structural biology, targeted medicinal chemistry and screening capabilities, we have identified and optimized a series of small molecule ATP-competitive inhibitors of JAK2.  This presentation describes the promising preclinical data for the novel JAK2 inhibitor CYT387, that is now in formal pre-clinical studies.

11:10 NVP-AEB071: Oral and Specific Inhibitor of PKC for the Prevention of Graft Rejection and the Treatment of Autoimmune Diseases
Jürgen Wagner, Ph.D., Director, G.D.C, Novartis, Institutes for Biomedical Research
Inhibition of T-cell activation is the most efficient way to prevent transplant rejection. Among the immunosuppressants currently on the market, only calcineurin inhibitors (CNI) inhibit T-cell activation, but their long term use is associated with side-effects (nephrotoxicity and cardiovascular side effects). NVP-AEB071 is the first LMW inhibitor preventing T-cell activation via a calcineurin-independent pathway. NVP-AEB071 inhibits all classical and novel protein kinase C isotypes. Herein, we present the case story of NVP-AEB071 including the medicinal chemistry approaches, critical PK properties of the compound, preclinical data including in vivo models in rodents and non-human primates as well as positive proof-of-concept results obtained with NVP-AEB071 in psoriasis patients. Finally, we could also discuss the need of inhibition of multiple PKC isotypes versus specific inhibition of individual PKCs, namely PKC theta, alpha or beta, to effectively suppress solid organ graft rejection. Indeed, results obtained with various single or double PKC ko mice in models for transplantation suggest that specific inhibition of single isotypes would not be sufficient for this indication.

11:40 Targeting Protein Kinases in CNS Disorders
D. Martin Watterson, Ph.D.,  J. G. Searle Professor and Co-Director, University Center for Drug Discovery and Chemical Biology, Northwestern University
Protein kinases are well-established therapeutic targets in oncology.  However, drug discovery and development campaigns targeting protein kinases for CNS injury and neurodegenerative diseases have the additional challenge of effective brain penetrance as well as the standard considerations of ADME and safety.  Early stage discovery examples will be discussed.

12:10pm Panel Discussion with Speakers

12:40 Close of Kinase Inhibitors Conference


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view Discovery On Target 2008
Targeting RB