Day 1 | Day 2
DAY TWO: FRIDAY, OCTOBER 16, 2009
8:00 am Morning Coffee
8:30 Chairperson’s Opening Remarks
8:40 Studying Cell Signal Transduction Pathways by Visualizing Protein Interactions and Phosphorylation in situ Using Fixed Cells and Tissues through the in situ Proximity Ligation Assay
Simon Fredriksson, Ph.D., Chief Scientific Officer, Biomarker Discovery, Olink Bioscience
The in situ proximity ligation assay provides a new means of visualizing intra-cellular signal transduction pathways and for studying drug mechanism of action. This technique utilizes dual recognition of two primary antibodies and converts pair wise proximal binding events into bright fluorescent spots which are digitally countable using a standard fluorescence microscope. Cells natively expressing proteins and also tissue material from pre-clinical studies can be analyzed to quantify the level of which a drug candidate can disrupt a protein-protein interaction or down regulate a specific protein phosphorylation event. Thereby on- and off-target events can be quantified with high precision and specificity. This unique strategy for studying mechanisms of action in real world tissue samples will provide the users with very important information on how to study their drug mechanism in ways not obtainable by any other means.
9:10 Novel High-Throughput Ubiquitination Methodology: Application in Drug Discovery Targeting Ubiquitin Regulatory Pathway
Charitha Madiraju, Ph.D., Post-doctoral Fellow, Drug Discovery, Apoptosis, Immunology, Burnham Institute for Medical Research
A novel high-throughput ubiquitination methodology was developed and will be presented with its applications in drug target identification and discovery of chemicals targeting ubiquitin pathway for treatment of autoimmune diseases that are of clinical significance.
9:40 Sponsored Presentation (Opportunities Available)
10:10 Coffee Break
10:40 Introducing Early SPR Methods into Pipeline Discovery and MOA Screening
Hassan Issafras, Ph.D., Scientist II, XOMA
Characterization of both target protein and antibody mechanism of action (MOA) can facilitate many phases of therapeutic antibody discovery and development, impacting the strategy used for early stage discovery, in vivo proof-of-concept studies, toxicological assessment, clinical trial design and commercial development. Antibody MOA analysis often starts with the development of methods to monitor target activation such as receptor ligand binding and assembly of an activated signaling complex. Surface plasmon resonance (SPR) based methods serve as one of the primary tools for elucidating the biophysical interactions that underlie the mechanisms of target and antibody activation. Due to the unique properties of each antibody-target interaction and specific design goals, there is a continual need to innovate novel assays for each therapeutic antibody project. SPR platforms that offer flexible assay design and relatively high throughput are essential to meet this demand and address the wide range of molecular interactions involved in the development of therapeutic antibodies. SPR instruments with parallel flow cell arrangement allow for comparative side-by-side analysis of multiple antibodies, immobilization conditions, regeneration conditions and antigen concentrations greatly reducing assay development and optimization time. Specific examples of SPR based assays used for mechanism of action studies will be presented.
Sponsored by
11:10 Cellular Target Profiling and Quantitative Phosphoproteomics Reveal Insight into a Drug’s Efficiency and Cellular Mode of Action
Jutta Fritz, Ph.D., MBA, Head, Technology and Business Development, KINAXO Biotechnologies GmbH
Multi-targeted kinase inhibitors have emerged as promising anti-cancer drugs. Due to their broad selectivity, it is particularly challenging to understand their mode of action in a cellular context. Therefore, system-wide approaches integrating drug target identification and global phosphoproteome analysis are essential to gain insight into the inhibitor’s impact on signal transduction. A comprehensive approach using chemical proteomics and quantitative phosphoproteomics reveals a drug’s target profile and allows quantification of phosphorylation patterns in relation to drug administration. This approach allows monitoring of the integration of signaling and might predict potential side effects and point to additional therapeutic applications.
11:40 High Performance Assays and Drug Effectiveness – A Panel Discussion
Moderator: Peter J. Tummino, Ph.D., Senior Director, Biology, Oncology Research & Development, GlaxoSmithKline Pharmaceuticals
Panelists:
Rumin Zhang, Ph.D., Senior Principal Scientist, New Lead Discovery, Schering-Plough Research Institute
David Swinney, Ph.D., Director, Biochemical Pharmacology, Roche Palo Alto
Robert A. Copeland, Ph.D., Executive Vice President & Chief Scientific Officer, Epizyme, Inc.
12:00 pm Close of Mechanism of Action Conference
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Christina Lingham
Cambridge Healthtech Institute
250 First Avenue, Suite 300
Needham, MA 02494
Tel: 781-972-5464
Fax: 781-972-5425
email: clingham@healthtech.com
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781-972-5431
awolfson@healthtech.com