April 26, 2017 | 11 am to 12 pm EDT

Sponsored by

Webinar Description:

Profiling the properties of agents for eventual therapeutic utility is an essential part of drug discovery and development. Evaluating the in vitro potency of kinase or epigenetic inhibitors in a wide panel of enzyme assays is critical, not only to guiding SAR knowledge for improving drug design, but also for evaluating selectivity, which has important consequences for both biological activity and safety. Evaluation of the same inhibitors in cellular models yields information on the activity of these inhibitors in a more physiologically relevant environment. Using both enzymatic and cellular assays helps to define how an inhibitor works, the signaling networks affected by it, and its ultimate therapeutic application. 

In our webinar, we will demonstrate the power of evaluating several well-known kinase and epigenetic inhibitors in complementary profiling panel assays to better predict behavior that has implications for clinical activity. Our examples will highlight the need to not only understand an inhibitor’s fundamental activity(ies) at its designated target(s), but also its cellular context, when assessing the maximum potential clinical utility. With careful evaluation of the in vitro enzyme activity profiles of inhibitors using KinaseProfiler™, along with cellular response profiles and genomic biomarker identification using the OncoPanel™ Cell-Based Profiling Service, a more complete picture of their biological activity can be generated. This kind of comprehensive analysis also opens up the possibility for expanding the clinical utility of an existing target, or therapeutic asset, by potential repurposing for other indications.

Learning Objectives:

• Understand the value of both enzymatic and cellular analyses to obtain the most physiologically relevant data for oncology therapeutics in drug discovery
• Navigate the potential impact of both on-target and off-target activities for oncology therapeutics in a cellular context
•  Appreciate how comprehensive enzymatic and cellular data can provide information on the potential repurposing of  therapeutics for other indications

Speaker:

Alastair J. King, Ph.D., Principal Scientist, OncoPanel Group Leader, Eurofins Pharma Discovery Services
Dr. King has over 17 years of research experience, with a focus on oncology drug discovery, cellular assays, and laboratory automation.  After completing his post-doctoral studies in the areas of vision biochemistry and mitogenic pathway signaling, he has held positions of increasing responsibility at SmithKline Beecham, GlaxoSmithKline, Johnson & Johnson, and Eurofins Pharma Discovery Services, where he is currently group leader of the OncoPanel™ Cell-Based Profiling Service.  He has significant experience in assay development across a variety of target types and therapeutic areas, using a broad range of formats for low to high-throughput applications.  Dr. King has led international strategic initiatives and drug discovery teams, including that which discovered dabrafenib (Tafinlar®) for the treatment of metastatic melanoma.  Since his undergraduate studies, where he worked on kinases that regulate protein translation, one of his major interests has been the area of protein phosphorylation and the prosecution of targets within that space for drug discovery.  Dr. King holds a Ph.D. in Biochemistry from the University of Southampton and a B.Sc. in Biochemistry from the University of Bristol.  He is also a member of the American Association for Cancer Research, and has received numerous awards for his work.