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Short Course

Monday, June 6 

9:00-12:00 pm Pre-Conference Short Course*

The Art and Science of Kinases –
What You Need to Know
 

Kent StewartInstructor: Kent Stewart, Ph.D., Research Fellow, Department of Structural Biology, Global Pharmaceutical Research and Development, Abbott

This instructional course has been designed for both chemists and biologists who are new to kinase research or have some experience in the field and would like to learn more. The Art and Science of Kinases course will cover topics that are critical to know for any kinase research program. This course will cover;

  • Protein structure; structural basis for “inactive” and “active” (DFG-out/in) forms; active site residues and electrostatics; gatekeeper; hinge, back-pocket.
  • Assays: different formats and readout; factors that control IC50 and Ki; ATP-concentration; off-rate; solubility; reasons for compound success and failure.
  • Inhibitors: approved drugs; inhibitor types; Type1/2; ATP-site directed; allosteric; covalent; hot-spots for ligand potency; common chemotypes.
  • Kinome selectivity: kinomics; visualizing and interpreting heat maps; conserved and variable active-site residues.
  • Technologies: high-throughput screening; fragment-based design; structure-based drug design.
  • Example case studies; late-stage challenges.

 

Instructor Biography: Dr. Kent Stewart has over 27 years experience in drug discovery, including contributions to over 15 kinase research programs at Abbott.  Over 90 research publications in drug research with over 20 devoted to kinase research.  Contributed to 8 candidate compounds, including 3 kinase candidates, with one in advanced clinical evaluation.  Specialist in computer-aided drug design.  Ph.D. in Organic Chemistry from University of California, Los Angeles, and post-doctoral work in biochemistry at the Rockefeller University. 

* Separate Registration Required 


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