Monday, June 17 • 9:00 – 12:00 pm 

Short Course: The Art and Science of Kinases*   

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.

Course Instructors:

Kent D. Stewart, Ph.D., Research Fellow, Structural Biology, AbbVie

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.

Maricel Torrent, Ph.D., Senior Scientist III, Molecular Modeling, AbbVie

Maricel Torrent has over 10 years experience in drug discovery working as a Molecular Modeler in pharma at Merck and Abbott. Scientific contributions to 10 kinase research programs over the last decade. Over 40 research publications and five patent applications covering an array of kinase and non-kinase targets. Invited speaker at internal professional conferences. Expertise in computer-aided drug design and in cross-discipline communication. PhD in Computational Chemistry from University of Girona, Spain. Post-doctoral work in molecular modeling of enzymes and biomolecules at Emory University, Atlanta.

*Separate Registration Required