Short Course: The Art and Science of Kinases
Monday, June 4 9:00 am – 12:00 pm
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 Stewart, Ph.D., Research Fellow, Structural Biology, Abbott & Maricel Torrent, Ph.D., Senior Scientist, Abbott