The kinase inhibitor field is maturing. This conference is designed to examine the question of what lays ahead, what is in store for the pharmaceutical industry and what new avenues are opening up be in regards to technologies and methods used or in regards to novel targets and therapeutic approaches explored. What novel kinase indications are “out there”, in addition to cancer as a target, what other therapeutic areas are blossoming?
Key issues such as addressing resistance, selectivity versus safety, developing lead compounds, integrating chemistry and biology, using promising techniques such as fragment – and structure based design as well as optimizing PK and PD and how to analyze the flood of data available will be addressed in this conference.
- Strategies for Overcoming Resistance
- Targeting Cancer, Inflammation, Autoimmune Diseases, and CNS
- Conformational Changes in Protein Kinases
- Novel Paths towards Identifying Kinase Inhibitors
- Optimizing Leads and Inhibitors
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