SC13: Introduction to Targeted Covalent Inhibitors
WEDNESDAY, SEPTEMBER 27, 2017 | 7:00 - 9:30 PM
Covalent inhibitors of kinases have re-emerged as a drug design strategy due to more examples of their safety and efficacy in patients. Covalent inhibitors have the advantage of increased selectivity and longer action of duration but there are still important issues about their design and application that need to be better understood. This course will cover practical as well as theoretical issues that a medicinal chemist needs to keep in mind in developing covalent inhibitors.
- Overview of covalent drugs, irreversible and reversible inhibitors including recent clinical examples
- Biochemical analysis of covalent inhibitors
- Design considerations for targeted covalent inhibitors
- De-risking covalent inhibitors
- Mechanism of drug resistance
Instructors:
Brian Gerstenberger, Ph.D., Principal Scientist, Inflammation & Immunology: Medicinal Chemistry, Pfizer Inc.
Mark Schnute, Ph.D., Associate Research Fellow, Biotherapeutics Chemistry & Immunoscience Research, Pfizer Global R&D
Brian Gerstenberger, Ph.D., Principal Scientist, Inflammation & Immunology: Medicinal Chemistry, Pfizer Inc.
Dr. Brian Gerstenberger has ten years experience as a medicinal chemistry in the design and synthesis of drug molecules for immunological, inflammation, epigenetic, and antibacterial indications at Pfizer R&D. He obtained his undergraduate degree at Siena College in New York before moving to University of California at Santa Cruz to gain a Ph.D. During his research career he has author on over twenty research papers and patents. He has made contributions to nomination of clinical candidates including a compounds entering Phase I and II clinical trials. He has also contributed in the Structural Genomic Consortium/Pfizer collaboration leading to the discovery and disclosure a number of tool compounds including PFI-3 for SETD7 and PFI-4 for BRPF1.
Mark Schnute, Ph.D., Associate Research Fellow, Biotherapeutics Chemistry & Immunoscience
Dr. Mark Schnute received his Ph.D. degree in organic chemistry from the University of Illinois at Urbana-Campaign. He then completed a postdoctoral research fellowship at Stanford University. Mark then joined the medicinal chemistry group at Pharmacia. There he led several programs towards the development of antivirals including the advancement a novel broad-spectrum, non-nucleoside herpes antiviral into clinical trials. Mark then joined the Inflammation research group at Pfizer. With Pfizer, his research has focused on the development of treatments for osteoarthritis, rheumatoid arthritis and autoimmune diseases. His areas of interest have been in novel approaches to kinase inhibition and the investigation of modulators for inflammatory lipid signaling pathways.