SC11: Introduction to Targeted Covalent Inhibitors

Wednesday, September 23, 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.

Topics to be covered include:

• 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:

Mark Schnute, Ph.D., Associate Research Fellow, Biotherapeutics Chemistry & Immunoscience Research, Pfizer Global R&D

Christoph Zapf, Ph.D., Principal Scientist, Worldwide Medicinal Chemistry, Pfizer Research Labs

Instructor biographies:

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.

Dr. Christoph Zapf is a Principal Scientist in the Biotherapeutics Chemistry department within Worldwide Medicinal Chemistry at Pfizer. One of his main tasks as a Design Chemist is to conceive and deliver new small molecule drug candidates that have the highest chance of survival in the development phase and clinical trials. Christoph received his master’s degree in chemistry in Germany before moving to San Diego in 1998 to pursue his graduate education under the guidance of Prof Murray Goodman at UCSD. After receiving his Ph.D. degree in 2003 he moved to Princeton University where he carried out postdoctoral studies in Total Synthesis in the laboratories of Prof Erik Sorensen. Christoph launched his career in 2005 in the Chemical and Screening Sciences department at Wyeth in Pearl River, NY and was folded into Pfizer’s Worldwide Medicinal Chemistry group following the merger in 2009. Christoph subsequently relocated to Cambridge, Massachusetts where he has worked as a design chemist since 2011. Over the years Christoph has worked on a range of pharmaceutical targets spanning from oncology to antiviral to most recently anti-inflammatory agents.

<<Back to Short Courses