SC5: Chemoproteomics Enabling Drug Discovery

MONDAY, JUNE 2 | 8:00 – 10:45 AM

ABOUT THIS COURSE:

This course explores the use of chemical biology approaches, particularly chemoproteomics, as an avenue for generating new targets and leads for drug discovery. Design, synthesis and applications of activity-based probes, reactivity-based probes, photoaffinity probes and utility of bioorthogonal chemistry in chemoproteomics will be discussed in detail. Case studies highlighting applications of chemoproteomics for target and off-target identification, target engagement and/or selectivity profiling in cells will be reviewed.

WHAT YOU WILL LEARN:

  • Chemical biology approaches as an avenue for new targets and leads
  • Chemoproteomics for target ID, target engagement and/or selectivity profiling in cells
  • Design, synthesis and applications of activity-based probes, reactivity-based probes and photoaffinity probes in chemoproteomics
  • Utility of bioorthogonal chemistry in chemoproteomics
  • Covalent fragment screening for the coupled discovery of targets and leads
  • Choosing the appropriate quantitative MS technique for chemoproteomics: SILAC, ReDiMe, TMT (MS2 or MS3?)
  • Case studies highlighting applications for target and off-target identification

INSTRUCTOR BIOGRAPHY:

Johnson_DougDoug Johnson, PhD, Senior Director, Chemical Biology & Proteomics, Biogen

Douglas Johnson is a Senior Director of Chemical Biology & Proteomics at Biogen in Cambridge, MA. Prior to moving to Biogen, Doug was at Pfizer for 18 years where his most recent position was Senior Scientific Director and Head of Chemical Biology in Cambridge, MA. Prior to Pfizer, Doug was an NIH postdoctoral fellow at Harvard University in the laboratory of Professor David A. Evans. He obtained his Ph.D. in organic chemistry at The Scripps Research Institute under the guidance of Professor Dale L. Boger and graduated summa cum laude from the University of Minnesota with a BS in chemistry. He is an author or inventor on more than 90 publications and patents.

amEnde_ChrisChristopher am Ende, Senior Principal Scientist, Pfizer Inc.

Christopher W. am Ende is the Chemical Biology and Exploratory Project Synthesis lead in the Internal Medicine group at Pfizer. Chris received a B.S. in Biochemistry from the University of Delaware, conducting undergraduate research with Professor Neal J. Zondlo designing lanthanide-binding peptides. He then pursued his graduate studies at Stony Brook University working with Professor Peter J. Tonge where he developed slow, tight binding inhibitors of InhA, the enoyl reductase from M. tuberculosis and under the direction of Kathlyn A. Parker, completed the first total synthesis of the natural product bisabosqual A. He has published >50 journal articles and patents, serves as a steering committee member for the New York Academy of Sciences Chemical Biology Discussion Group and was named American Chemical Society Young Investigator. Additionally, Chris is an Adjunct Assistant Professor of Chemistry at Connecticut College.

Majmudar_JaimeenJaimeen Majmudar, PhD, Principal Scientist, Chemical Biology, Pfizer, Inc.

Jaimeen Majmudar is a Principal Scientist in the Chemical Biology group at Pfizer, Cambridge, MA. Jaimeen joined Pfizer in 2016. Prior to joining Pfizer, Jaimeen was the American Heart Association postdoctoral research fellow at the University of Michigan, where he developed novel chemo-proteomic methods for the detection of redox-mediated PTMs in the laboratory of Prof. Brent Martin. Jaimeen obtained his Ph.D. from Purdue University in 2012 from the laboratory of Prof. Richard A. Gibbs, where he developed inhibitors of Kras modifying enzymes. Jaimeen has published >20 research papers and has contributed to 3 patents. Jaimeen is the 2020 Chair of “Chemical Biology in the Hub” and is a Board member on the organizing committee.