SC6: EMERGING CHEMICAL TOOLS FOR PHENOTYPIC SCREENING AND TARGET DECONVOLUTION

MONDAY, AUGUST 24 | 2:00 - 5:00 PM

This course is designed to provide an introduction as well as best practices on the use of chemical biology probes and assays that have been developed for applications in early drug discovery. Chemists and biologists working in lead generation, assay development, phenotypic screening, target discovery and deconvolution, target engagement and finding mechanism-of-action studies will all benefit from attending this course. The instructors will share their knowledge and expertise and there will be time for open discussion and exchange of ideas.

Topics to be Covered:

• Chemical biology tools and probes for MoA studies
• Constructing annotated chemical sets for effective screening
• Covalent inhibitor discovery
• In-cell cysteine profiling
• Target deconvolution
• Case studies highlighting use of small molecules for target identification and validation

Instructors:

Paul Brennan, PhD, Professor, Medicinal Chemistry, Alzheimer's Research UK, Oxford Drug Discovery Institute, University of Oxford

Paul Brennan received his PhD in organic chemistry from the University of California, Berkeley under the mentorship of Paul Bartlett working on synthetic methodology for combinatorial chemistry and synthesizing inhibitors for new anti-bacterial targets. Following three years of postdoctoral research with Steve Ley in Cambridge University on the total synthesis of rapamycin, Paul returned to California to take a position at Amgen. His research was focused on designing and synthesizing kinase inhibitors for oncology. After two years at Amgen, Paul accepted a position as medicinal chemistry design lead at Pfizer in Sandwich, UK. Over the next six years Paul designed and synthesized compounds for most major drug classes: kinases, GPCR’s, CNS-targets, ion-channels and metabolic enzymes. In 2011 Paul joined the Structural Genomics Consortium as a principal investigator to discover chemical probes for epigenetic proteins. He is currently a Professor of Medicinal Chemistry and head of chemistry of the Alzheimer’s Research UK, Oxford Drug Discovery Institute at the University of Oxford.

Hua Xu, PhD, Associate Director, Chemical Biology Platforms, Cygnal Therapeutics

Hua Xu received his PhD in Chemistry from Stony Brook University. After conducting his post-doctoral research at Albert Einstein College of Medicine, he joined Pfizer as a chemical biologist in 2013, where he led the chemical biology efforts for a number of drug discovery programs in immunology and inflammation, rare diseases, and cardiovascular & metabolic diseases with a focus on target identification and selectivity profiling. Hua is the recipient of 2016 ACS Young Investigator Award. After seven years at Pfizer, he joined Cygnal Therapeutics as an associate director in 2020, and is currently developing and applying novel chemical tools and technologies to advance drug discovery in the field of exoneural biology.

Brent Martin, PhD, Senior Principal Scientist, Chemical Biology/Chemoproteomics, Molecular & Cellular Pharmacology, Janssen R&D 

Brent Martin received his Ph.D. in Pharmacology at the University of California in San Diego, working with Nobel Laureate Professor Roger Tsien, where he developed new chemical strategies for correlated fluorescence and electron microscopy. He then carried out postdoctoral studies with Professor Benjamin Cravatt at the Scripps Research Institute developing new strategies for activity-based profiling, high-throughput screening, and chemical proteomics. As faculty member at the University of Michigan in Ann Arbor, he continued expanding the scope of activity-based profiling methods, while also establishing new bioconjugation reactions to detect and profile protein lipidation, redox modifications, and cysteine occupancy. Brent is the recipient of the NCI Howard Temin K99/R00 award in Cancer Research, the NIH Director’s New Innovator Award, and the NIGMS MIRA Established Investigator Award. As head of Chemical Biology at Janssen, Brent is leading efforts to apply chemical biology approaches to advance drug discovery.

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