Ignite Academic Theater Presentation

Introduction to Disulfide Trapping, a site-directed fragment screening technology

Monday, February 5
1:40 PM - 1:55 PM
Location: Exhibition Theater

The aim of this presentation is to invite collaborations using disulfide-trapping technology to discover small-molecule ligands for challenging drug targets.  Disulfide-trapping (Tethering) is a site-directed fragment-discovery method in which libraries of disulfide-containing fragments are screened for binding to cysteine-containing proteins.  Established applications include discovery of fragments at protein-protein interfaces, stabilizing specific conformations of allosteric proteins, and development of selective, covalent inhibitors of cysteine containing enzymes (including kRas).  New applications include stabilizing protein-protein interactions and discovering molecules that bind to structured RNA.

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Michelle Arkin

Associate Professor, Pharm Chem; co-Director, Small Molecule Discovery Center
University of California - San Francisco

The Small Molecule Discovery Center is a research ‘colaboratory’ that works with academic and biotech investigators to develop small-molecule probes and drug leads. Dr. Arkin’s lab is particularly focused on chemical biology of allosterically regulated enzymes and protein-protein interactions to address mechanisms of neurodegeneration, and cancer. Michelle is as an investigator in the NCI’s Chemical Biology Consortium and the Tau Consortium, an editor of the NIH’s Assay Guidance Manual, and board president of the Academic Drug Discovery Consortium. Prior to UCSF, Michelle was one of the first employees at Sunesis Pharmaceuticals, where she served as project leader for new drug targets in cancer and immunology and associate director of cell biology. She was closely involved in two drug programs currently in humans (vosaroxin, an experimental anticancer agent, and lifitegrast, approved by the FDA in 2016).

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