SEP 24, 2014 3:00 PM PDT

Site-directed ligand discovery for cryptic sites and other challenging targets

Speaker
  • Associate Director of Biology at the Small Molecule Discovery Center, Assistant Adjunct Professor in the Department of Pharmaceutical Chemistry at UCSF
    Biography
      Michelle Arkin is the Associate Director of Biology at the Small Molecule Discovery Center (SMDC) and Assistant Adjunct Professor in the Department of Pharmaceutical Chemistry at UCSF. She directs the high-throughput screening facility at the SMDC and engages in small-molecule discovery research. Michelle's research interests focus on developing innovative approaches to tackle challenging targets (such as protein-protein interfaces and allostery) and orphan/neglected diseases, including infectious and neurodegenerative diseases. Michelle received her PhD in chemistry at Caltech and then held a Daymon Runyon Cancer Foundation postdoctoral fellowship at Genentech. She was among the first scientists at Sunesis Pharmaceuticals, where she helped to develop fragment-based approaches for inhibiting protein-protein interactions and biophysical tools to characterize protein/small-molecule interactions. From 2005 to 2007, she was the Associate Director of Cell Biology at Sunesis and led the translational science team for Voreloxin, an anti-cancer agent entering phase 3 clinical trials. 
       

    Abstract

    Protein-protein interactions and allosterically regulated enzymes have been challenging but important targets for probe- and drug discovery. We and others have found that fragment-based lead discovery can provide chemical starting points and furthermore serve as insightful probes of protein conformation. The Tethering method of fragment discovery links thiol containing compounds to specific cysteine residues and therefore serves as a site-directed approach to interrogating cryptic allosteric sites and protein interfaces.


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