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

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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SEP 24, 2014 3:00 PM PDT

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



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