Synthetic approaches to peptide drug design

Peptide drugs are an increasingly important class of therapeutic agents, often exhibiting higher target affinity and fewer side effects in comparison to their small molecule counterparts.  Despite such promising bioactivity, peptide therapeutics are plagued by their susceptibility to proteolytic degradation, poor oral bioavailability, and limited cell permeability. We are interested in probing new synthetic strategies, including macrocyclization, peptide stapling, and chemoselective backbone modifications, to enhance the drug-like properties of bioactive peptides. Multi-disciplinary projects will involve solution- and solid-phase organic synthesis, structural and computational analysis, and biological screening of peptide analogues.