Related Experiment Videos
Side-chain-to-tail thiolactone peptide inhibitors of the staphylococcal quorum-sensing system
R John Scott1, Lu-Yun Lian, S Hanna Muharram
1School of Pharmaceutical Sciences, University of Nottingham, University Park, Nottingham NG7 2RD, UK.
Bioorganic & Medicinal Chemistry Letters
|July 11, 2003
Abstract:
The expression of many staphylococcal virulence factors are regulated by the agr locus via a two-component signal transduction system (TCSTS), which is activated in response to a secreted autoinducer peptide (AIP). By exploiting the unique chemical architecture of the naturally occurring AIP-1, several potent inhibitors of staphylococcal TCSTS were designed and synthesized using either a linear or branched solid-phase approach. These inhibitors are competitive binders and contain the crucial 16-membered side-chain-to-tail thiolactone peptide pharmacophore.