Author/Authors :
R. John Scott، نويسنده , , Lu-Yun Lian، نويسنده , , S. Hanna Muharram، نويسنده , , Alan Cockayne، نويسنده , , Stewart J. Wood، نويسنده , , Barrie W. Bycroft، نويسنده , , Paul Williams، نويسنده , , Weng C. Chan، نويسنده ,
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.
