Side-chain-to-tail thiolactone peptide inhibitors of the staphylococcal quorum-sensing system

Scott, R. John; Lian, Lu Yun; Muharram, S. Hanna; Cockayne, Alan; Wood, Stewart J.; Bycroft, Barrie W.; Williams, Paul; Chan, Weng C.

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. © 2003 Elsevier Ltd. All rights reserved.

Citation

Scott, R. J., Lian, L. Y., Muharram, S. H., Cockayne, A., Wood, S. J., Bycroft, B. W., Williams, P., & Chan, W. C. (2003). Side-chain-to-tail thiolactone peptide inhibitors of the staphylococcal quorum-sensing system. Bioorganic and Medicinal Chemistry Letters, 13(15), 2449-2453. https://doi.org/10.1016/S0960-894X%2803%2900497-9

• Journal Article Type: Article
• Acceptance Date: May 15, 2003
• Online Publication Date: Jun 20, 2003
• Publication Date: Aug 4, 2003
• Deposit Date: Sep 10, 2020
• Journal: Bioorganic and Medicinal Chemistry Letters
• Print ISSN: 0960-894X
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 13
• Issue: 15
• Pages: 2449-2453
• DOI: https://doi.org/10.1016/S0960-894X%2803%2900497-9
• Public URL: https://nottingham-repository.worktribe.com/output/3105713
• Publisher URL: https://www.sciencedirect.com/science/article/abs/pii/S0960894X03004979?via%3Dihub