Side-chain-to-tail thiolactone peptide inhibitors of the staphylococcal quorum-sensing system
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, seve...
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Published in | Bioorganic & medicinal chemistry letters Vol. 13; no. 15; pp. 2449 - 2453 |
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Main Authors | , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
04.08.2003
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | 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.
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(03)00497-9 |