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

被引：44
作者：
Scott, RJ
Lian, LY
Muharram, SH
Cockayne, A
Wood, SJ
Bycroft, BW
Williams, P
Chan, WC
机构：
[1] Univ Nottingham, Sch Pharmaceut Sci, Nottingham NG7 2RD, England
[2] Univ Nottingham, Inst Infect Immun & Inflammat, Nottingham NG7 2RD, England
[3] Univ Manchester, Inst Sci & Technol, Dept Biomol Sci, Manchester M60 1QD, Lancs, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 15期
基金：
英国医学研究理事会; 英国生物技术与生命科学研究理事会;
关键词：
D O I：
10.1016/S0960-894X(03)00497-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2449 / 2453
页数：5
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