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
相关论文
共 30 条
  • [21] Transcriptional control of the agr-dependent virulence gene regulator, RNAIII, in Staphylococcus aureus
    Morfeldt, E
    Tegmark, K
    Arvidson, S
    [J]. MOLECULAR MICROBIOLOGY, 1996, 21 (06) : 1227 - 1237
  • [22] Staphylococcus aureus agr genotypes with enterotoxin production capabilities can resist neutrophil bactericidal activity
    Mullarky, IK
    Su, C
    Frieze, N
    Park, YH
    Sordillo, LM
    [J]. INFECTION AND IMMUNITY, 2001, 69 (01) : 45 - 51
  • [23] Alpha-toxin and gamma-toxin jointly promote Staphylococcus aureus virulence in murine septic arthritis
    Nilsson, IM
    Hartford, O
    Foster, T
    Tarkowski, N
    [J]. INFECTION AND IMMUNITY, 1999, 67 (03) : 1045 - 1049
  • [24] agr Expression precedes escape of internalized Staphylococcus aureus from the host endosome
    Qazi, SNA
    Counil, E
    Morrissey, J
    Rees, CED
    Cockayne, A
    Winzer, K
    Chan, WC
    Williams, P
    Hill, PJ
    [J]. INFECTION AND IMMUNITY, 2001, 69 (11) : 7074 - 7082
  • [25] Virulence- and antibiotic resistance-associated two-component signal transduction systems of Gram-positive pathogenic bacteria as targets for antimicrobial therapy
    Stephenson, K
    Hoch, JA
    [J]. PHARMACOLOGY & THERAPEUTICS, 2002, 93 (2-3) : 293 - 305
  • [26] S-ALKYLMERCAPTO GROUPS FOR SH-PROTECTION OF CYSTEINE .1. SYNTHESIS AND STABILITY OF SOME S-(ALKYLMERCAPTO)CYSTEINES
    WEBER, U
    HARTTER, P
    [J]. HOPPE-SEYLERS ZEITSCHRIFT FUR PHYSIOLOGISCHE CHEMIE, 1970, 351 (11): : 1384 - +
  • [27] WEINSHENKER NM, 1988, ORG SYNTH, V6, P951
  • [28] WEINSHENKER NM, 1972, TETRAHEDRON LETT, V32, P3281
  • [29] Staphylococcus aureus agr and sar global regulators influence internalization and induction of apoptosis
    Wesson, CA
    Liou, LE
    Todd, KM
    Bohach, GA
    Trumble, WR
    Bayles, KW
    [J]. INFECTION AND IMMUNITY, 1998, 66 (11) : 5238 - 5243
  • [30] WILLIAMS P, 2002, EXPER OPIN THER TAR, V6, P1
123