Tuning the Activity of a Short Arg-Trp Antimicrobial Peptide by Lipidation of a C- or N-Terminal Lysine Side-Chain

被引：73

作者：

Albada, H. Bauke ^{[1
]}

Prochnow, Pascal ^{[2
]}

Bobersky, Sandra ^{[1
]}

Langklotz, Sina ^{[2
]}

Schriek, Patrick ^{[2
]}

Bandow, Julia E. ^{[2
]}

Metzler-Nolte, Nils ^{[1
]}

机构：

[1] Ruhr Univ Bochum, Dept Chem & Biochem, Fac Biol & Biotechnol, D-44780 Bochum, Germany

[2] Ruhr Univ Bochum, Grp Microbial Antibiot Res, Fac Biol & Biotechnol, D-44780 Bochum, Germany

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2012年 / 3卷 / 12期

关键词：

Lipidated antimicrobial peptides; ferrocenoyl; anticancer; nonhemolytic; ANTIBACTERIAL ACTIVITIES; IN-VITRO; RESISTANT;

D O I：

10.1021/ml300148v

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The attachment of lipids to C- or N-terminally positioned lysine side-chain amino groups increases the activity of a short synthetic (Arg-Trp)(3) antimicrobial peptide significantly, making these peptides even active against pathogenic Gram-negative bacteria. Thus, a peptide with strong activity against S. aureus (1.1-2 mu M) and good activity against A. baumannii and P. aeruginosa (9-18 mu M) was identified. The most promising peptide causes 50% hemolysis at 285 mu M and shows some selectivity against human cancer cell lines. Interestingly, the increased activity of ferrocenoylated peptides is mostly due to the lipophilicity of the organometallic fragment.

引用

页码：980 / 984

页数：5

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