title: Tuning the activity of a short arg-trp antimicrobial Peptide by lipidation of a C- or N-terminal lysine side-chain.
abstract: 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 μM) and good activity against A. baumannii and P. aeruginosa (9-18 μM) was identified. The most promising peptide causes 50% hemolysis at 285 μM 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.
authors.affiliation: Inorganic Chemistry I-Bioinorganic Chemistry, Department of Chemistry and Biochemistry, and Group Microbial Antibiotic Research, Faculty for Biology and Biotechnology, Ruhr University Bochum , Universitätsstrasse 150, 44780 Bochum, Germany.
authors.forename: H Bauke
authors.initials: HB
authors.lastname: Albada
authors.affiliation: Inorganic Chemistry I-Bioinorganic Chemistry, Department of Chemistry and Biochemistry, and Group Microbial Antibiotic Research, Faculty for Biology and Biotechnology, Ruhr University Bochum , Universitätsstrasse 150, 44780 Bochum, Germany.
authors.forename: Pascal
authors.initials: P
authors.lastname: Prochnow
authors.affiliation: Inorganic Chemistry I-Bioinorganic Chemistry, Department of Chemistry and Biochemistry, and Group Microbial Antibiotic Research, Faculty for Biology and Biotechnology, Ruhr University Bochum , Universitätsstrasse 150, 44780 Bochum, Germany.
authors.forename: Sandra
authors.initials: S
authors.lastname: Bobersky
authors.affiliation: Inorganic Chemistry I-Bioinorganic Chemistry, Department of Chemistry and Biochemistry, and Group Microbial Antibiotic Research, Faculty for Biology and Biotechnology, Ruhr University Bochum , Universitätsstrasse 150, 44780 Bochum, Germany.
authors.forename: Sina
authors.initials: S
authors.lastname: Langklotz
authors.affiliation: Inorganic Chemistry I-Bioinorganic Chemistry, Department of Chemistry and Biochemistry, and Group Microbial Antibiotic Research, Faculty for Biology and Biotechnology, Ruhr University Bochum , Universitätsstrasse 150, 44780 Bochum, Germany.
authors.forename: Patrick
authors.initials: P
authors.lastname: Schriek
authors.affiliation: Inorganic Chemistry I-Bioinorganic Chemistry, Department of Chemistry and Biochemistry, and Group Microbial Antibiotic Research, Faculty for Biology and Biotechnology, Ruhr University Bochum , Universitätsstrasse 150, 44780 Bochum, Germany.
authors.forename: Julia E
authors.initials: JE
authors.lastname: Bandow
authors.affiliation: Inorganic Chemistry I-Bioinorganic Chemistry, Department of Chemistry and Biochemistry, and Group Microbial Antibiotic Research, Faculty for Biology and Biotechnology, Ruhr University Bochum , Universitätsstrasse 150, 44780 Bochum, Germany.
authors.forename: Nils
authors.initials: N
authors.lastname: Metzler-Nolte
keywords: Lipidated antimicrobial peptides; anticancer; ferrocenoyl; nonhemolytic