title: A Biosurfactant-Inspired Heptapeptide with Improved Specificity to Kill MRSA.
abstract: The emergence and rapid spread of methicillin-resistant Staphylococcus aureus (MRSA) poses a serious threat to public health. New antibiotics and strategies are urgently needed to combat S. aureus associated infections. Bacaucin, a novel cyclic lipopeptide from Bacillus subtilis CAU21, is reported. Bacaucin shows broad antibacterial activity against Gram-positive bacteria, but is also hemolytic and cytotoxic. However, bacaucin-1, a bacaucin-inspired ring-opened heptapeptide, shows specific antibacterial activity against MRSA by a membrane-disruptive mechanism without detectable toxicity to mammalian cells or induction of bacterial resistance. Bacaucin-1 was efficient in preventing infections in both in vitro and in vivo models and is a valuable prototype antibiotic with high potential against S. aureus infections.
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, National Center for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University, Yuanmingyuan West Road No.2, Beijing, 100193, China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, National Center for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University, Yuanmingyuan West Road No.2, Beijing, 100193, China.
authors.forename: Shuangyang
authors.initials: S
authors.lastname: Ding
authors.affiliation: Institute of Food Safety, Department of Veterinary Sciences, Ludwig-Maximilians-University Munich, 85764, Oberschleißheim, Germany.
authors.forename: Richard
authors.initials: R
authors.lastname: Dietrich
authors.affiliation: Institute of Food Safety, Department of Veterinary Sciences, Ludwig-Maximilians-University Munich, 85764, Oberschleißheim, Germany.
authors.forename: Erwin
authors.initials: E
authors.lastname: Märtlbauer
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, National Center for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University, Yuanmingyuan West Road No.2, Beijing, 100193, China.|Department of Biomedical Engineering, Duke University, Durham, NC, 27708, USA.
authors.forename: Kui
authors.initials: K
authors.lastname: Zhu
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D001412:Bacillus subtilis / Q000737:chemistry*; D055808:Drug Discovery; D006801:Humans; D055666:Lipopeptides / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D051379:Mice; D008826:Microbial Sensitivity Tests; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D013203:Staphylococcal Infections / Q000188:drug therapy*
chemical_list: D000900:Anti-Bacterial Agents; D055666:Lipopeptides; D010456:Peptides, Cyclic; C009365:surfactin peptide
keywords: MRSA; antibiotics; bacteria; drug discovery; peptides