title: Self-assembling lipopeptides with a potent activity against Gram-positive bacteria, including multidrug resistant strains.
abstract: OBJECTIVE
  To explore the potential of de novo designed cyclic lipopeptides and its linear counterparts as antibacterial agents.
  
  
  METHODS
  The lipopeptides were synthesized via solid-phase peptide synthesis and the cyclization was achieved by using succinic acid linker. The antimicrobial activities of the lipopeptides were evaluated in vitro against a variety selection of Gram-negative and Gram-positive bacteria including clinical isolates of multidrug-resistant strains.
  
  
  RESULTS
  The synthesized lipopeptides were able to self-assemble into nanoparticles in an aqueous environment, with three exhibiting potent antibacterial activity against Gram-positive bacteria, including clinically relevant multidrug-resistant bacteria.
  
  
  CONCLUSIONS
  The lead compounds have the potential to be developed as new antibacterials that are effective against Gram-positive bacteria, including multidrug-resistant isolates.
authors.forename: Fazren
authors.initials: F
authors.lastname: Azmi
authors.forename: Alysha G
authors.initials: AG
authors.lastname: Elliott
authors.forename: Zeinab G
authors.initials: ZG
authors.lastname: Khalil
authors.forename: Waleed M
authors.initials: WM
authors.lastname: Hussein
authors.forename: Angela
authors.initials: A
authors.lastname: Kavanagh
authors.forename: Johnny X
authors.initials: JX
authors.lastname: Huang
authors.forename: Michelle
authors.initials: M
authors.lastname: Quezada
authors.forename: Mark A T
authors.initials: MA
authors.lastname: Blaskovich
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Capon
authors.forename: Matthew A
authors.initials: MA
authors.lastname: Cooper
authors.forename: Mariusz
authors.initials: M
authors.lastname: Skwarczynski
authors.forename: Istvan
authors.initials: I
authors.lastname: Toth
mesh_terms: D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D006461:Hemolysis / Q000187:drug effects; D056945:Hep G2 Cells; D006801:Humans; D055666:Lipopeptides / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry* / Q000648:ultrastructure; D008826:Microbial Sensitivity Tests; D046529:Microscopy, Electron, Transmission; D009369:Neoplasms / Q000188:drug therapy
chemical_list: D000900:Anti-Bacterial Agents; D055666:Lipopeptides