N-terminal amphipathic helix as a trigger of hemolytic activity in antimicrobial peptides: a case study in latarcins

FEBS Lett. 2009 Jul 21;583(14):2425-8. doi: 10.1016/j.febslet.2009.06.044. Epub 2009 Jun 27.

Abstract

In silico structural analyses of sets of alpha-helical antimicrobial peptides (AMPs) are performed. Differences between hemolytic and non-hemolytic AMPs are revealed in organization of their N-terminal region. A parameter related to hydrophobicity of the N-terminal part is proposed as a measure of the peptide propensity to exhibit hemolytic and other unwanted cytotoxic activities. Based on the information acquired, a rational approach for selective removal of these properties in AMPs is suggested. A proof of concept is gained through engineering specific mutations that resulted in elimination of the hemolytic activity of AMPs (latarcins) while leaving the beneficial antimicrobial effect intact.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antimicrobial Cationic Peptides* / chemistry
  • Antimicrobial Cationic Peptides* / genetics
  • Antimicrobial Cationic Peptides* / metabolism
  • Hemolysis*
  • Molecular Sequence Data
  • Mutation
  • Protein Structure, Secondary*
  • Spider Venoms* / chemistry
  • Spider Venoms* / genetics
  • Spider Venoms* / metabolism

Substances

  • Antimicrobial Cationic Peptides
  • Spider Venoms