Modular determinants of antimicrobial activity in platelet factor-4 family kinocidins

Biochim Biophys Acta. 2007 Mar;1768(3):609-19. doi: 10.1016/j.bbamem.2006.11.010. Epub 2006 Nov 30.

Abstract

Mammalian platelets contain an array of antimicrobial peptides, termed platelet microbicidal proteins (PMPs). Human and rabbit PMPs include known chemokines, such as platelet factor-4 (hPF-4); PMP-1 is the rabbit orthologue of hPF-4. Chemokines that also exert direct antimicrobial activity have been termed kinocidins. A consensus peptide domain library representing mammalian PF-4 family members was analyzed to define structural domains contributing to antimicrobial activity against a panel of human pathogens. Secondary conformations were assessed by circular dichroism spectrometry, and molecular modeling was employed to investigate structural correlates of antimicrobial efficacy. Antimicrobial activity against isogenic peptide-susceptible or -resistant Staphylococcus aureus, Salmonella typhimurium, and Candida albicans strain pairs mapped to the C-terminal hemimer (38-74) and modular domains thereof (49-63 and 60-74). Increasing electrostatic charge and steric bulk were general correlates of efficacy. Structural data corroborated spatial distribution of charge, steric bulk and putative secondary structure with organism-specific efficacy. Microbicidal efficacies of the cPMP antimicrobial hemimer and C-terminal peptide (60-74) were retained in a complex human-blood biomatrix assay. Collectively, these results suggest that modular determinants arising from structural components acting independently and cooperatively govern the antimicrobial functions of PF-4 family kinocidins against specific target pathogens.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Blood Platelets / chemistry
  • Candida albicans / drug effects
  • Chemokines / chemistry*
  • Chemokines / pharmacology*
  • Circular Dichroism
  • Colony Count, Microbial
  • Dose-Response Relationship, Drug
  • Humans
  • Mass Spectrometry
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Sequence Data
  • Platelet Factor 4 / chemistry*
  • Platelet Factor 4 / pharmacology*
  • Protein Conformation
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Salmonella typhimurium / drug effects
  • Staphylococcus aureus / drug effects
  • Static Electricity
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Chemokines
  • Platelet Factor 4