Easy strategy to protect antimicrobial peptides from fast degradation in serum

Antimicrob Agents Chemother. 2010 Sep;54(9):4003-5. doi: 10.1128/AAC.00300-10. Epub 2010 Jun 28.

Abstract

Antimicrobial peptides are promising novel peptide leads, but their low serum stability often limits their further consideration in drug development programs. Here, we describe a generally applicable strategy to stabilize peptides against serum proteases by replacing arginine residues with alpha-amino-3-guanidino-propionic acid (Agp). Peptide NH(2)-RRWRIVVIRVRR-CONH(2) was nearby totally degraded after 8 h in mouse serum, whereas the variant with Agp substituted was degraded less than 20%. The antimicrobial activity was not affected.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry*
  • Anti-Infective Agents / pharmacology
  • Antimicrobial Cationic Peptides / chemical synthesis*
  • Antimicrobial Cationic Peptides / chemistry*
  • Antimicrobial Cationic Peptides / pharmacology
  • Arginine / chemistry
  • Drug Stability
  • Mice
  • Microbial Sensitivity Tests
  • Serum / chemistry

Substances

  • Anti-Infective Agents
  • Antimicrobial Cationic Peptides
  • Arginine