Antimicrobial Peptides Against Bacterial Pathogens

Applications

This technology is a novel antimicrobial peptide with applications as a therapeutic antibiotic drug.

Problem Addressed

Antibiotic resistant bacteria are an urgent threat to modern medicine. Worldwide there are 30 million new antibiotic-resistant infections diagnosed every year and 5 million of these cases will result in death. Furthermore, the emergence of antibiotic resistant bacteria currently outpaces new drug development, and there is therefore a desperate need to develop new antibiotic therapies. Antimicrobial peptides (AMPs) have been proposed as a promising new antibiotic modality. AMPs are small naturally occurring proteins with potent antimicrobial properties; however, most AMPs either display only limited antimicrobial activity or are highly toxic to human cells. This technology is a panel of new rationally-designed AMPs that display both improved toxicity profiles and improved potency.

Technology

This technology is a panel of derivatives of the wasp-derived AMP polybia-CP. While wild type polybia-CP is a potent antimicrobial, it is also highly toxic to human cells. These inventors rationally designed changes that stabilize the helical structures and tune physicochemical properties of the polybia-CP parent compound, which respectively resulted in increased antibiotic activity against bacteria and decreased toxicity in human cells. The two lead compound derivatives are highly effective in treating P. aeruginosa infections in an in vivo mouse model. A single dose of the top polybia-CP derivative is five orders of magnitude more effective than the parent compound and was able to nearly eradicate P. aeruginosa in the skin of infected mice within 4 days.

Advantages

  • Highly effective rationally designed antimicrobial peptide
  • Effective against Gram-positive and Gram-negative bacteria
  • More stable, more effective, and less toxic than the parent antimicrobial peptide