Description:
- Antibacterial therapeutic
Abstract
USC researchers engineered novel cyclotide with effective broad-spectrum antibacterial activity against several ESKAPE bacterial strains and clinical isolates. Cyclotides are micro-proteins (˜30 residues long) that have shown remarkable stability, are easily synthesized and have shown good oral bioavailability. They also exhibit a broad array of biological activities such as protease inhibitory, anti-microbial, insecticidal, cytotoxic, anti-HIV, and hormone-like activities.
The most active antibacterial cyclotide was very stable in serum, showed little hemolytic activity and provided protection in vivo in a murine model of P. aeruginosa peritonitis. These results highlight the potential of the cyclotide scaffold for the development of novel antimicrobial therapeutics for the treatment of bacteremia.
Benefit
- Novel engineered cyclotides based on a naturally occurring cyclotide
- Demonstrated activity against MDR ESKAPE bacterial strains
- Showed little hemolytic activity and extremely stable in serum
- Straightforward chemical synthesis
Market Application
The search for novel antimicrobial agents to combat microbial pathogens is intensifying in response to the emergence of rapid drug resistance to current antibiotic therapeutics. In a hospital setting these MDR bacterial strains lead to a multitude of complications among patients. Respiratory failure and septicemia are the leading causes of mortality among hospitalized patients.
Publications
Chem. Eur. J. 2021 Sep 1; 27(49): 12702-1270
Other
US Patent pending