Related Experiment Video
Updated: Mar 7, 2026
Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
Published on: January 26, 2016
Rediscovering the octapeptins
Tony Velkov1, Kade D Roberts2, Jian Li3
1Drug Development and Innovation, Drug Delivery, Disposition and Dynamics, Australia. Tony.Velkov@monash.edu.
Abstract:
Covering: 1975 up to the end of 2016The decline in the discovery and development of novel antibiotics has resulted in the emergence of bacteria that are resistant to almost all available antibiotics. Currently, polymyxin B and E (colistin) are being used as the last-line therapy against life-threatening infections, unfortunately resistance to polymyxins in both the community and hospital setting is becoming more common. Octapeptins are structurally related non-ribosomal lipopeptide antibiotics that do not exhibit cross-resistance with polymyxins and have a broader spectrum of activity that includes Gram-positive bacteria. This makes them a precious and finite resource for the development of new antibiotics against these problematic polymyxin-resistant Gram-negative pathogens, in particular Pseudomonas aeruginosa, Acinetobacter baumannii and Klebsiella pneumoniae. This review surveys the progress in understanding octapeptin chemistry, mechanisms of antibacterial activity and biosynthesis. With the lack of cross-resistance and their broad antibacterial activity, the octapeptins represent ideal candidates for the development of a new generation of polymyxin-like lipopeptide antibiotics targeting polymyxin-resistant 'superbugs'.
Insights
Octapeptins are promising lipopeptide antibiotics effective against polymyxin-resistant superbugs. They offer a potential new class of drugs to combat difficult-to-treat Gram-negative infections.
Area of Science:
- Microbiology
- Medicinal Chemistry
- Drug Discovery
Background:
- Declining antibiotic discovery leads to widespread resistance.
- Polymyxins (B and E/colistin) are last-resort treatments but face rising resistance.
- Gram-negative pathogens like Pseudomonas aeruginosa, Acinetobacter baumannii, and Klebsiella pneumoniae are major threats.
Purpose of the Study:
- To review the chemistry, antibacterial mechanisms, and biosynthesis of octapeptins.
- To highlight octapeptins as potential alternatives to polymyxins.
- To explore octapeptins for developing new antibiotics against resistant bacteria.
Main Methods:
- Literature review of studies from 1975 to 2016.
- Analysis of octapeptin structure-activity relationships.
- Examination of biosynthesis pathways and resistance mechanisms.
Main Results:
- Octapeptins are non-ribosomal lipopeptides with a distinct mechanism of action.
- They exhibit no cross-resistance with polymyxins.
- Octapeptins possess broad-spectrum activity, including against Gram-positive bacteria.
Conclusions:
- Octapeptins represent a valuable resource for combating polymyxin-resistant Gram-negative infections.
- Their unique properties make them ideal candidates for a new generation of lipopeptide antibiotics.
- Further development of octapeptins could address the critical need for novel antibacterial agents.
Related Concept Videos
01:33Peptide Identification Using Tandem Mass Spectrometry
This technique helps gather information regarding the protein from which the peptide was obtained and to study the peptides’ amino acid sequence. Identifying peptides from a complex mixture is an important component of the growing field of...
02:43Peptide Bonds