Discovery of potent antimicrobial peptide analogs of Ixosin-B

Antimicrobial peptides (AMPs) are recognized as a potential alternative class of antimicrobial agents because of their selectivity for prokaryotic cells and promise of minimizing the development of bacterial resistance. We developed a lead 11-mer peptide, KRLRRVWRRWR-amide (Fig. 1), which exhibited...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-06, Vol.22 (12), p.4185-4188
Main Authors: Lung, Feng-Di T., Wang, Kai-Shiuan, Liao, Zih-Jie, Hsu, Sheng-Kai, Song, Fei-Yi, Liou, Chien-Chung, Wu, Yu-Shan
Format: Article
Language:English
Subjects:
amides
Amino Acid Sequence
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Antimicrobial activity
Antimicrobial agents
Antimicrobial Cationic Peptides - chemical synthesis
Antimicrobial Cationic Peptides - pharmacology
Antimicrobial peptides
Biological and medical sciences
Erythrocytes
Erythrocytes - drug effects
Escherichia coli
Escherichia coli - drug effects
Escherichia coli - growth & development
Hemolysis
Hemolytic activity
Infection
Ixosin-B
Medical sciences
Microbial Sensitivity Tests
Microbial Viability - drug effects
Molecular Sequence Data
Pathogens
Pharmacology. Drug treatments
Protein Structure, Secondary
Pseudomonas aeruginosa
Pseudomonas aeruginosa - drug effects
Pseudomonas aeruginosa - growth & development
Staphylococcus aureus
Staphylococcus aureus - drug effects
Staphylococcus aureus - growth & development
Structure-Activity Relationship
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Summary:Antimicrobial peptides (AMPs) are recognized as a potential alternative class of antimicrobial agents because of their selectivity for prokaryotic cells and promise of minimizing the development of bacterial resistance. We developed a lead 11-mer peptide, KRLRRVWRRWR-amide (Fig. 1), which exhibited potent antimicrobial activity and no hemolytic activity. Antimicrobial peptides (AMPs) represent the first defense line against infection when organisms are infected by pathogens. These peptides are generally good targets for the development of antimicrobial agents. Peptide amide analogs of Ixosin-B, an antimicrobial peptide with amino acid sequence of QLKVDLWGTRSGIQPEQHSSGKSDVRRWRSRY, were designed, synthesized and examined for antimicrobial activities against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. Within the peptides synthesized, we discovered an 11-mer peptide, KRLRRVWRRWR-amide, which exhibited potent antimicrobial activity while very little hemolytic activity in human erythrocytes was observed even at high dose level (100μM). With further modifications, this peptide could be developed into a potent antimicrobial agent in the future.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.04.018