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PMID: 9756752 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Identification and characterization of novel antimicrobial decapeptides generated by combinatorial chemistry.

Antimicrobial agents and chemotherapy ·Vol. 42 ·No. 10 ·1998-10-00 ·Pages 2534-41

Hong SY, Oh JE, Kwon M, Choi MJ, Lee JH, Lee BL, Moon HM, Lee KH

Abstract

Novel combinatorial libraries consisting of simplified amino acid sequences were designed to screen for peptides active against the Candida albicans membrane. A novel decapeptide, KKVVFKVKFK, that had a unique primary amino acid sequence was identified in this work. This peptide irreversibly inhibited the growth of C. albicans and showed a broad range of antibacterial activity but no hemolytic activity. Circular dichroism spectra revealed that the predominant secondary structure of this peptide strongly depended on the membrane-mimetic environments; the peptide preferred to form an amphipathic alpha-helical structure in the presence of 50% trifluoroethanol, while it preferred to adopt a distorted alpha-helical structure in the presence of sodium dodecyl sulfate micelles. Experiments in which dye was released from vesicles indicated that this novel antimicrobial peptide killed microorganisms through the action on the membrane as its primary target. Replacement of amino acids in this active decapeptide on the basis of information from the libraries could provide unique information about factors affecting its antimicrobial activity such as its secondary structure, net positive charge, and hydrophobicity.

MeSH Terms
Anti-Bacterial Agents Anti-Infective Agents/pharmacology Antifungal Agents/pharmacology Bacteria/drug effects Candida albicans/drug effects Circular Dichroism Depsipeptides Drug Design Hemolysis/drug effects Oligopeptides/pharmacology Structure-Activity Relationship
Chemicals
Anti-Bacterial Agents Anti-Infective Agents Antifungal Agents Depsipeptides Oligopeptides lysyl-lysyl-valyl-valyl-phenylalanyl-lysyl-valyl-lysyl-phenylalanyl-lysine
Authors & Affiliations
8 authors, click to expand affiliations / ORCID
Hong S Y
Protein Chemistry Laboratory, Mogam Biotechnology Research Institute, Kyunggi-Do, 449-910, Korea.
Oh J E
Kwon M
Choi M J
Lee J H
Lee B L
Moon H M
Lee K H
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Article Info
Journal
Antimicrobial agents and chemotherapy
Abbr.
Antimicrob Agents Chemother
ISSN
0066-4804
DOI
10.1128/AAC.42.10.2534
Published
1998-10-00
Pages
2534-41
Language
English
Region
United States
NLM ID
0315061
PMCID
PMC105883
Subset
IM
External Links
PubMed source DOI: 10.1128/AAC.42.10.2534 PMC Full Text View journal details
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