The effect of charge increase on the specificity and activity of a short antimicrobial peptide.
By using short linear antimicrobial peptides as a model system, the effect of peptide charge on the specificity between Candida albicans (fungi) and Gram-positive bacteria was investigated. In a present study, we added and/or deleted lysine residue(s) at the C-terminal and/or N-terminal end(s) of an antimicrobial peptide (KKVVFKVKFK-NH(2)) and synthesized the peptides that had similar alpha helical structures in a lipid membrane mimic condition. The increase of peptide charge improved antifungal activity without the change of antibacterial activity. Structure-activity relationship study about the peptides revealed that the net positive charge must play an important role in the specificity between C. albicans and Gram-positive bacteria and the increase of the net positive charge without the moderate change of secondary structure could improve activity for C. albicans rather than Gram-positive bacteria.
Hong
S Y
SY
Department of Biochemistry, Yonsei University, 134 Shinchon-Dong, Seodaemun-Gu, Seoul 120-749, South Korea.
Park
T G
TG
Lee
K H
KH
D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D023181:Antimicrobial Cationic Peptides / Q000737:chemistry / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects*; D002412:Cations / Q000737:chemistry*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology; D017433:Protein Structure, Secondary; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D023181:Antimicrobial Cationic Peptides; D002412:Cations; D009842:Oligopeptides