Antibiotic activity of Leu-Lys rich model peptides

To develop novel antibiotic peptides useful as therapeutic drugs, short model peptides rich in Leu and Lys were designed by changing not only the net positive charge by Lys-deletion but also in the hydrophobic helix region by Leu-deletion from a peptide analogue of cecropin A (1-8)-magainin 2 (1-12)...

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Veröffentlicht in:Biotechnology letters 2003-08, Vol.25 (16), p.1305-1310
Hauptverfasser: Park, Yoonkyung, Lee, Dong Gun, Hahm, Kyung-Soo
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container_title Biotechnology letters
container_volume 25
creator Park, Yoonkyung
Lee, Dong Gun
Hahm, Kyung-Soo
description To develop novel antibiotic peptides useful as therapeutic drugs, short model peptides rich in Leu and Lys were designed by changing not only the net positive charge by Lys-deletion but also in the hydrophobic helix region by Leu-deletion from a peptide analogue of cecropin A (1-8)-magainin 2 (1-12) (CA-MA) known as P5. In particular, one peptide (P6), which was obtained by deleting Lys residues (positions 1, 3, 5, 9, 10, 13, 14) and Leu residues (positions 4, 7, 8, 11, 12, 15) and keeping Pro (position 6) and Trp (position 2), showed a strong antimicrobial and antitumor activity at 0.2-3.1 microM without hemolytic activity against human erythrocyte cells. Furthermore, P6 causes significant morphological alterations of the bacterial surfaces at 3.1 microM as shown by scanning electron microscopy.
doi_str_mv 10.1023/A:1024995105208
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subjects Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Anti-Infective Agents - chemical synthesis
Anti-Infective Agents - pharmacology
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Bacteria - drug effects
Bacteria - ultrastructure
Cell Line, Tumor - drug effects
Cell Survival - drug effects
Dose-Response Relationship, Drug
Drug Design
Drug Screening Assays, Antitumor
Erythrocytes
Erythrocytes - drug effects
Fungi - drug effects
Hemolysis - drug effects
Humans
Leucine - chemistry
Leucine - pharmacology
Lysine - chemistry
Lysine - pharmacology
Microbial Sensitivity Tests
Neoplasms - drug therapy
Peptide Fragments
Peptides
Proteins
Scanning electron microscopy
title Antibiotic activity of Leu-Lys rich model peptides
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