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Table 1. MIC (µM) and hemolytic activity (50 µM) of the Jelleine-I analoguesPeptide S.aureus E.coli % Hemolysis1 H-PFKLSLHL-NH 2 6.25-12.5 1.56 272 H-AFKLSLHL-NH 2 25 3.125 93 H-PFKLALHL-NH 2 25-50 12.5 84 H-AFKLVLHL-NH 2 25 6.25 05 H-AFKLLLHL-NH 2 12.5 25 16 H-AFKLILHL-NH 2 1.56 1.56 07 H-AFKLFLHL-NH 2 12.5 3.125 18 H-AFKLNLHL-NH 2 100 6.25 39 H-AFKLWLHL-NH 2 3.125 6.25 3610 H-XFKLVLHL-NH 2 25 100 011 H-XFKLLLHL-NH 2 12.5 100 312 H-XFKLILHL-NH 2 100 >100 013 H-XFKLFLHL-NH 2 6.25 100 014 H-XFKLNLHL-NH 2 6.25 1.56 4415 H-XFKLWLHL-NH 2 25 - 116 H-XFKLKLHL-NH 2 - 3.125 7Our most promising candidate was [Ala 1 , Ile 5 ] Jelleine-I which displayed improvedMIC-activities towards S. aureus and E. coli (1.56 µM both strains) as compared withJelleine-I, which showed 6.25-12.5 µM and 1.56 µM against S. aureus and E. coli,respectively. Furthermore, [Ala 1 , Ile 5 ] Jelleine-I showed no hemolytic activity.AcknowledgementsJette Petersen and Sophie Andresen are thanked for skilled technical assistance. This work wassupported by the Danish Council for Strategic Research, the Augustinus Foundation, the Frimodt–Heineke Foundation, the Family Hede Nielsen Foundation, the JS Foundation and the Aase & EjnarDanielsens Foundation.References1. Fontana, R., et al. Peptides 25, 919-928 (2004).2. http://www.cmdr.ubc.ca/bobh/methods.htm.3. Ryge,T.S., Hansen, P.R. J. Peptide Science 11,727-734 (2005).377
Proceedings of the 31 st European Peptide SymposiumMichal Lebl, Morten Meldal, Knud J. Jensen, Thomas Hoeg-Jensen (Editors)European Peptide Society, 2010Antimicrobial Activity of Small 3-(2-Naphthyl)-L-AlanineContaining PeptidesPaul R. Hansen 1,3 and Niels-Frimodt Møller 2,31 IGM-Bioorganic Chemistry, Faculty of Life Sciences, University of Copenhagen,Denmark; 2 National Center for Antimicrobials and Infection Control, SSI, Denmark;3 Danish National Center for Antibiotic Research and Development, DenmarkIntroductionAntibiotic-resistant pathogens have become a very serious problem world-wide. Mostalarming is the discovery of Gram-negative Enterobacteriaceae containing New Delhimetallo- -lactamase 1 (NDM-1) which are highly resistant to many antibiotic classes,including -lactams, fluoroquinolones, and aminoglycosides—the main antibiotic classesfor the treatment of Gram-negative infections [1].Antimicrobial peptides (AMPs) are a part of the innate immunity in all multicellularorganisms and are promising lead structures for developing new antimicrobial agents [2].However, AMPs often display undesirable pharmaceutical properties, such as susceptibilityto proteolytic breakdown. This may be circumvented by incorporation of non-standardamino acids into the peptide, such as 3-(2-naphthyl)-L-alanine.In the present study, we investigated the antimicrobial activities of 6 peptidescontaining 3-(2-naphthyl)-L-alanine: H-XFXLKKK-NH 2 (1), H-FXLKKK-NH 2 (2), H-XFLKKK-NH 2 (3), H-XKFKXKLKK-NH 2 (4), H-KFKXKLKK-NH 2 (5), H-XKFKKLKK-NH 2 (6), X being the non-proteinogenic amino acid.Results and DiscussionThe peptides were synthesized using standard Fmoc chemistry, on a TentaGel RAM resin(50 mg, loading 0.24 mmol/g). Activation of the Fmoc amino acids and formation ofpeptide bonds were carried out using DIC and HOBt. All Fmoc amino acids and couplingreagents were used in fourfold excess. Fmoc deprotection was accomplished by treatmentwith 20% piperidine in NMP (1 x 3 min and 1 x 7 minutes). The peptides were cleavedfrom the solid support along with the permanent side chain protection groups usingTFA/H 2 O/TIS/thioanisole (90:5:2.5:2.5: v/v).The crude peptides were purified by preparative HPLC and characterized byMALDI-TOF-MS. A stock peptide solution in 1% DMSO was prepared and theconcentration was determined by amino acid analysis. The peptides were tested againstclinically relevant bacteria and fungi as described previously [3].The MIC of each peptide was determined using a microtitre broth dilution assaymodified from the method of Hancock [4]. Briefly, serial twofold dilutions of the peptideswere made in solutions of 0.2% bovine serum albumin and 0.01% acetic acid in 96-wellpolypropylene microtiter plates in volumes of 50 µL. To each well was added 50 µL of thetest organism in Mueller Hinton Broth to a final concentration of approximately 2×10 5CFU/mL. The plates were incubated overnight at 37°C (two days for the fungi) and theMIC of each peptide was read as the lowest concentration of peptide that inhibited visiblegrowth of the organism. All MIC determinations were performed in duplicate, and are theaverage of three independent determinations.Freshly drawn human erythrocytes in citrate-dextrose-phosphate (CDP) buffer, fromCopenhagen University Hospital were used to determine the hemolytic activity as describedby Ryge and Hansen [5].378
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Peptides 2010Tales of PeptidesProce
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Peptides 2010Tales of PeptidesProce
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IntroductionWe had the distinct hon
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Scientific programIn planning the 3
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31 st EUROPEAN PEPTIDE SYMPOSIUMSep
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published by John Wiley & Sons as a
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The Josef Rudinger AwardThis award
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Young Investigators' SymposiumThe y
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xxiv
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Design of Peptidyl-Inhibitors for G
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Synthetic Antifreeze Glycopeptide A
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Synthesis and Oxidative Folding of
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Convergent Syntheses of Huprp106-12
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Bactericidal Activity of Small Beta
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Bradykinin Analogues Acylated on Th
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Antimicrobial Activity of Small 3-(
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Interaction of Curcumin with A-Synu
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Fluorescent and Luminescent Fusion
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Cellular Expression of the Human An
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2D IR Spectroscopy of Oligopeptides
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large, non-redundant subset of prot
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The aberrantly glucosylated peptide
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Table 1. Proline cis/trans ratios o
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Table 1. Yields, UV-vis absorption
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Table 1. Purity of the targeted tri
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processes are blocked. Interestingl
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(tb4 n ,1 m )MTII(tb1 n ,4 m )MTIIF
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Fig. 2. a) Part of the 400 MHz HR-M
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Once printed, the amino acid partic
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A) PSA, few seconds73B) PSA, 45 min
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short β strands. In contrast, nume
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neg. control Cs9-Rhd MM-218Fig. 2.
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Table 1. The general structure of t
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% ID in the liver 1 h p.i.100908070
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Peptidyl phosphoranes were first re
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obtained from the same sardines and
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MccJ25 variants were produced by si
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Fig. 2. Proposed signaling mechanis
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Table 1. mCD4-HS12 antiviral activi
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Subject index(S)-2-(1-adamantyl)gly
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chip 18chiral triazine condensing r
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heat stress 348helical conformation
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O-acyl isopeptide method 112obesity
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SH2-ligands 210short collagen-relat
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Author indexAboye, Teshome Leta 142
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Chi, Hongfang 480Chiche, Laurent 6C
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Geronikaki, Athina 444Gessmann, Ren
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Kostova, Kalina 528Kotzia, Georgia
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Nagata, Koji 162Nagayev, Igor Yu. 5
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Salvarese, Nicola 518Sammet, Benedi
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Vauquelin, Georges 138Veiga, Ana Sa
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