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ClClHNO R 1NHR 1 =CH 2Ph, CH(CH 3) 2 and CH 2CH(CH 3) 2OH NNClClHNO R 1NHR 1 =CH 2Ph, CH(CH 3) 2 and CH 2CH(CH 3) 2OOHFig.Figure1.1.StructureStructure of peptideof peptidefragment linkedfragmentto tacrine moleculelinkedto tacrine molecule.ClClHNO R 1NHR 1 =CH 2Ph, CH(CH 3) 2 или CH 2CH(CH 3) 2Fig. 3. Structure of peptide fragments linkedto 6-aminohexanoic acid.OH NOOHFig. 2. Figure Structure 2. of of peptide peptide fragment fragmentsynthesizedsynthesized.ClClHNO R 1 HNNHR 1 =CH 2Ph, CH(CH 3) 2 and CH 2CH(CH 3) 2OONHFig. 4. Hybrid structures comprising6-aminohexanoic acid linker.Nmethyl esters of 6-aminohexanoic acid linkers were monitored by means of IRspectroscopy (KBr pills, FT-IR sPerkin-Elmer 1600 Series spectrophotometer). All finalcompounds were purified using silica gel flash chromatography using the same systems asthose applied for TLC monitoring.A series of coupling reagents (TCTU, TBTU, DCC and N-cyclohexyl-N-[β-(Nmethylmorpholino)-ethyl-]carbodiimide)were studied in order to obtain the best resultsaccording to yields and purity of final products. Commensurate and best results wereobtained using TCTU and N-cyclohexyl-N-[β-(N-methylmorpholino)-ethyl-]carbodiimide.A kinetic investigations according to AChE et BuChE and biological trials are inprogress.AcknowledgmentsWe would like to thank for a financial support of National Research Fund of Bulgaria, Contract MU-FS-03.References1. Mary, A., Renko, D.Z., Guillou, C., Thal, C. Bioorg. Med. Chem. 6, 1835 (1998).2. Han, S.Y., Sweeney, J.E., Bachman, E.S., Schweiger, E.J., Forloni, G., Coyle, J.T., Davis, B.M.,Joullie, M.M. Eur. J. Med. Chem. 27, 673 (1992).3. Carroll, P., Furst, G.T., Han, S.Y., Joullie, M.M. Bull. Soc. Chim. Fr. 127, 769 (1990).4. Sweetman, S., Martindale, (Eds.) The complete drug reference, 34th ed. London: PharmaceuticalPress, 2004.5. Vezenkov, L., Georgieva, M., Danalev, D., Ivanov, Tch., Ivanova, G. Protein & Peptide Lett. 16,1024-1028 (2009).6. Dovey, H.F., et al. J. Neurochem. 76, 173-181 (2001).303
Proceedings of the 31 st European Peptide SymposiumMichal Lebl, Morten Meldal, Knud J. Jensen, Thomas Hoeg-Jensen (Editors)European Peptide Society, 2010Inhibition of Amyloid Formation in Model PeptidesEnrico Brandenburg 1 , Hans v. Berlepsch 2 , and Beate Koksch 11 Organische Chemie, Institut für Chemie und Biochemie, Freie Universität Berlin,Takustraße 3, 14195, Berlin, Germany; 2 Forschungszentrum für Elektronenmikroskopie,Institut für Chemie und Biochemie, Freie Universität Berlin, Fabeckstraße 36a, 14195,Berlin, GermanyIntroductionMany neurodegenerative diseases such as Alzheimer’s disease, type II diabetes,Parkinson’s disease and Creutzfeldt-Jacob disease, are associated with failure of a peptideor protein to adopt, or remain in, its functional conformational state. Often, these undergo aconformational change from the native and mainly unfolded or particularly helically foldedstate into β-sheet rich, insoluble and fibrillar assemblies, that have a characteristic cross-βstructure.We present the inhibition of amyloid formation in two de novo designed modelpeptides by a third de novo designed α-helical ideal coiled coil peptide. The design of allthree peptides is based on the naturally occurring coiled coil folding motif in which a 26residue primary sequence is characterized by a periodicity of seven residues (heptadrepeat), commonly denoted a to g [1,2].Results and DiscussionBy introducing only a few changes to the primary sequence of an ideal coiled-coil modelpeptide we were able to access a subset of model peptides having dramatically differentbehaviours. Peptide A forms a stable coiled coil with itself at neutral pH and works as aninhibitor of conformational change. The incorporation of three valine residues as β-sheetinducing features leads to peptide B which undergoes a conformational change at neutralpH from an α-helical coiled coil to a β-sheet rich amyloid-like fibril with a twisted ribbonlikemorphology. In contrast, the additional presence of lysine residues in peptide C resultsin a large positively charged domain which destabilizes the α-helical coiled coil. ThisFig. 1. Helical wheel diagram of the model peptides A, B and C.Fig. 2. (a) ThT assay of non-seeded peptide B and (b) seeded peptide B at pH 7.4 afterdifferent incubation times and for different equivalents of A (100µM B, 10µM ThT).304
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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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