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Table 1. Antiviral activity of alloferon, Any-GS and their analogues (IC 50 [μg/ml])PeptidesHHV-1 MCVero cellswild-typeHHV-1HHV-1 MCwild-typeHHV-1HEp-2 cells971PT CVB2wildtypeCVB2alloferon (I) 305.00 479.00 * * * *[Ala 1 ]-alloferon (II)# # # # # #[Lys 1 ]-alloferon (III)147.09 4.95 241.90 230,00 107.04 74,00[Arg 1 ]-alloferon (IV)321.10 928.2 # # 629.33 #Any-GS (V) 235.30 216.60 * * * *[2-5]-Any-GS(VI)[1-4]-Any-GS(VII)[1-3]-Any-GS(VIII)[Arg 1 ]-Any-GS (IX)[Gln 1 ]-Any-GS (X)[Gly 1 ]-Any-GS (XI)[Lys 1 ]-Any-GS (XII)[Ala 1 ]-Any-GS (XIII)469.37 187.17 315.07 166.08 199.45 128.91235.50 371.00 * * * *283.78 198.96 521.66 * 342.03 232.10176.65 58.56 277.40 222.40 217.98 121.08238.95 220.42 214.98 148.45 429.58 346.98410.94 213.64 191.62 102.76 197.92 158.92281.56 409.59 417.52 659.55 275.45 206.93409.47 310.57 90.88 179.97 287.20 138.56* not determined, # without effectMoreover, peptides IX was very active only against 971 PT Coxsackie (IC 50 = 121.08μg/ml) but peptide X was active against wild-type HHV-1 (IC 50 = 148.45 μg/ml).Our results indicate that the antiviral activity of tested peptides depends upon the virusand cell line used. Further studies are planned to elucidate the antiviral mechanism of testedpeptides in different cell-virus models.AcknowledgmentsThis work was supported by the Polish Ministry of Science and Higher Education (Grant No. N N204085638), the University of Wroclaw (Grant No. 2237/W/WCh/09) and by the Medical University ofWarsaw grants AM20/W1 and W2/2008–2009.References1. Chernysh, S., Kim, S.I., Bekker, G., Pleskach, V.A., Filatova, N.A., Anikin, V.B., Platonov, V.G.,Bulet, P. PNAS 99, 12628-12632 (2002).2. Suzuki, K., Minagawa, T., Minakawa, T., Kumagai, T., Naya, S., Endo, Y., Osanai, M., Kuwano, E.J. Insect Physiol. 36, 855-860 (1990).3. Yang, P., Abe, S. Zhao, Y., An, Y., Suzuki, K. J. Insect Biotech. Sericology 73, 7-13 (2004).4. Kuczer, M., Dziubasi, K., Midak-Siewirska, A., Zahorska, R., Łuczak, M., Konopińska, D. J. Pept.Sci. 16, 186-92 (2010).605
<strong>Proceedings</strong> of the 31 st European Peptide SymposiumMichal Lebl, Morten Meldal, Knud J. Jensen, Thomas Hoeg-Jensen (Editors)European Peptide Society, 2010Novel Calpain InhibitorsZoltán Bánóczi 1 , Levente E. Dókus 1 , Ágnes Tantos 2 , Attila Farkas 2 ,Péter Tompa 2 , Péter Friedrich 2 , and Ferenc Hudecz 1,31 Research Group of Peptide Chemistry, Eötvös L. University Hungarian Academy ofSciences, Budapest, Hungary; 2 Institute of Enzymology, Biological Research Center,Hungarian Academic of Sciences, Budapest, Hungary; 3 Department of Organic Chemistry,Eötvös L. University, Budapest 112 POB 32, H-1518, HungaryIntroductionCalpains are intracellular cysteine proteases and are of considerable interest due to theirimplication in numerous physiological events. Besides physiological functions, they play akey role in some well-studied pathological processes. The overactivation of calpains, whichresults in the disorder in Ca 2+ homeostasis, increases the degradation of the enzymesubstrates and could contribute to the development of the Alzheimer and/or Huntingtondiseases and also to death of nervous cells caused by traumatic brain injury, spinal cordinjury [1].One of the main methods to study the calpain function is to inhibit the enzyme.Unfortunately, there is only one specific calpain inhibitor of native origin known, thecalpastatin protein. Other inhibitors, mentioned in the literature, are not specific. Use ofthese inhibitors might confuse the interpretation of the results [2]. The use of calpastatin orits region B as specific inhibitors, is <strong>com</strong>promised by limited cell-penetration. The calpaininhibition may be important not only in the functional studies, but also in blocking ofcalpain overactivation in different diseases. These claims require more selective inhibitors,and trigger intensive research in this field.Results and DiscussionOur aim is to develop new, specific and cell-permeable calpain inhibitor(s), to be used foranalysis of calpain function under different conditions and also for the development ofdrugs to treat different calpain dependent diseases. For this, our plan was to synthesizeazapeptide inhibitors based on the calpain substrate (TPLKSPPPSPR) described by us [3].In these new inhibitors, the Lys residue after which the calpain cleaves the substrate wasreplaced by azaglycine (aGly) moiety. Besides this azapeptide, which is similar to thesubstrate sequence (TPLaGlySPPPSPR), shorter peptides were prepared (TPLaGlySPPPSand TPLaGlySP) to study the role of the amino acids at the C-terminal in inhibition. Forexamining the importance of amino acids in the position P 2 and P 3 aGlySPPPS,TPVaGlySPPPS, TPTaGly-NH 2 -S(Bzl)PPPS(Bzl) MBHA-resin SPPPS, TSLaGlySPPPS andTWLaGlySPPPS azapeptidesBoc-NH-NH 2 , CDI in DMFwere synthesized based on thepreference matrix [3]. TheBoc-NH-NH-CO-NH-S(Bzl)PPPS(Bzl)33% TFA/DCMNH 2 -NH-CO-NH-S(Bzl)PPPS(Bzl)MBHA-resinMBHA-resinazapeptides containing aGly wereproduced by solid phase peptidesynthesis on MBHA resin usingBoc/Bzl strategy (Figure 1). The1. Boc-Leu-OHazaglycine moiety was incorporatedwith the reaction of 1,1’-2. Boc-Pro-OH3. Boc-Thr(Bzl)-OHcarbonyldiimidazole (CDI) and4. Ac 2 OBoc-hydrazide. The cleavedAc-T(Bzl)PL-NH-NH-CO-NH-S(Bzl)PPPS(Bzl)HF/p-cresoleMBHA-resin peptides were purified by RP-HPLC and were characterized byanalytical RP-HPLC and ESI-MSAc-TPL-NH-NH-CO-NH-SPPPS-NH 2(Table 1).Figure 1. Outline of a typical synthesis of azapeptide inhibitorsThe inhibitory effect ofFig. 1. Outline of a typical synthesis of azapeptide peptides was determined ininhibitors.calpain buffer (10 mM HEPES,150 mM NaCl, 1 mM EDTA, 5mM benzamidine, 0.5 mM phenylmethylsulfonyl fluoride, 10 mM -mercaptoethanol, pH606
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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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Page 601 and 602: Proceedings of the 31 st European P
Page 651: Proceedings of the 31 st European P
Page 679 and 680: Subject index(S)-2-(1-adamantyl)gly
Page 681 and 682: chip 18chiral triazine condensing r
Page 683 and 684: heat stress 348helical conformation
Page 685 and 686: O-acyl isopeptide method 112obesity
Page 687 and 688: SH2-ligands 210short collagen-relat
Page 689 and 690: Author indexAboye, Teshome Leta 142
Page 691 and 692: Chi, Hongfang 480Chiche, Laurent 6C
Page 693 and 694: Geronikaki, Athina 444Gessmann, Ren
Page 695 and 696: Kostova, Kalina 528Kotzia, Georgia
Page 697 and 698: Nagata, Koji 162Nagayev, Igor Yu. 5
Page 699 and 700: Salvarese, Nicola 518Sammet, Benedi
Page 701 and 702: Vauquelin, Georges 138Veiga, Ana Sa
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