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The Boc-Val-Pro-ACV and Boc-Ile-Pro-ACV was dissolved in 20 ml of TFA and stirred at0 ◦ C for 1h to remove the Boc- group. Following removal of the TFA in vacuum, DIPEAwas added to a solution of Val-Pro-ACV or Ile-Pro-ACV and solution stirred for 10 min.Antiviral activityVirus: Herpes simplex virus type 1 (HSV-1), strain DA.Cytotoxicity and anti-herpetic activity against HSV-1 of the newly synthesized dipeptideesters of acyclovir was tested in GMK cells.To exclude non-specific antiviral activities, the derivatives of acyclovir were tested forcytotoxicity on confluent monolayer’s of host cells. The results demonstrate a goodcompatibility of the new acyclovir analogous for the tested cell lines. None of thecompounds inhibited the HSV-1-induced cytopathic effect in GMK cells.In conclusion, novel esters of acyclovir have been synthesized with dipeptide H-Val-Pro-OH and H-Ile-Pro-OH and their antiherpetic activity have been explored.The results in our investigations showed that these modification of acyclovir reducedantiviral effect in comparison with modification of acyclovir with amino acids(valacyclovir).AcknowledgmentsFor the support of this work we are grateful to the National Science Fund of Bulgaria (ContractsVUL-304/07) and South-West University ‘Neofit Rilski’’, Blagoevgrad, Bulgaria (SRP-C2/2010).References1. Dantzig, A.H., Bergin, L. Biochim Biophys Acta. 1027, 211-217 (1990).2. Hashimoto, N., Fujioka, T., Toyoda, T., Muranushi, N., Hirano, K. Pharm. Res. 11, 1448-1451(1994).3. Ganapathy, M.E., Brandsch, M., Prasad, P.D, Ganapathy, V., Leibach, F.H. J. Biol. Chem. 270,25672-25677 (1995).4. Han, H., de Vrueh, R.L., Rhie, J.K., Covitz, K.M, Smith, P.L., Lee, C.P., Oh, D.M., Sadee, W.,Amidon, G.L. Pharm. Res. 15, 1154-1159 (1998).5. Inui, K., Terada, T., Masuda, S., Saito, H. Nephrol. Dial Transplant. 15, 11-13 (2000).6. Lupia, R.H., Ferencz, N., Lertora, J.J., Aggarwal, S.K., George, W.J., Agrawal, K.C. Antimicrob.Agents Chemother. 37, 818-824 (1993).7. Anand, B.S., Nashed, Y.E., Mitra, A.K. Curr. Eye Res. 26,151-163 (2002).8. Tantry, S.J., Vasanthakumar, G., Suresh Babu, V.V. Lett. Peptide Sci. 10, 51-55 (2003).537
Proceedings of the 31 st European Peptide SymposiumMichal Lebl, Morten Meldal, Knud J. Jensen, Thomas Hoeg-Jensen (Editors)European Peptide Society, 2010New SOCS1-KIR Mimetic Peptides Through the Screening ofFocused Simplified Combinatorial LibrariesDaniela Marasco 1,2 , Nunzianna Doti 2 , Pasqualina L. Scognamiglio 1 ,Stefania Madonna 3 , Menotti Ruvo 2 , Carlo Pedone 1,2 ,and Cristina Albanesi 31 Department of Biological Sciences, School of Biotechnological Sciences, University“Federico II”, Naples, 80134, Italy; 2 Institute of Biostructures and Bioimaging –IBB-CNR,Naples, 80134, Italy; 3 IDI-IRCCS, Roma, 00167, ItalyIntroductionSuppressor Of Cytokine Signalling (SOCS) proteins are negative feedback regulators ofseveral pathways involved in immune response, particularly the JAK/STAT (Januskinase/Signal Transducer and Activator of Transcription) [1]. Usually their basal levels arelow, but they can be selectively induced by cytokines, such as IFN . SOCS1 inhibits IFNsignalling for its capacity to bind and inactivate JAK2 protein and consequently to blockthe IFNγ-induced tyrosine phosphorylation of IFN receptor (IFN R) and STAT1activation. It has been demonstrated that keratinocytes avoid the detrimental consequencesof an excessive stimulation by IFN- over-expressing SOCS1 thus hindering the expressionof many pro-inflammatory genes, including those involved in skin diseases, such aspsoriasis and allergic contact dermatitis (ACD) [2]. A three-dimensional model of thecomplex between SOCS-1 and JAK2 [3] shows that the Kinase Inhibitory Region (KIR) ofSOCS-1 protrudes towards the catalytic region of JAK2 and occupies the ATP binding site.In this work we identify new peptides mimicking KIR-SOCS-1 binding activity through anELISA-based screening of a focused simplified combinatorial peptide library [4].Results and DiscussionThrough direct binding ELISAs, we confirmed the ability of KIR region (52-67) of SOCS1to bind to JAK2 catalytic site (1001-1013) both in the phosphorylated (Tyr1007), namedpJAK2, and in the non-phosphorylated form, JAK2) (Figure 1). We quantified thisinteraction in terms of KD values of about 100 µM (Table 1).Then to investigate crucial residues of KIR 52-67 region involved in JAK2recognition, we synthesized Ala-scanning peptides. Their binding capacities to both JAK2peptides were analyzed through direct ELISAs. Data analysis suggested that the keyresidues of KIR for JAK2 recognition are localized in 52-61 region. Then we synthesizedand analyzed the binding properties of this shorter sequence, named New-KIR. ELISAexperiments provided K D values in the low micromolar range. Therefore the deletion of sixamino acids in the C-terminal region of KIR led to new-KIR, able to bind to JAK2 catalyticsite with a 4-fold greater affinity.1.00.8Abs, 490nm0.60.4KIR vs JAK2KIR vs pJAK2CP vs JAK2CP vs pJAK20.20.00 100 200 300 400 500 600 700Peptide concentration, ( M)Fig. 1. ELISA direct binding between KIR peptide 52-67vs JAK2 and p-JAK2.538
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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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