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Coupling between the mono-6-deoxy-β-cyclodextrin and the side chain-protected GnRHpeptide analogue was performed with the NHS/DCC method in DMF were both reactantsare soluble.At the final step all the protected groups (tert-butyl, trityl and Pbf) were removed bytriturating the final conjugate for 3h with 60% TFA/CH 2 Cl 2 containing triethylsilane asscavenger as shown in the Figure 1.A (GnRH analogue)– β-CD derivative has been successfully synthesized andcharacterized by ESI-MS. Future work will include, synthesis and identification ofpermethylated or not β-Cyclodextrin/GnRH analogues (linear and cyclic ones) usingchromatographic and spectroscopic methods. Moreover, docking simulations of thesynthesized conjugates into a homology modeling-derived structure of the human GnRHreceptor will be performed in order to visualize the potential role of the cyclodextrin moietyin the ligand/receptor interaction. Finally, in vitro experiments will be carried out usingseveral cancer lines in order to evaluate the stability and bioavailability of the conjugatescompared to commercially available GnRH agonists or antagonists.AcknowledgmentsD. Laimou is financial supported by Karatheodoris Grant of University of Patras, GreeceReferences1. Wenz, G. Angew. Chem. 106, 851-870 (1994).2. Bender, Μ.L., Komiyama, M. "Cyclodextrin Chemistry", Springer-Verlag 12, 311-337 (1978).3. Breslow, R., Dong, S.D. Chem. Rev. 98, 1997-2011 (1998).4. Albers, E., Muller, B.W. Critical Reviews in Therapeutic Drug Carrier Systems 12, 311-37 (1995).5. Parrot-Lopez, H., Djedaini, F., Perly, B., Coleman, A.W., Galons, H., Miocque, M. TetrahedronLett. 31, 1999-2002 (1990).6. Baba, Y., Matuso, H., Schally A.V. Biochemic. Biophysic. Res. Commun. 44, 459-463 (1971).7. Evans, R.M., Doelle, G.C., Alexander, A.N., Uderman H.D., Rabin, D. J. Clin. Endoer. Metab. 58,862-867 (1984).8. Mantzourani, E., Laimou, D., Matsoukas, M., Tselios, T. Anti-Inflammatory & Anti-Allergy Agentsin Medicinal Chemistry 13, 294-306 (2008).9. Laimou, D.K., Katsara, M., Matsoukas, M.I., Apostolopoulos, V., Troganis, A.N., Tselios, T.V.Amino Acids March 2010, In press.155
Proceedings of the 31 st European Peptide SymposiumMichal Lebl, Morten Meldal, Knud J. Jensen, Thomas Hoeg-Jensen (Editors)European Peptide Society, 2010Novel Synthesis of Benzophenone Units forPhoto-Affinity LabelingShirly Naveh 1 , Carni Lipson 2 , Michal Breker 3 , Yftah Tal-Gan 1 ,Maya Schuldiner 3 , Michal Sharon 2 , and Chaim Gilon 11 Institute of Chemistry, The Hebrew University of Jerusalem, 91904, Jerusalem, Israel;2 Department of Biological Chemistry, The Weizmann Institute of Science, 76100, Rehovot,Israel; 3 Department of Molecular Genetics, Weizmann Institute of Science,76100, Rehovot, IsraelIntroductionPeptides are a common tool for the study of protein-protein interactions. Benzophenone(BP) is an attractive photo-affinity label which covalently binds to the inactive C-H bondsof the protein, upon exposure to UV irradiation [1]. In order to use BP for the study ofprotein interactions, a peptide-BP conjugate must be synthesized. The addition of BP to thetarget molecule has often proven to be a difficult synthetic step. Here we describe a onepot, two step synthesis of BP units that are compatible with standard solid phase peptidesynthesis procedures. The proximity between the BP moiety and the peptidepharmacophores can affect both binding and activity, thus we developed BP units usingspacers of varying lengths. In addition, the spacer has a dominant effect on the site at whichthe BP binds to the protein, and the use of various lengths enables more complete mappingof the binding site.Results and DiscussionIn order to mainstream the use of BP, we have developed a one pot, two steps synthesis ofBP units suitable for standard solid phase peptide synthesis procedures. The synthesis isbased on coupling between the carboxy group of Boc-amino-alkylene carboxylic acid andthe amine of 2-amino-benzophenone, followed by Boc removal (Figure 1). Coupling wasperformed using phosgene as the coupling reagent. The product was treated with TFA toobtain the BP unit. Purification was performed on silica gel.Fig. 1. Synthesis of BP units.Fig. 2. Structure of SN1 containing photo-affinity label.156
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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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