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2,0x10 -5A0,0B0,0∆A = A L-A R4,0x10 -5 0.3-2,0x10 -5-4,0x10 -5-6,0x10 -5-8,0x10 -50.61.07.011.016.021.0350 400 450 500 550Wavelength (nm)∆A = A R - A L-1,0x10 -4-2,0x10 -4-3,0x10 -40,01,03,07,011,021,0200 220 240 260Wavelength (nm)Fig. 2. (A) UV-visible CD spectra of curcumin and (B) far-UV CD spectra of AS, at differentcurcumin/AS molar ratios as indicated inside each figure.Curcumin is not optically active and exhibits induced CD bands at 425 nm (negative) andat 374 nm (positive) upon binding to AS (Figure 2A). The Cotton bands observed in thepresence of AS are of opposite sign to that reported for the curcumin-human albumincomplex [5], suggesting that curcumin adopts an opposite chirality in the complex with AS.The far-UV CD spectra of AS (4.0 µM) at different curcumin-to-protein molar ratiosare characterized by a decrease in the intensity of the negative band at about 198 nm,indicative of a reduction of the random coil conformation (Figure 2B). The absence of anordered CD spectrum suggests that curcumin-induced structural changes are localized insmall portions of AS. The binding constant estimated from the far-UV CD data using anonlinear least-squares computer fit to the equation based on 1:1 binding stoichiometry [6]was 1.0±0.3×10 5 M -1 , in agreement with that determined by fluorescence titration.Chemical shift perturbation mapping was used to identify the curcumin bindinginterface of AS. The experiment consists of a stepwise addition of ligand (56 mM inacetone-d 6 ) to an 15 N-labelled AS sample (0.3 mM), monitoring the chemical shifts of thebackbone amide resonances of the protein. Backbone amide resonances of free AS in 20mM phosphate buffer, pH 6.8, assigned using 2D- 15 N-HSQC-TOCSY, and 2D- 15 N-HSQC-NOESY experiments, were in agreement with those reported in the literature [7]. ControlHSQC experiments were performed to evaluate the effect of acetone on the amideresonances of AS.Residues which directly interact with curcumin are likely to display the biggestchemical shift changes. It is possible that ligand-induced conformational restrictions mayaffect also amide resonances of residues involved in long-range interactions [8]. Residuesinvolved in the interaction with curcumin are G41, K45, V52, A56, I88, A90, A91, T92,G93, V95, L113, M116, M127, Q134, D135 and A140.Our data shows that curcumin binds to the AS monomer in a 1:1 stoichiometry(K d = 10±3 µM) and this interaction prevents curcumin degradation in aqueous solution.This result, in addition to literature data, supports the possible application of curcumin asmodulator of AS aggregation. Further studies will be performed to analyze the capability ofcurcumin to disaggregate AS fibrils.References1. Pandey, N., et al. Acta Neuropathol. 115, 479-489 (2008).2. Leung, M.H.M., Kee, T.W. Langmuir 25, 5773-5777 (2009).3. Min, J., et al. J. Mol. Struct. 692, 71-80 (2004).4. Fan, T.C., et al. J. Biol. Chem. 283, 25468-25474 (2008).5. Pulla Reddy, et al. Lipids 34, 1025-1029 (1999).6. Siligardi, G., et al. J. Biol. Chem. 277, 20151-20159 (2002).7. Bodner, C.R., et al. Biochemistry 49, 862-871 (2010).8. Dedmon, M.M., et al. J. Am. Chem. Soc. 127, 476-477 (2005).435
Proceedings of the 31 st European Peptide SymposiumMichal Lebl, Morten Meldal, Knud J. Jensen, Thomas Hoeg-Jensen (Editors)European Peptide Society, 2010Synthesis, Antiproliferative Activity on Prostate Cancer Cells,Enzymatic Stability and Conformational Studies ofNew GnRH AnaloguesFotini N. Lamari 1 , Eleni V. Pappa 1 , Zinovia Spyranti 1 ,Aikaterini A. Zompra 1 , Zoi Diamantopoulou 2 , Panagiotis Katsoris 2 ,G. Liapakis 3 , Georgios A. Spyroulias 1 , and Paul Cordopatis 11 Department of Pharmacy, University of Patras, Patra, 26504, Greece; 2 Department ofBiology, University of Patras, Patra, 26500, Greece; 3 Department of Medicine,University of Crete, Crete, 71003, GreeceIntroductionGnRH (pGlu 1 -His 2 -Trp 3 -Ser 4 -Tyr 5 -Gly 6 -Leu 7 -Arg 8 -Pro 9 -Gly 10 -NH 2 ) analogues have beenused in oncology to induce reversible chemical castration. In addition to the classichypophysiotropic action of GnRH, it has been shown that many malignant cells, such asprostate cancer cells, secrete GnRH and express the GnRH receptor/s [1-3].Leuprolide ([DLeu 6 , desGly 10 )-GnRH-NHEt]) is a commercially available GnRHagonists but despite its long record of use, issues concerning its conformation have not yetbeen resolved. In order to further study the structure-activity relationships we synthesizedeleven new leuprolide analogues with multiple amino acid changes in positions 4 and 6(Table 1) and studied their effect on prostate cancer cell proliferation (PC3 and LNCaP celllines) [4,5]. To improve enzymatic stability, NMeSer was incorporated in position 4 and therate of hydrolysis by α-chymotrypsin and subtilisin was investigated. DLeu 6 of Leuprolidewas substituted by DLys [alone or modified by conjugation of Gly, Ala, Sar, αMeVal,NMeVal or Gly(tBu)], D-or L-Glu and Ser 4 by NMeSer.Conformational studies of leuprolide and three more analogues (IX, X, XI) have beenperformed in an attempt to elucidate structural changes occurring upon substitution ofnative residues and to study structure-activity relationship for these analogues.Results and DiscussionAfter 72 h treatment the peptides slightly inhibited the proliferation of PC3 and LNCaPcells. Leuprolide and analogues V, VI and X had a comparable effect on PC3 cellproliferation while, there was no significant difference between the effect of analogues withTable 1. New analogues of GnRHPeptideGnRH AnaloguesGnRH pGlu 1 -His 2 -Trp 3 -Ser 4 -Tyr 5 -Gly 6 -Leu 7 -Arg 8 -Pro 9 -Gly 10 -NH 2Leuprolide[DLeu 6 , desGly 10 ]-GnRH-NHEtI[NMeSer 4 ,DLys 6 , desGly 10 ]-GnRH-NHEtII[NMeSer 4 ,DLys 6 (Sar), desGly 10 ]-GnRH-NHEtIII[NMeSer 4 ,DLys 6 (Ala), desGly 10 ]-GnRH-NHEtIV[NMeSer 4 ,DLys 6 (Gly), desGly 10 ]-GnRH-NHEt{DLys 6 [Gly(tBu), desGly 10 ]}-GnRH-NHEtVVIVIIVIIIIXXXI{NMeSer 4 ,DLys 6 [Gly(tBu), desGly 10 ]}-GnRH-NHEt[NMeSer 4 ,DLys 6 (αMeVal), desGly 10 ]-GnRH-NHEt[NMeSer 4 ,DLys 6 (NMeVal), desGly 10 ]-GnRH-NHEt[Glu 6 , desGly 10 ]-GnRH-NHEt[DGlu 6 , desGly 10 ]-GnRH-NHEt[NMeSer 4 ,DGlu 6 , desGly 10 ]-GnRH-NHEt436
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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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