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Local organizing CommitteeJens BuchardtPaul R. HansenPeter HeegaardPhaedria St. HilaireBirthe KragelundThomas E. NielsenKristian StrømgaardInternational Scientific <strong>com</strong>mitteeFernando AlbericioDavid AndreuAnnette G. Beck-SickingerPaul CordopatisRonald FrankYoshiaki KisoHilkka LankinenTom MuirAnna-Maria PapiniAntonello PessiClaudio TonioloJohn Wadexiii
Page 2 and 3: Peptides 2010Tales of PeptidesProce
Page 4 and 5: Peptides 2010Tales of PeptidesProce
Page 8 and 9: IntroductionWe had the distinct hon
Page 10: Scientific programIn planning the 3
Page 13: 31 st EUROPEAN PEPTIDE SYMPOSIUMSep
Page 20 and 21: European Peptide SymposiaSymposium
Page 22 and 23: The 2010 Leonidas Zervas AwardThe L
Page 24 and 25: Dr. Bert L. Schram Poster Awards:Th
Page 26 and 27: Table of ContentsN-Pi Interactions
Page 28 and 29: Radical Scavenging Activity of Hydr
Page 30 and 31: Computational Study on Helical Stru
Page 32 and 33: Automated Microwave-Assisted Peptid
Page 34 and 35: Peptide Nucleic Acids with Chiral B
Page 36 and 37: Role of Triple Hyp-Pro Substitution
Page 38 and 39: Mechanism in Inhibition of Histone
Page 40 and 41: Lasiocepsin: Novel Antimicrobial Pe
Page 42 and 43: N-Linked Homodimers of the Kinin B1
Page 44 and 45: Synthesis and Biological Evaluation
Page 46 and 47: Molecular Modeling of Single and Mu
Page 49 and 50: Proceedings of the 31 st European P
Page 65 and 66:
Proceedings of the 31 st European P
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Page 69 and 70:
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parallel, we developed the cell-per
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BocHNSEMOBO OONH5bOHNISEMOORink-MBH
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Fig. 3. X-Ray diffraction structure
Page 96 and 97:
Table 1. Molar conversion yields of
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with piperidine were obtained. For
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Fig. 1. Formation of a DKP thioeste
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Fig. 1. CD spectrum of oxytocin (OT
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Table 2. Results of evaluation of r
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NHHNOONHHNO+HOOHRHNONHO N H OOHOHHN
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45401x10 -3 M concentrationStabiliz
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35302520151050-5-10100 200 300 400
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1+H 2O1RHHCOH 1 2HC N C COOHRHCHOHC
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Fig. 1. NA free of metal (left) and
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O+ZHNOONbzOHH +ZHNOOONbzH + OROH R=
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ONH 2CHCNSONHH 2COCH 2COCH 2CH 2NCH
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Fig. 2. α-Tfm-Alanine containing d
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Fig. 3. Synthesis of (S)- and (R)-
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Fig. 3. Preparation of C-terminal C
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aliphatic amines (Figure 1) as deca
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Fig. 2. Synthesized -chloromethyl k
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Table 1. Irradiation times (t irr i
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Table 1. Peptides which were reacte
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Θ / (deg cm 2 dmol -1 )synthesis o
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polymyxin bicyclic peptide analogue
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Lys Phe GlnZ OBzl Z OH H OBu tTBTU/
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Table 1. Synthesis of tetrahydro-β
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Table 1. Synthesis of Fmoc-aza-β 3
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The effect of dimeric analogs on th
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acids were incorporated using the F
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Table 1. Synthetic protocol in Libe
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α,β-unsaturated ketones in protic
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Table 1. Overall yield of N β -Fmo
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concentration (40 mg of the linear
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Fig. 3. Activity of CovX-Bodies in
Page 158 and 159:
obtained in 80% yield (Scheme 2). T
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Fig. 1. (A) Reduced-form amylin(1-1
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Table1. Conformational search with
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conditions and the subsequent coupl
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Table 1. Molecular properties of Zw
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Table 1. Cyclization of linear O-ac
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all the final results of the synthe
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According to HPLC, purity of the cr
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Synthesis of the peptide bond in aq
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tert-butylcarbonylation of the hydr
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AcknowledgmentsThis work was partia
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We next sought practical conditions
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Table 1. Overview of the synthesize
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Fig. 2. Crude synthetic and prepara
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amine of the previous amino acid in
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SHCH 3Ocyclication/pH 7.5OON(AA)nON
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Results and DiscussionLinear cyclov
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Table 1. Fragments obtained from cl
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NMR-analysis allowed full structura
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Table 2. IC50 values for the bindin
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Detection of Fm-Pip (= 301 nm)UV de
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OHONBocO OSH 2 NO 2 SOO Ni ii iiiON
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Coupling between the mono-6-deoxy-
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AB0 50 100 150Fig. 3. Yeast cells w
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Fig. 2. Analytical HPLC of the prod
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The canonic M2e epitope entailed co
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Fig. 2. 1 H- 15 N HSQC spectra of 1
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Fig. 1. Planetary ball-mill for the
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Fig. 2. TAMRA cross-reaction. (A)Fl
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Scheme 1. On-resin peptide cyclizat
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Fig. 2. Analytical RP-HPLC of (A) p
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Table 1. Integration results of RP-
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Table 1. Coupling conditions for th
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Table 1.Cyclization of H-Ala-Ala-Me
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Table 1. Thermodynamic and kinetic
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Table 1. A summary of synthesis yie
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In order to minimize the volume of
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MeOOMeHN8OOOa -fH 2 NH 2 NOHX'NHNHO
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Fig. 1. HPLC of crude [Asn 641Fig.
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Table 1. Room temperature- vs MW-as
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Fig. 2. LC-MS analyses of final pro
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Table 1. Racemization during SPPS o
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Response (RU)201816141210864200 5e-
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Table 1. Sonogashira cross-coupling
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observed for few residues including
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Intens.x108Dppa-Gly-Arg-Thr-Leu (L)
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ones most susceptible for proteolys
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Table 1. Yields of peptide segments
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H 2NSOONHHHNONOONHHHNNOOOONHHHNNOOO
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Table 1. Yields of selected crude p
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peptides (2,7,9) were unable to red
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Table 1. Summary of peptide synthes
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H peptide Aa N1-4aSSDisulfide bridg
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number of conditions were screened
Page 266 and 267:
Scheme 3. Synthesis of thioacid fro
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Fig. 2. Secondary structure of hete
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Fig. 3. Comparison of conventional
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HO 2 CXY6a 3,5-diamino-6b 3-amino-4
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Table 1. Inhibitory activity of the
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significant when it is greater or e
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Table 1. IC 50 in µmol; Cell lines
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Scheme 2.Fig. 3. Three representati
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Coupling was done by the TBTU metho
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present in cell walls of Gramnegati
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Table 1. Inhibition of FP-2 (%) at
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Table 1. Sequences and MIC activity
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Table 1. Diastereoselectivity studi
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Research work on Myelin: In our stu
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Table 1. In vitro antihypertensive
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alkylating agent 4, in the presence
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Table 1. Kinetic parameters of KIII
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andom sampling algorithms. The star
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Binding assays and digestion assays
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Fig. 1. Far UV CD spectra in water
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Fig. 3. RP-HPLC of DualAG, A: 0.1%T
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Interaction between positively char
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Fig. 1. Antitumor activity against
Page 312 and 313:
Biological results:By varying the l
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the scaffold, sequentially modified
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Pictet-Spengler reaction with p-nit
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The cell translocation ability of Q
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We have developed these modules in
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Fig. 3. GC-MS n analysis of culture
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Table 1. The quantity of identified
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protocol previously described [2].
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(pH=6.5) and 1.0 M sodium acetate)
Page 330 and 331:
Replacement of residue Leu68 by hyd
Page 332 and 333:
Human cystatin C as a protein conta
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Cyst-13 complex. Literature data su
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Table 1. Results of extraction/exci
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Table 1. Proteins identified by MAL
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Table 1. Evaluation of the inhibiti
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They were the sequences: RCTGVSVIRR
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Fig. 2. 2D-FL spectra of the fiftee
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antiviral activity against both vir
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Table 1. Cytotoxicity (IC 50 ) a of
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ClClHNO R 1NHR 1 =CH 2Ph, CH(CH 3)
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peptide also undergoes a conformati
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Table 1. Structure and in vitro pro
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Table1. Structures and activities o
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Table 1. Antitumor activity in vivo
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properties and further adaptation f
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Death of animals from acute toxicit
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350ABlood glucose level (mg/dl)3002
Page 366 and 367:
Lys7 by alanine residue did not aff
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Table 1. Pharmacological properties
Page 370 and 371:
Table 1. GI 50 values (in µM) for
Page 372 and 373:
We also developed a very convenient
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The final deprotection of the prote
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Fig. 1. Effect of AA on PTP opening
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Fig. 3. Coupling strategy 2: ring c
Page 380 and 381:
Table 1. Peptide sequences and corr
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R 3H 2 NONHOOHNONH 2R 3 :HNN H N NN
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1 2 3 4 5 6Lanes:1 - negative contr
Page 386 and 387:
In order to prevent racemisation, C
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1350.66271800.5463z=4z=390(A)807060
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The binding of hemopressin at the C
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Scheme 2. Synthetic strategy for th
Page 394 and 395:
Fig. 2. Supposed binding of Val-Pro
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16.1 of DhHP-6 has not daf-16 depen
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Table 1. HDAC inhibitory activity a
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These peptides were engineered succ
Page 402 and 403:
Table 1. Binding affinity to opioid
Page 404 and 405:
Results and DiscussionIn vivo studi
Page 406 and 407:
HOHOROOAcNHCO-L-X-D-Glu-NH 2HOHHOHO
Page 408 and 409:
Fig. 1. Structures of Pro 3 -TL and
Page 410 and 411:
Fig. 2. The level of expression of
Page 412 and 413:
Table 1. Biological assays of the s
Page 414 and 415:
Table 4. Some nonpeptide oxytocin a
Page 416 and 417:
Aggregated peptides per vesicle5002
Page 418 and 419:
Fig. 2. Structures of P5 (left) and
Page 420 and 421:
0.003AL15AL4Absorbance0.0020.001022
Page 422 and 423:
chemically-modified functional Ad h
Page 424 and 425:
Table 1. MIC (µM) and hemolytic ac
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Table 1. MIC (µM) and hemolytic ac
Page 428 and 429:
Table 1. Antibacterial activity (MI
Page 430 and 431:
Fig. 2. Left: CD spectra in methano
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Fig. 2. CD spectra in water of (⋅
Page 434 and 435:
These methods provided the complete
Page 436 and 437:
membrane, all peptides acquired a h
Page 438 and 439:
The conformational preferences of s
Page 440 and 441:
Fig. 2. 3D-Representation of the 54
Page 442 and 443:
Table 1. Chemical characteristics a
Page 444 and 445:
Results and DiscussionSite-directed
Page 446 and 447:
Antibacterial activities. Each isol
Page 448 and 449:
Fig. 2. (A) Integrated heat per inj
Page 450 and 451:
Fig. 2. Effect of L-MCa andD-MCa on
Page 452 and 453:
Fig. 1. Phase contrast images of GU
Page 454 and 455:
Table 1. Antimicrobial and hemolyti
Page 456 and 457:
(Figure 1-B). Both lymphocyte cell
Page 458 and 459:
Fig. 1. GPMVs from RBL-2H3 cells we
Page 460 and 461:
Vv-AMP1Vv-AMP1...vaearRTCESQSHRFKGT
Page 462 and 463:
phosphate buffer (IGP) and was noth
Page 464 and 465:
Table 1. Apoptogenic and translocat
Page 466 and 467:
Fig. 1. The AMPA profile of eosinop
Page 468 and 469:
HNOHOHOHOHNOHOAcNHO OHOOOHNH 2HO HO
Page 470 and 471:
determine if they could retain the
Page 472 and 473:
Fig. 2. Evolutionary diversity of p
Page 474 and 475:
Table 1. GPI and MVD assay of TIPP
Page 476 and 477:
Results and DiscussionThe three-dim
Page 478 and 479:
Fig. 2. Effect of lGnRH-III, and lG
Page 480 and 481:
Page 482 and 483:
2,0x10 -5A0,0B0,0∆A = A L-A R4,0x
Page 484 and 485:
NMeSer 4 and their counterparts. Be
Page 486 and 487:
Page 488 and 489:
chymotrypsinpepsin1. H-Tyr-D-Dap-Ph
Page 490 and 491:
Fig. 1. Average IR and VCD spectra
Page 492 and 493:
Table 1. Physicochemical properties
Page 494 and 495:
Table 1. Physicochemical properties
Page 496 and 497:
Table 1. Biological activities of o
Page 498 and 499:
Fig. 1. The 50 last conformations o
Page 500 and 501:
Results and DiscussionThe M1154 was
Page 502 and 503:
Table 1. Opioid receptor binding af
Page 504 and 505:
Table 1. Identification of neuropep
Page 506 and 507:
[AzaPhe 4 ]GHRP-6 6Fig. 1. Circular
Page 508 and 509:
Table 1. Analytical data and antago
Page 510 and 511:
OD ratio33031530011060105432102/1 4
Page 512 and 513:
Broad NH signals spread within the
Page 514 and 515:
Fig. 3. Inhibition constants of mul
Page 516 and 517:
Fig. 1. Antiproliferative activity
Page 518 and 519:
Table 1. Association equilibrium co
Page 520 and 521:
Table 1. Inhibitory activity of SFT
Page 522 and 523:
Table 1. Antibody recognition of re
Page 524 and 525:
Table 1. Analytical characterizatio
Page 526 and 527:
In case of an oligonucleotide conta
Page 528 and 529:
Table 1. Ac-peptidyl-MCA as substra
Page 530 and 531:
The selected peptides were assayed
Page 532 and 533:
Table 1. The ratio of anti-OVA IgG1
Page 534 and 535:
Paw pressure (g/cm 2 )3503002502001
Page 536 and 537:
Furthermore, expression vectors for
Page 538 and 539:
Table 1. Biological evaluation of n
Page 540 and 541:
Table 1. Overlapping peptides of tT
Page 542 and 543:
Fig. 2. From top to bottom, Compari
Page 544 and 545:
solved using molecular replacement
Page 546 and 547:
Table 1. Sequences and analytical d
Page 548 and 549:
Identity of the protein was checked
Page 550 and 551:
Table 1. In-vitro metabolic stabili
Page 552 and 553:
Table 1. Design of the new glycopep
Page 554 and 555:
Fig. 1. The best ligand pose of YPE
Page 556 and 557:
Table 1. Folding dynamics of Ac-WIT
Page 558 and 559:
100806040200*###Glu - + + + +PGP -
Page 560 and 561:
Fig. 1. Inhibition of ACE by SCR pe
Page 562 and 563:
84 (chronic myeloid leukemia), SKW-
Page 564 and 565:
Table 2. Enzymatic Digestion of GnR
Page 566 and 567:
30 min at pH 7. Radiochemical yield
Page 568 and 569:
FRET-CR9. The efficiency of FRET-CD
Page 570 and 571:
40000350003000025000200001500010000
Page 572 and 573:
B)Glp-His-Trp-Lys(Ac)-His-Asp-Trp-L
Page 574 and 575:
step, benzyl protection has been re
Page 576 and 577:
Fig. 2. Effects of compounds 2 (a-b
Page 578 and 579:
Table 1. Analytical Data for Homobi
Page 580 and 581:
The GnRH-III based bioconjugates wi
Page 582 and 583:
24 hours. The native configuration
Page 584 and 585:
The Boc-Val-Pro-ACV and Boc-Ile-Pro
Page 586 and 587:
Table 1. K D values (expressed in
Page 588 and 589:
We studied molecular-weight distrib
Page 590 and 591:
Fig. 2. Side-chain region of the TO
Page 592 and 593:
Fig. 2. Staining of SHSY-5Y cells i
Page 594 and 595:
Fig. 1. Photoaffinity labeling. Fig
Page 596 and 597:
Solid-phase synthesis on the 2-Cl-T
Page 598 and 599:
Table 1. Stimulation of antibody pr
Page 600 and 601:
Table 1. Inhibitory effect of CARD-
Page 602 and 603:
Sidechain-to-backbone cyclized pept
Page 604 and 605:
Fig. 2. ITC characterization of Rib
Page 606 and 607:
Table 1. Antiviral activity of HpVs
Page 608 and 609:
eceptor antagonists may serve medic
Page 610 and 611:
AcknowledgmentsWe thank Fuji Film R
Page 612 and 613:
Table 1. Values of the partition co
Page 614 and 615:
60fluorescência fluorescence(u.a)4
Page 616 and 617:
Table 1. Differential cell counts i
Page 618 and 619:
Fig. 1. The -sheet stacks 6xAmyl 10
Page 620 and 621:
Lys28 is fluctuating with the -shee
Page 622 and 623:
Fig. 2. Synthesized peptides and (A
Page 624 and 625:
performed at 25 o C with mixing tim
Page 626 and 627:
1 2 3 4OO NHHNOClOOMeOO NHHNOClOOHH
Page 628 and 629:
3 10 -helical structure, that of 2
Page 630 and 631:
abFig. 2. AFM images of Z-Aib 6 -N
Page 632 and 633:
0,440,400,36E 1/ 2(V vs SCE)0,320,2
Page 634 and 635:
Fig. 2. Plots of chemical shifts of
Page 636 and 637:
Counts400003000020000Unlabeledi, i+
Page 638 and 639:
esorption, this effect interferes w
Page 640 and 641:
Table 1. Affinity to μ and δ opio
Page 642 and 643:
Table 1. Proton chemical shifts and
Page 644 and 645:
with Zn 2+ ions. Peptides containin
Page 646 and 647:
Table 1. Root mean square (RMS) dev
Page 648 and 649:
configuration (1’S, 1S, 3R) in th
Page 650 and 651:
Fig. 2. Amide-I region of the 2D IR
Page 652 and 653:
Table 1. Antiviral activity of allo
Page 654 and 655:
Table 1. Characteristics, K i and I
Page 656 and 657:
concentration. We at first checked
Page 658 and 659:
Preliminary time scans allowedto as
Page 660 and 661:
Table 1. Half lives of the tested p
Page 662 and 663:
stabilization are the non-H-bonded
Page 664 and 665:
Table 1. Gold nanoparticles obtaine
Page 666 and 667:
Fig. 2. Schematic representation of
Page 668 and 669:
Fig. 2. FTIR and UV-vis (inset) spe
Page 670 and 671:
OPhPh(E)-chalconeR-{L-Leu-L-Leu-dAA
Page 672 and 673:
Table 1. Sequences and properties o
Page 674 and 675:
The particle size distribution of t
Page 676 and 677:
-fac -fac -mer -mer0.0 kJ/mol 0.0 k
Page 678 and 679:
The fact that 1,4-DHP lipid molecul
Page 680 and 681:
Apo-B 272apoptosis 300, 416apoptoso
Page 682 and 683:
drug delivery 270, 514drug discover
Page 684 and 685:
loop closure 508loop search times 5
Page 686 and 687:
photolysis 82photoreaction 586photo
Page 688 and 689:
tryptophan binding site 22tTG(1-230
Page 690 and 691:
Biernat, Monika 96Bifulco, Maurizio
Page 692 and 693:
Dorosh, Marina Yu. 310Dorpe, Sylvia
Page 694 and 695:
Huggins, Kelly N. L. 22Hull, Willia
Page 696 and 697:
Mammi, Stefano 328, 332, 434, 542Ma
Page 698 and 699:
Pipkorn, Rüdiger 206Pisa, Margheri
Page 700 and 701:
Stoineva, Ivanka B. 346, 536Storozh
Page 702:
655
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