Proceedings book download - 5Z.com

More documents

Recommendations

Info

Scientific programIn planning the 31st EPS, the organizers aimed at creating the strongest possiblescientific program broadly within peptide science. There was more emphasis on new,enabling developments in peptide chemistry than in some previous peptide symposia.in addition the organizers wanted to highlight peptides as drugs and had a dedicatedsession towards this topic, chaired by Thomas Hoeg-Jensen and Waleed Danho.The plenary and invited speakers were Herbert Waldmann, Tom W. Muir, ErnestGiralt, William F. DeGrado, Ivan Huc , Fernando Albericio, Horst Kessler, PaulAlewood, Annette Beck-Sickinger, William Lubell, Ronald Raines, and RichardDiMarchi, who were invited to present the latest developments in peptide science fromaround the world. in addition the two awardees, Helma Wennemers and Stephen B. H.Kent contributed to the strong program. The speakers were invited to present newdevelopments in peptide synthesis, both in SPPS and in ligation methods, peptidechemical biology including the role of farnesylation and palmitoylation, peptidemedicinal chemistry, foldamers related to peptides, structural aspects of peptides andproteins and more.The scientific <strong>com</strong>mittee ranked all abstracts. Based on their ranking, thespeakers for the oral and young investigator presentations were selected.The young investigator sessions as well as the Zervas and Rudinger awardsessions were all integrated into the main program to encourage attendance. Thesessions covered were: Peptide biochemistry and biology; synthetic chemistry ofamino acids and peptides; young investigator session; general peptide science; ligation;peptides as drugs; peptidomimetics; protein design and protein modification; peptidematerials and peptide properties; antibacterial and cell penetrating peptides;lipopeptides; signaling, hormones and neuro-peptides; peptide biology; chemicalbiology and proteomics. Needless to say, the actual lecture topics covered a widerrange than this. The parallel sessions Monday and Wednesday were a success, in spiteof some initial technical problems on Monday afternoon.In summary, there were 5 plenary lectures, 7 invited lectures, 2 award lectures,12 young investigator lectures and 52 oral presentations. Finally, as mentioned abovethere were close to 600 poster presentations, and two afternoons in the program werededicated to poster sessions. There were generally lively discussions after lectures,which contributed to a scientifically very strong program.ix
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 12 and 13: Message from the Chairman of the Eu
Page 14: Local organizing CommitteeJens Buch
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 61 and 62:
Proceedings of the 31 st European P
Page 63 and 64:
Page 65 and 66:
Page 67 and 68:
Page 69 and 70:
Page 71 and 72:
Page 73 and 74:
Page 75 and 76:
Page 77 and 78:
Page 79 and 80:
Page 81 and 82:
Page 83 and 84:
Page 85 and 86:
Page 87:
Page 90 and 91:
parallel, we developed the cell-per
Page 92 and 93:
BocHNSEMOBO OONH5bOHNISEMOORink-MBH
Page 94 and 95:
Fig. 3. X-Ray diffraction structure
Page 96 and 97:
Table 1. Molar conversion yields of
Page 98 and 99:
with piperidine were obtained. For
Page 100 and 101:
Fig. 1. Formation of a DKP thioeste
Page 102 and 103:
Fig. 1. CD spectrum of oxytocin (OT
Page 104 and 105:
Table 2. Results of evaluation of r
Page 106 and 107:
NHHNOONHHNO+HOOHRHNONHO N H OOHOHHN
Page 108 and 109:
45401x10 -3 M concentrationStabiliz
Page 110 and 111:
35302520151050-5-10100 200 300 400
Page 112 and 113:
1+H 2O1RHHCOH 1 2HC N C COOHRHCHOHC
Page 114 and 115:
Fig. 1. NA free of metal (left) and
Page 116 and 117:
O+ZHNOONbzOHH +ZHNOOONbzH + OROH R=
Page 118 and 119:
ONH 2CHCNSONHH 2COCH 2COCH 2CH 2NCH
Page 120 and 121:
Fig. 2. α-Tfm-Alanine containing d
Page 122 and 123:
Fig. 3. Synthesis of (S)- and (R)-
Page 124 and 125:
Fig. 3. Preparation of C-terminal C
Page 126 and 127:
aliphatic amines (Figure 1) as deca
Page 128 and 129:
Fig. 2. Synthesized -chloromethyl k
Page 130 and 131:
Table 1. Irradiation times (t irr i
Page 132 and 133:
Table 1. Peptides which were reacte
Page 134 and 135:
Θ / (deg cm 2 dmol -1 )synthesis o
Page 136 and 137:
polymyxin bicyclic peptide analogue
Page 138 and 139:
Lys Phe GlnZ OBzl Z OH H OBu tTBTU/
Page 140 and 141:
Table 1. Synthesis of tetrahydro-β
Page 142 and 143:
Table 1. Synthesis of Fmoc-aza-β 3
Page 144 and 145:
The effect of dimeric analogs on th
Page 146 and 147:
acids were incorporated using the F
Page 148 and 149:
Table 1. Synthetic protocol in Libe
Page 150 and 151:
α,β-unsaturated ketones in protic
Page 152 and 153:
Table 1. Overall yield of N β -Fmo
Page 154 and 155:
concentration (40 mg of the linear
Page 156 and 157:
Fig. 3. Activity of CovX-Bodies in
Page 158 and 159:
obtained in 80% yield (Scheme 2). T
Page 160 and 161:
Fig. 1. (A) Reduced-form amylin(1-1
Page 162 and 163:
Table1. Conformational search with
Page 164 and 165:
conditions and the subsequent coupl
Page 166 and 167:
Table 1. Molecular properties of Zw
Page 168 and 169:
Table 1. Cyclization of linear O-ac
Page 170 and 171:
all the final results of the synthe
Page 172 and 173:
According to HPLC, purity of the cr
Page 174 and 175:
Synthesis of the peptide bond in aq
Page 176 and 177:
tert-butylcarbonylation of the hydr
Page 178 and 179:
AcknowledgmentsThis work was partia
Page 180 and 181:
We next sought practical conditions
Page 182 and 183:
Table 1. Overview of the synthesize
Page 184 and 185:
Fig. 2. Crude synthetic and prepara
Page 186 and 187:
amine of the previous amino acid in
Page 188 and 189:
SHCH 3Ocyclication/pH 7.5OON(AA)nON
Page 190 and 191:
Results and DiscussionLinear cyclov
Page 192 and 193:
Table 1. Fragments obtained from cl
Page 194 and 195:
NMR-analysis allowed full structura
Page 196 and 197:
Table 2. IC50 values for the bindin
Page 198 and 199:
Detection of Fm-Pip (= 301 nm)UV de
Page 200 and 201:
OHONBocO OSH 2 NO 2 SOO Ni ii iiiON
Page 202 and 203:
Coupling between the mono-6-deoxy-
Page 204 and 205:
AB0 50 100 150Fig. 3. Yeast cells w
Page 206 and 207:
Fig. 2. Analytical HPLC of the prod
Page 208 and 209:
The canonic M2e epitope entailed co
Page 210 and 211:
Fig. 2. 1 H- 15 N HSQC spectra of 1
Page 212 and 213:
Fig. 1. Planetary ball-mill for the
Page 214 and 215:
Fig. 2. TAMRA cross-reaction. (A)Fl
Page 216 and 217:
Scheme 1. On-resin peptide cyclizat
Page 218 and 219:
Fig. 2. Analytical RP-HPLC of (A) p
Page 220 and 221:
Table 1. Integration results of RP-
Page 222 and 223:
Table 1. Coupling conditions for th
Page 224 and 225:
Table 1.Cyclization of H-Ala-Ala-Me
Page 226 and 227:
Table 1. Thermodynamic and kinetic
Page 228 and 229:
Table 1. A summary of synthesis yie
Page 230 and 231:
In order to minimize the volume of
Page 232 and 233:
MeOOMeHN8OOOa -fH 2 NH 2 NOHX'NHNHO
Page 234 and 235:
Fig. 1. HPLC of crude [Asn 641Fig.
Page 236 and 237:
Table 1. Room temperature- vs MW-as
Page 238 and 239:
Fig. 2. LC-MS analyses of final pro
Page 240 and 241:
Table 1. Racemization during SPPS o
Page 242 and 243:
Response (RU)201816141210864200 5e-
Page 244 and 245:
Table 1. Sonogashira cross-coupling
Page 246 and 247:
observed for few residues including
Page 248 and 249:
Intens.x108Dppa-Gly-Arg-Thr-Leu (L)
Page 250 and 251:
ones most susceptible for proteolys
Page 252 and 253:
Table 1. Yields of peptide segments
Page 254 and 255:
H 2NSOONHHHNONOONHHHNNOOOONHHHNNOOO
Page 256 and 257:
Table 1. Yields of selected crude p
Page 258 and 259:
peptides (2,7,9) were unable to red
Page 260 and 261:
Table 1. Summary of peptide synthes
Page 262 and 263:
H peptide Aa N1-4aSSDisulfide bridg
Page 264 and 265:
number of conditions were screened
Page 266 and 267:
Scheme 3. Synthesis of thioacid fro
Page 268 and 269:
Fig. 2. Secondary structure of hete
Page 270 and 271:
Fig. 3. Comparison of conventional
Page 272 and 273:
HO 2 CXY6a 3,5-diamino-6b 3-amino-4
Page 274 and 275:
Table 1. Inhibitory activity of the
Page 276 and 277:
significant when it is greater or e
Page 278 and 279:
Table 1. IC 50 in µmol; Cell lines
Page 280 and 281:
Scheme 2.Fig. 3. Three representati
Page 282 and 283:
Coupling was done by the TBTU metho
Page 284 and 285:
present in cell walls of Gramnegati
Page 286 and 287:
Table 1. Inhibition of FP-2 (%) at
Page 288 and 289:
Table 1. Sequences and MIC activity
Page 290 and 291:
Table 1. Diastereoselectivity studi
Page 292 and 293:
Research work on Myelin: In our stu
Page 294 and 295:
Table 1. In vitro antihypertensive
Page 296 and 297:
alkylating agent 4, in the presence
Page 298 and 299:
Table 1. Kinetic parameters of KIII
Page 300 and 301:
andom sampling algorithms. The star
Page 302 and 303:
Binding assays and digestion assays
Page 304 and 305:
Fig. 1. Far UV CD spectra in water
Page 306 and 307:
Fig. 3. RP-HPLC of DualAG, A: 0.1%T
Page 308 and 309:
Interaction between positively char
Page 310 and 311:
Fig. 1. Antitumor activity against
Page 312 and 313:
Biological results:By varying the l
Page 314 and 315:
the scaffold, sequentially modified
Page 316 and 317:
Pictet-Spengler reaction with p-nit
Page 318 and 319:
The cell translocation ability of Q
Page 320 and 321:
We have developed these modules in
Page 322 and 323:
Fig. 3. GC-MS n analysis of culture
Page 324 and 325:
Table 1. The quantity of identified
Page 326 and 327:
protocol previously described [2].
Page 328 and 329:
(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
Page 334 and 335:
Cyst-13 complex. Literature data su
Page 336 and 337:
Table 1. Results of extraction/exci
Page 338 and 339:
Table 1. Proteins identified by MAL
Page 340 and 341:
Table 1. Evaluation of the inhibiti
Page 342 and 343:
They were the sequences: RCTGVSVIRR
Page 344 and 345:
Fig. 2. 2D-FL spectra of the fiftee
Page 346 and 347:
antiviral activity against both vir
Page 348 and 349:
Table 1. Cytotoxicity (IC 50 ) a of
Page 350 and 351:
ClClHNO R 1NHR 1 =CH 2Ph, CH(CH 3)
Page 352 and 353:
peptide also undergoes a conformati
Page 354 and 355:
Table 1. Structure and in vitro pro
Page 356 and 357:
Table1. Structures and activities o
Page 358 and 359:
Table 1. Antitumor activity in vivo
Page 360 and 361:
properties and further adaptation f
Page 362 and 363:
Death of animals from acute toxicit
Page 364 and 365:
350ABlood glucose level (mg/dl)3002
Page 366 and 367:
Lys7 by alanine residue did not aff
Page 368 and 369:
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
Page 374 and 375:
The final deprotection of the prote
Page 376 and 377:
Fig. 1. Effect of AA on PTP opening
Page 378 and 379:
Fig. 3. Coupling strategy 2: ring c
Page 380 and 381:
Table 1. Peptide sequences and corr
Page 382 and 383:
R 3H 2 NONHOOHNONH 2R 3 :HNN H N NN
Page 384 and 385:
1 2 3 4 5 6Lanes:1 - negative contr
Page 386 and 387:
In order to prevent racemisation, C
Page 388 and 389:
1350.66271800.5463z=4z=390(A)807060
Page 390 and 391:
The binding of hemopressin at the C
Page 392 and 393:
Scheme 2. Synthetic strategy for th
Page 394 and 395:
Fig. 2. Supposed binding of Val-Pro
Page 396 and 397:
16.1 of DhHP-6 has not daf-16 depen
Page 398 and 399:
Table 1. HDAC inhibitory activity a
Page 400 and 401:
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
Page 426 and 427:
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
Page 432 and 433:
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
show all

Proceedings book download - 5Z.com

Create successful ePaper yourself

Delete template?

Save as template?