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eceptor antagonists may serve medicinal chemists in novel drug design or be used as drugcandidates themselves [1].Bee, wasp and ant venoms are available in a relatively limited number of species(except for social honeybees). The venom analyses of a few specimens of the solitary beeOsmia rufa by LC-ESI-MS and nanoESI-MS showed more than 50 different compoundswith molecular masses ranging from 400 to 4000 Da [2]. The major component, at 1924.20Da, was revealed after sequencing by de novo MS/MS and Edman degradation to be a17-residue cysteine-free peptide, named osmin. Preliminary assays showed that osmininhibits bacterial and fungal growth at micromolar concentrations and 3D models withalpha-helical structure showed an amphipathic pattern typical of antimicrobial peptides(AMPs) [2].Bradykinin-potentiating peptides (BPPs) are angiotensin-converting enzyme inhibitorsidentified in several species. Originally discovered in the ’60s, they led to the developmentof Captopril, a drug to treat hypertension. The characteristic structural features areinvariable N-terminal pyroglutamate residues and two consecutive C-terminal prolineresidues. The development and validation of original methodology for high throughputdiscovery of BPPs in venoms combined to LC-ESI-MS/MS in precursor ion scan mode, 20BPP-like sequences were discovered in venom of Bothrops moojeni snake [3].Finally, the genome, venom transcriptome and proteome of Conus consors (Figure 2)are currently exhaustively studied. Identification, characterisation and synthesis of novelbioactive compounds are investigated [4]. After high throughput bioactivity screening,selected peptides are further characterised in vivo and their potential as novelbiopharmaceutical drug candidates is evaluated. Additionally, the biodiversity, ecology andmolecular evolution of a wide range of venomous gastropod species are studied.We believe that our unique techniques, combining mass spectrometry to in silico dataand text mining strategies, are a straightforward discovery approach for novel biomoleculesfrom animal venoms and other natural sources.Fig. 2. HPLC UV of milked venom (MV) and dissected venom (DV) of Conus consors conesnail (bottom figure).AcknowledgmentsCONCO, the cone snail genome project for health, is funded by the European Commission:LIFESCIHEALTH-6 Integrated Project LSHB-CT-2007-037592. We are grateful to the governmentsof New Caledonia and French Polynesia.References1. Hayashi, et al. Peptides 25(8), 1243-1251 (2004).2. Stöcklin, et al. Toxicon. 55(1), 20-27 (2010).3. Menin, et al. Toxicon. 51(7), 1288-1302 (2008).4. Biass, et al. J. Proteomics 72(2), 210-218 (2009).561
Proceedings of the 31 st European Peptide SymposiumMichal Lebl, Morten Meldal, Knud J. Jensen, Thomas Hoeg-Jensen (Editors)European Peptide Society, 2010Application of Conjugated Glutamic Acid Peptide (GAP) to aNovel 4-Anilinoquinoline EGFR Inhibitor forTumor-Targeted ImagingChumpol Theeraladanon 1 , Nobukazu Takahashi 1 , Masaaki Shiina 2 ,Keisuke Hamada 2 , Yuuki Takada 1 , Hisashi Endo 3 , Ukihide Tateishi 1 ,Takashi Oka 1 , Kazuhiro Ogata 2 , David J. Yang 4 , and Tomio Inoue 11 Department of Radiology, Graduate School of Medicine, Yokohama City University,Yokohama, 236-0004, Japan; 2 Department of Biochemistry, Graduate School of Medicine,Yokohama City University, Yokohama, 236-0004, Japan; 3 Department of Pharmacy,Yokohama City University Hospital, Yokohama, 236-0004, Japan; 4 Division ofDiagnostic Imaging, The University of Texas M. D. Anderson Cancer Center,Houston, Texas, 77030, U.S.A.IntroductionGlutamic Acid Polypeptide (GAP) is a targeted drug delivery peptide. It would be suitableto conjugate anti-cancer as well as chelate to radiometal with its acid residues for imagingor radiotherapeutic application. Despite the fact that GAP is commercially available,various ranges of peptide chain (MW 750-50,000) leads to occasionally difficultexplanation of experiment results when it exerts action though glutamate receptors. Herein,we designed the decapeptide GAP (MW 1309.16) as an optimized homing agent to carry anovel 4-anilinoquinoline epidermal growth factor receptor (EGFR) inhibitor aiming todevelop 68 Ga-GAP-YCU07 to image functional ER(+) diseases such as breast cancer.Results and DiscussionDecapeptide GAP was synthesized by peptide synthesizer. This well characterized GAP isa potential decapeptide targeted carrier and chelator, which conjugates rationally designednovel 4-anilinoquinoline EGFR Tyrosine Kinase Inhibitor, [6,7-dimethoxyethoxy]-quinolin-4-yl]-(3-ethynylphenyl)-amine (YCU07) via peptide linkage (Figure 1).OH 2 NOOHNHOHNOn = 10OOHFig. 1. GAP-YCU07.OOOOONHNNAccording to the pharmacophore model for inhibitor competing at EGFR binding site, thequinoline nucleus of YCU07 was successfully synthesized employing Ring-ClosingMetathesis (RCM) methodology. Facile radiolabeling with GAP technology provided 68 Ga-GAP-YCU07 which one molecule of GAP-YCU07 possibly chelated a maximum of three68 Ga ions. Injection of 68 Ga labeled conjugated GAP-YCU07 to nude mice implanted withA431 evaluated the biodistribution and was imaged by using animal PET camera and CTresulting in accumulation of 68 Ga-GAP-YCU07 in the receptor positive tumor with uptakevalues of 1.50±0.09, 2.36±0.36 %ID/g at 30 and 90 min, respectively.562
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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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Proceedings of the 31 st European P
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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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