Peptides for the New Millennium: Proceedings of the 16th American Peptide Symposium June 26–July 1, 1999, Minneapolis, Minnesota, U.S.A.

Front Matter....Pages 1-2
Mimetic peptides, demanding enzymes and drug discovery....Pages 3-16
Front Matter....Pages 17-18
Bruce W. Erickson: In memoriam....Pages 19-19
Engineering of a cysteine-containing variant of quadrin, a protein containing the oligomerization site of the hepatitis delta antigen....Pages 20-21
Characterization of betabellins 15D and 16D, designed beta-sandwich proteins that have amyloidogenic properties....Pages 22-23
Design and synthesis of inhibitors of botulinum neurotoxin A and B metalloproteases....Pages 24-25
Dimerization inhibitors of HIV-1 protease: Effective inhibition requires the cross-linking of non-identical peptides....Pages 26-27
Backbone cyclic proteinomimetics derived from the arginine-rich domain of HIV-1 Tat and Rev proteins: One sequence, two conformations, two biological functions....Pages 28-29
Synthesis of several O -glycopeptide analogs of enkephalin....Pages 30-31
Investigating the role of turns in the folding of a predominantly β-sheet protein....Pages 32-33
Receptor-bound conformations of integrin α IIb β 3 antagonists by 15 N-edited NMR spectroscopy....Pages 34-35
Design, synthesis, and characterization of two core modules of bovine pancreatic trypsin inhibitor....Pages 36-37
The fine tuning of high affinity and selective non-peptide agonists of the δ-opioid receptor via solution and solid-phase....Pages 38-39
Cyclic dodecapeptides (LLLD) 3 form ion channels in lipid bilayers....Pages 40-41
Synthesis and evaluation of potential affinity labels for opioid receptors....Pages 42-43
Front Matter....Pages 45-45
Polyethyleneglycol-based chains of precise length for chemobodies....Pages 47-49
 N α -2-(4-Nitrophenylsulfonyl)ethoxycarbonyl (Nsc) as an amino-protecting group and its application for peptide synthesis....Pages 50-52
Nsc- and Fmoc-amino acids for automated solid-phase peptide synthesis: Comparative study of the stability in various conditions....Pages 53-54
 In situ generation of Fmoc amino acid chlorides for extremely difficult couplings to sterically hindered secondary amines in solid-phase peptide synthesis....Pages 55-57
Evaluation of ivDde as a quasi-orthogonal protecting group for Fmoc solid-phase peptide synthesis....Pages 58-59
 N in -4-Nitrobenzenesulfonyl (Nbs): A new protecting group for the indole moiety of tryptophan....Pages 60-61
Front Matter....Pages 45-45
Practical asymmetric synthesis of β-substituted glutamic acids....Pages 62-63
Formation of substituted aromatic rings in amino acid systems via ruthenium activated S N Ar reactions....Pages 64-65
 O -Acetyl-L-homoserine: A versatile synthon for the synthesis of L-homoserine peptides and 3-amino-2-pyrrolidinones....Pages 66-67
Asymmetric synthesis of free unusual β aminoacid esters via Yb(OTf) 3 -caalyzed C-C bond formation and simultaneous deprotection/purification....Pages 68-70
High yield synthesis of heterocyclic β-substituted alanine derivatives....Pages 70-71
Synthesis of (2 S ,4 R )-4-aminoethyl-L-Pro and (2S,4R)-4 -carboxymethyl-L-Pro from (2 S ,4 R )- N α -Boc-4-hydroxy-L-Pro methyl ester....Pages 72-73
A highly effective method for synthesis of N ω -substituted arginines....Pages 74-75
Diffusion phenomena and reactivity using polymer supports: A principal investigation....Pages 76-78
Solid-phase peptide synthesis in the N → C direction....Pages 78-79
Diisopropylethylamine salts for protected amino acids: Direct synthesis of peptides on solid-phase....Pages 80-81
Synthesis of phosphorylated CRE BP1(19-106) amide using a phosphopeptide thioester prepared directly by an Fmoc solid-phase method....Pages 82-83
Preparation of phosphohistidyl peptides via oxidative coupling of H -phosphonates....Pages 84-85
Preparation and incorporation into small peptides and combinatorial libraries of phosphohistidine analogs for study of prokaryotic two-component signal transduction systems....Pages 86-88
Synthesis of phosphonamides and thiophosphonamides by a one-pot activation-coupling-oxidation protocol....Pages 89-90
Synthesis of phosphonopeptide and thiophosphonopeptide analogs as inhibitors of carboxypeptidase A....Pages 91-93
Application of solid-phase Ellman’s reagent for preparation of disulfide-paired isomers of α-conotoxin SI....Pages 94-95
Alternative solid-phase reagents for formation of intramolecular sulfur-sulfur bridges in peptides under mild conditions....Pages 96-97
An evaluation of a novel safety catch linker for development of cyclic peptide libraries....Pages 98-99
Solid-phase synthesis of peptide aldehydes by a Backbone Amide Linker (BAL) strategy....Pages 100-101
Backbone Amide Linker (BAL) methodology to accommodate C -terminal hindered, unreactive, and/or sensitive modifications....Pages 102-103
Front Matter....Pages 45-45
A new tartaric acid-based linker for the synthesis of C -terminal peptide α-oxo-aldehydes....Pages 104-106
A new approach to the guanidinylation of peptides and peptidomimetics including aminoglycosides and related drugs....Pages 107-108
Photoaffinity-labeled probes for the study of isoprenoid recognition sites....Pages 109-110
Orthogonal methods for the synthesis of multiply labeled peptide probes and substrates....Pages 111-112
Strategies for the synthesis of labeled peptides....Pages 113-114
Orthogonal segment ligation....Pages 115-117
Use of orthogonal ligation methods for the synthesis of a hetero peptide dendrimer....Pages 118-119
Minimization of side reactions during removal of the formyl protecting group from the ε-amino group of lysine....Pages 120-121
Mechanistic studies of an unusual amide bond scission....Pages 122-123
Novel methods of making (amidated) peptides: Rapid gram quantities as intein fusions and ton quantities from fusion proteins in the milk of transgenic animals....Pages 124-125
Process research toward scale-up and industrial preparation of RPR 109891 (Klerval ™ )....Pages 126-128
Synthesis of cyclic hexapeptide core of antifungal drug candidates....Pages 129-130
Large scale synthesis of a 27-mer: Identification, characterization and suppression of a diastereomer contaminant....Pages 131-132
The chemical synthesis of agouti-related protein form C....Pages 133-135
Chemical synthesis and characterization of the hypothalamic form of CART: CART(69–116), a new anorectic neuropeptide....Pages 136-137
Application of hydrated salt as a source of essential water for enzymatic peptide synthesis in organic media....Pages 138-139
Enzymatic synthesis of N -protected amino acid-steroid derivatives in organic solvent....Pages 140-141
Peptide amidase-catalyzed C -terminal peptide amidation in a mixture of organic solvents....Pages 142-143
Extending the utility of subtilisin-catalyzed peptide synthesis in organic solvents....Pages 144-145
Backbone amide protection in solid-phase synthesis of peptide isosters derived from N -terminal γ-aldehydes....Pages 146-147
Front Matter....Pages 45-45
An efficient preparation of O -succinimidyl carbamate derivatives from N -protected β-amino acids: Application to the synthesis of urea containing pseudopeptides and oligoureas....Pages 148-149
Mimicry of peptide backbone and side-chain functions: Syntheses of 5- and 7-hydroxymethyl indolizidinone amino acids and indolizidinone amino dicarboxylate, constrained Ser-Pro and Glu-Pro surrogates....Pages 150-152
A flexible regioselective method for bicyclization of peptides....Pages 153-154
Stereoselective synthesis of dipeptidomimetics using chiral allylic aziridines....Pages 155-156
Partially-modified retro-inverso βturn tetrapeptidomimetic....Pages 157-158
Front Matter....Pages 159-159
Targeted libraries....Pages 161-163
New technique for high-throughput synthesis of peptides, peptidomimetics and nonpeptide small organic molecule arrays....Pages 164-166
Identification of miniproteins using cellulose-bound duotope scans....Pages 167-169
Combinatorial peptide synthesis, NMR-aided screening and testing of low molecular weight RNA-ligands....Pages 170-171
Synthetic peptide analogs compared with phage display....Pages 172-173
Rapid parallel synthesis of 584 betides, peptides composed largely of beta-amino acids with side-chains not found in natural peptides....Pages 174-175
SPOCC resins: Polar and chemically inert resins for organic synthesis and library enzyme assays....Pages 176-178
Preparation and applications of a thioacetal handle for solid-phase synthesis....Pages 179-180
“Traceless” solid-phase synthesis of benzimidazole libraries....Pages 181-182
Synthesis of small cyclic peptides: An auxiliary approach to address the “difficult cyclization” problem....Pages 183-185
On-resin cyclization of the cyclic depsipeptide callipeltin B....Pages 186-188
Combinatorial chemistry: Solid-phase synthesis of heterocyclic compounds from C α -functionalized amino acids....Pages 189-190
Highly efficient and versatile construction of secondary structure peptide mimetic libraries: Application to biology and drug development....Pages 191-193
The usage of a β-sheet template with diversity points to generate libraries using the Irori method....Pages 194-195
Solid-phase syntheses of libraries derived from 2-amino-4-carboxy-thiophenol moiety....Pages 196-197
Front Matter....Pages 159-159
Solid-phase synthesis of thiol and thioether functions containing peptides and complex organic molecules....Pages 198-199
Front Matter....Pages 201-201
Implant and transdermal innovations for peptide and protein delivery....Pages 203-205
Loligomers: Multi-tasking intracellular peptide shuttles....Pages 206-208
Utilization of cell-adhesion peptides to improve drug delivery....Pages 209-211
Peptide shuttles for cytoplasmic delivery and nuclear targeting of chemotherapeutic agents....Pages 212-213
Delivering peptides and peptidomimetics across membrane barriers: A prodrug approach....Pages 214-216
Control of apoptosis by using small molecule regulators of Bcl-2 family proteins....Pages 217-218
Bradykinin antagonists: Anti-cancer drugs for the new millennium?....Pages 219-221
Development of the first CGRP-antagonist with nanomolar affinity....Pages 222-223
DP IV-inhibitors: Potential antidiabetic drugs....Pages 224-226
Synthesis and pharmacological activity of a new antagonist of the OP4 receptor....Pages 227-228
Opioid dipeptide derivatives with a mixed μ antagonist/δ antagonist, partial μ agonist/δ antagonist or μ agonist/partial δ agonist profile....Pages 229-270
Constrainedδ opioid peptides: Analogs of DPDPE and deltorphin I containing trimethylphenylalanine instead of phenylalanine....Pages 231-232
Inhibition of α4γ1 integrin receptor interactions by bicyclic β-turn mimetics....Pages 233-234
Recent progress in the field of α v -integrin antagonists....Pages 235-237
Cytotoxic derivatives of luteinizing hormone-releasing hormone (LHRH): Synthesis and evaluation....Pages 238-239
From peptide to non-peptide: The design of LHRH antagonist mimetics....Pages 240-242
Identification of melanocortin-1 receptor selective small molecule agonists....Pages 243-244
Identification and exploitation of structural foci that influence conformational mobility in somatostatin agonists and antagonists....Pages 245-247
Phenyl piperidine-based orally active peptidomimetic agonists for somatostatin receptor subtype-2....Pages 248-249
Front Matter....Pages 201-201
The design and synthesis of non-peptide somatostatin receptor agonists....Pages 250-252
The discovery of orally-active pseudopeptide antagonists of the atrial natriuretic peptide clearance receptor....Pages 253-255
Identification of new blockers of HIV-1 infectivity from synthetic combinatorial libraries....Pages 256-257
Synthetic peptide-based reagents for blocking the entry and inactivation of HIV....Pages 258-259
Synthesis of model systems of the complement inhibitors, complestatin and chloropeptin....Pages 260-261
An intracellular approach for generating stable synthetic peptides and its potential applications....Pages 262-263
Front Matter....Pages 265-265
Talking about TOAC: A novel electron spin resonance probe of peptide conformation....Pages 267-269
Peptide folding induced by C α -methylated, chiral α-acids with a long aliphatic side chain....Pages 270-271
Constrained amino acid analogs in de novo peptide design....Pages 272-274
Peptide folding as a result of the incorporation of large-ring, cycloaliphatic C α,α -disubstituted glycines....Pages 275-276
Importance of secondary structure specificity determinants in protein folding and stability....Pages 277-279
A calorimetric study of the helix-coil transition using a side-chain bridged peptide that folds and unfolds cooperatively....Pages 280-282
 1 H-NMR structure of a 14-residue peptide incorporating a rigid, helix-stabilizing, (i, i+7)-side-chain bridge....Pages 283-284
The design of heterodimeric coiled-coil domains for diagnostic display systems....Pages 285-286
Structural investigations of designed glycosylated helix-loop-helix polypeptide motifs....Pages 287-288
Effect of D-amino acid substitutions on amphipathic α-helical structure....Pages 289-290
Metal induced assembly and folding of a triple stranded α-helical peptide....Pages 291-292
Design of small symmetrical four-helix bundle proteins....Pages 293-294
Cavitand templated de novo four-helix bundles....Pages 295-296
Expanding the repertoire of helical bundles: Stabilization of five+ helical bundles....Pages 297-299
Front Matter....Pages 265-265
Induction of α-helical protein-like molecular architecture by mono- and dialkyl hydrocarbon chains....Pages 300-301
The peptide 3 10 -helix: Historical background and recent structural studies and applications....Pages 302-304
The effects of stereochemistry and sequence on 5- t -butylproline type VI β-turn mimics....Pages 305-306
Torsion angle based design of a βI turn adopting dipeptide (Ac-Aib-AzGly-NH 2 )....Pages 307-308
Conformational analysis of azaproline and other turn inducers....Pages 309-310
Strain-free disulfide bridge and stabilization of β-ribbon structures in short peptides....Pages 311-312
Roles of proline residues in the structure and folding of a β-clam protein....Pages 313-315
Self-assembly of synthetic peptides: Formation of amphipathic surfaces and head-to-tail self-assembly....Pages 316-317
Rotamer number revealed as another parameter to gauge the quality of packing in folded proteins....Pages 318-319
The side-chain classification of loops from high resolution protein crystal structures....Pages 320-321
Dynamics and stability of partially folded and unfolded BPTI analogs....Pages 322-324
Conformational studies with optical spectroscopy of peptides taken from hairpin sequences in the human chorionic gonadotropin β-subunit....Pages 325-326
The mechanism of the propeptide-mediated folding of guanylyl cyclase activating peptides....Pages 327-329
The a-factor lipopeptide pheromone of Saccharomyces cerevisiae : Synthesis, bioactivity, and biophysical analyses of position 4, 5 analogs....Pages 330-331
Structural implications of a novel peptide dimerizer sequence when anchored to terminal ends of different peptide motifs....Pages 332-333
Hydrogen-bonded self-assembled peptide nanotubes from cystine-based macrocycles containing bisurea or hydrocarbon segments....Pages 334-336
Front Matter....Pages 337-337
Heterotrimeric collagen peptides as substrates of metalloproteinases....Pages 339-341
Selective hydrolysis of triple-helical peptides by matrix metalloproteinases....Pages 342-343
The stereoelectronic basis of collagen stability....Pages 344-346
Contribution of mainchain-mainchain hydrogen bonds to the conformational stability of triple-helical collagen....Pages 347-348
Front Matter....Pages 337-337
Density measurements and differential scanning calorimetry of collagen model peptides....Pages 349-351
Design, synthesis and conformations of novel triple-helical collagen mimetic structures....Pages 352-354
Effect of fluoro-substituted proline residues on the conformational stability of triple-helical collagen mimics....Pages 355-356
Modulating the conformational stability of triple-helical collagen by chemical modification....Pages 357-358
The assembly and analysis of collagen mimetics on a tris(2-aminoethyl) amine template....Pages 359-360
Creating functional collagen peptide architectures on solid surfaces....Pages 361-364
Front Matter....Pages 365-365
δ-Regions in proteins: Helices mispredicted as transmembrane segments by the threshold hydrophobicity requirement....Pages 367-369
Dimerization of transmembrane helices studied using de novo designed hydrophobic peptides....Pages 370-371
Transmembrane helix-helix recognition modeled by disulfide trapping in organic-aqueous solutions....Pages 372-373
Determination of the relative positions between TMH V and VI of the μ opioid receptor using site-directed mutagenesis....Pages 374-375
Biophysical studies on a transmembrane peptide of the Saccharomyces cerevisiae α-factor receptor....Pages 376-378
Helix-helix interactions between transmembrane α-helices 3 and 4 within the cystic fibrosis transmembrane conductance regulator protein....Pages 379-380
Chemical approach for evaluating role of the cysteine residues in pentameric phospholamban structure: Effect on sarcoplasmic reticulum Ca 2+ -ATPase....Pages 381-382
Synthesis and biophysical characterization of highly hydrophobic transmembrane peptides....Pages 383-384
Conformational studies of a detergent-bound transmembrane segment of the rat bradykinin receptor....Pages 385-386
Gramicidin A: Structure and dynamic properties....Pages 387-389
Front Matter....Pages 391-391
The proteome: Analysis and utility....Pages 393-395
NMR analysis tools for the peptide sciences....Pages 396-398
Studying structures attached to solid supports by high resolution magic angle spinning NMR (HR MAS NMR)....Pages 399-401
Determination of specific peptide-micelle interactions using NMR spectroscopy....Pages 402-403
Front Matter....Pages 391-391
Protein dynamics by hydrogen/deuterium exchange coupled to mass spectrometry: Purine nucleoside phosphorylase....Pages 404-406
Fragmentation and sequencing of cyclic peptides by MALDI-PSD mass spectrometry....Pages 407-408
LC/MS reversed-phase columns with excellent polypeptide resolution in low concentrations of TFA and acetic acid....Pages 409-410
Application of single bead FTIR in the optimization of solid-phase combinatorial and parallel syntheses....Pages 411-413
Analysis of local conformation within helical peptides via isotopeedited vibrational spectroscopy....Pages 414-416
Front Matter....Pages 417-417
The role of zymogenicity in caspase activation: How to trigger programmed cell death....Pages 419-421
Papain has a tolerance for D-stereochemistry at P 1 like caspases....Pages 422-423
Positive and negative selectivity in protease evolution: Investigation of the specificities of plasmin, t-PA, u-PA, and PSA using substrate phage display....Pages 424-426
Crystal structures of novel insect serine protease inhibitors complexed to bovine α-chymotrypsin....Pages 427-428
Inhibitors of the bradykinin-degrading enzyme, aminopeptidase P....Pages 429-430
Design and synthesis of AHHpA isosteres for the potential inhibition of methionine aminopeptidase-1....Pages 431-432
A first subnanomolar and in vivo active inhibitor of aminopeptidase A (EC 3.4.11.7)....Pages 433-434
A novel stable inhibitor of endopeptidases EC 3.4.24.15 and 3.4.24.16 potentiates bradykinin induced hypotension....Pages 435-437
Structural requirements for collagenolytic activity of matrix metalloproteinase 1 (MMP-1)....Pages 438-440
The synthesis of matrix metalloprotease inhibitor libraries using a hybrid mix/split parallel approach....Pages 441-442
Combinatorial library of phosphinic peptides for discovery of MMP inhibitors on solid-phase....Pages 443-444
Selectivity in inhibition of proteolytic enzymes from Plasmodium falciparum ....Pages 445-447
Proteolytic splicing of Hb α-chain peptides with internal deletions....Pages 448-449
 In vivo detection of tumor associated protease activity using long circulating fluorescent labeled peptide substrates....Pages 450-452
Novel inhibitors of the osteoclast specific cysteine protease, cathepsin K....Pages 453-455
Front Matter....Pages 417-417
A combinatorial approach to the identification of cysteine protease substrates and inhibitors by application of a solid-phase fluorescence quenching assay....Pages 456-458
Pseudopeptide farnesyl-protein transferase inhibitors containing 5,5-dimethylthiazolidine-4-carboxylic acid....Pages 459-460
Design of peptidomimetic farnesyltransferase inhibitors as anticancer agents....Pages 461-462
Protein farnesyltransferase exhibits pH-dependent activity towards H-Ras peptide substrates....Pages 463-464
Biosynthesis and enzymatic characterization of human SKI-1 and the processing of its inhibitory prosegment....Pages 465-466
Structural studies of peptide inhibitors bound to hepatitis C virus protease yield insights into the mechanism of action of the enzyme....Pages 467-469
Optimization of a continuous assay for obtaining sensitive kinetic data on the inhibition of the HCV NS3 protease....Pages 470-471
Molecular docking of peptide inhibitors to the hepatitis C virus NS3 protease....Pages 472-473
Analysis of substrate specificity of HIV protease species....Pages 474-475
Structure/activity studies of peptide library-based integrase inhibitors....Pages 476-477
(Z)-Alkene phospho-Ser- cis -Pro substrate analog for Pin1, a phosphorylation-dependent peptidyl-prolyl isomerase....Pages 478-480
 C -terminal peptides as inhibitors and probes of mammalian ribonucleotide reductase....Pages 481-483
Front Matter....Pages 485-485
Expressed protein ligation: A new tool for studying protein structure and function....Pages 487-489
Combinatorial synthesis of de novo metalloproteins with tuned redox potential....Pages 490-492
Catalysis of pyridoxal phosphate mediated transamination....Pages 493-495
Synthetic steps toward de novo designed catalytic five helix bundle proteins....Pages 496-497
HisH + -His reactive sites in catalytic four-helix bundle catalysts....Pages 498-499
Semisynthetic approaches for the design of proteins with catalytic activity using fatty acid binding protein as a scaffold....Pages 500-502
A peptide spacer in a fullerene (C 60 )-based donor-acceptor dyad....Pages 503-504
Complexation of metal ions by pseudopeptides....Pages 505-506
Front Matter....Pages 485-485
Photomodulation of conformational states in cyclic peptides by cis/trans isomerization of azobenzene....Pages 507-508
Design and synthesis of two potent amide linked cyclic analogs of the hormone angiotensin II confirm the importance of ring cluster and relay system in its possible bioactive conformation....Pages 509-510
Endothelin precursor isoforms: Structural basis for rational drug design of ECE inhibitors....Pages 511-512
Rational development of an anti-HIV protein active at low picomolar concentrations....Pages 513-515
Rational engineering of a miniprotein inhibitor of HIV-1 infectivity....Pages 516-518
Design and synthesis of a chimeric TASP molecule as potential inhibitor in cell adhesion processes....Pages 519-520
Design and synthesis of salt-insensitive cyclic α-defensins....Pages 521-522
Conformational studies on three synthetic C -terminal fragments of the α subunit of a Gs protein....Pages 523-524
Insights into glycoproteins: A structural motif for mucins from a glycopeptide....Pages 525-527
Front Matter....Pages 529-529
Towards artificial antibodies: Protein surface recognition by synthetic receptors....Pages 531-533
Synthetic oxytocin receptors prepared by molecular imprinting....Pages 534-535
Peptide mimetics of erythropoietin are powerful probes of receptor activation mechanisms....Pages 536-538
Recombinant, C -terminally tagged forms of the human insulin receptor extracellular domain retain insulin binding ability....Pages 539-540
New dimensions in the design of potent and receptor selective melanotropin analogs....Pages 541-542
Design and biological activity of new high-affinity ligands for the urokinase-type plasminogen activator receptor (CD87)....Pages 543-545
Total synthesis of maxadilan and its disulfide isomers, and structural requirements for binding to the PACAP type 1 receptor....Pages 546-547
Solid state conformation of serine 3 DPDPE....Pages 548-549
The cation-π interaction: From structural biology to neuroreceptor binding sites....Pages 550-552
Front Matter....Pages 553-553
Chemoenzymatic synthesis of lipidated peptide and protein conjugates: Tools for the study of biological signal transduction....Pages 553-557
Bone-targeted, nonpeptide inhibitors of the Src SH2 domain: Structure-based design and structure-activity relationships....Pages 558-560
Front Matter....Pages 553-553
Nonpeptide inhibitors of the pp60 c-src (Src) SH2 domain: Discovery of a novel phosphotyrosine mimetic....Pages 561-562
Phosphotyrosyl peptides targeted to the SH2 domain are potent inhibitors of the kinase activity of pp60 c-src ....Pages 563-565
Novel phosphotyrosyl mimetics for the preparation of potent small molecule Grb2 SH2 domain inhibitors....Pages 566-567
High affinity nonphosphorylated cyclic peptide inhibitors of Grb2-SH2/growth factor receptor interactions....Pages 568-570
NMR based solution structure and dynamics of a nonphosphorylated cyclic peptide inhibitor for the Grb2 SH2 domain....Pages 571-572
Potent Grb2-SH2 antagonists containing asparagine mimetics....Pages 573-575
Design and synthesis of a new tyrosine analog having χ 1 and χ 2 angles constrained to values observed for an SH2 domain-bound phosphotyrosyl residue....Pages 576-578
Synthesis of more rigid consolidated ligands for the dual Src homology domain SH(32) of Abelson: Strategies to achieve higher affinities....Pages 579-580
A common ligand-binding site in G-protein coupled receptors....Pages 581-582
Bound conformations for ligands of G-protein coupled receptors....Pages 583-584
Modeling of secretin-like G protein coupled receptors....Pages 585-586
Synthetic peptides of the α subunit of G s protein inhibit receptor mediated adenylyl cyclase....Pages 587-588
Point mutation in TM6 of the melanocortin-4 receptor results in agonist activity of the MC4R antagonist SHU9119....Pages 589-591
Modulation of NK-2 receptor associated G-protein signaling by alteration of the aromatic residue at position six in neurokinin A analogs....Pages 592-593
Peptide mimetics of receptor extracellular domains modulate signal transduction by P2Y 2 receptors....Pages 594-596
Molecular characterization of the interaction between parathyroid hormone and its receptor....Pages 597-599
Glucagon receptor causes glucagon-dependent activation of Erk1/2 in H22 stable cell lines....Pages 600-601
Peptides for elucidating the signal tranduction pathways of CTLA-4 and CD28....Pages 602-603
Design and synthesis of inhibitors of the protein tyrosine phosphatase, SHP-2....Pages 604-605
Front Matter....Pages 607-607
Efficacy: What is it, and why you should care....Pages 609-611
Front Matter....Pages 607-607
Development of a chemical microarray technology....Pages 612-613
Cyclopentapeptides as conformational templates for validating three dimensional models of pharmacophores....Pages 614-615
Novel opioid peptides as kappa opioid receptor antagonists....Pages 616-618
H-Tyr-Tic-Phe-OH related δ opioid agonists and antagonists have similar receptor-bound conformations but different pharmacophores....Pages 619-620
Mapping the binding epitopes of IGF-1 and a phage-library derived peptide that inhibits IGFBP-1 binding to insulin-like growth factor....Pages 621-623
Stereochemical requirements for receptor recognition of the μ-opioid peptide endomorphin-1: Biological activity, NMR and conformational analysis of D-amino acid substituted analogs....Pages 624-625
Stimulation and suppression of the immune response and hemopoiesis by novel natural and synthetic peptides....Pages 626-627
Relating peptide presentation and biological response through supported films of peptide amphiphiles....Pages 628-629
Studying the influence of prolyl amide geometry on bioactivity with 5- t -butylproline oxytocin analogs....Pages 630-631
The effect of disulfide bond replacement by a methylenedithioether bond on the biological activity of oxytocin and deaminooxytocin....Pages 632-633
Increased serum stability of neurotensin analogs containing arginine mimics....Pages 634-635
Synthesis and pharmacological evaluation of a new series of bombesin analogs....Pages 636-638
Molecular pharmacology of vasopressin receptors....Pages 639-640
Discovery of new lead for the design of antagonists of human vasopressin(VP)V 1b receptor....Pages 641-642
Biological studies on chimeric dimers of oxytocin and the V 2 -antagonist, d(CH 2 ) 5 [D-Ile 2 , Ile 4 ]arginine vasopressin....Pages 643-644
Structure and activity of human parathyroid hormone N -terminal fragments in solution....Pages 645-646
Homology-based analysis of thrombin receptors....Pages 647-648
Substitution of cysteic acid for the seven phosphorylated residues in bovine rhodopsin C -terminal peptide....Pages 649-650
The receptor binding domain of apolipoprotein E, linked to a model class A amphipathic helix, enhances internalization and degradation of LDL in fibroblasts....Pages 651-652
Multimeric forms of lebetin peptide enhance the inhibition of platelet aggregation....Pages 653-654
Front Matter....Pages 607-607
New LHRH antagonists with enhanced biological activity: Preclinical and clinical results....Pages 655-657
Novel, water soluble and long acting GnRH antagonists....Pages 658-659
Relaxin and relaxin-related peptides: Synthesis, structure and biological function....Pages 660-663
Towards defining the biologically active site of relaxin....Pages 664-665
Solution structure and RNA-binding activity of the N -terminal leucine-repeat region of hepatitis delta antigen....Pages 666-667
SAR of the novel neuropeptides orexin-A and B....Pages 668-670
Glucagon-like peptide-1 and analogs: A structure/function analysis....Pages 671-673
Engineering and chemical synthesis of the HCV protease transmembrane protein cofactor NS4A....Pages 674-675
Front Matter....Pages 677-677
Can a discontinuous viral antigenic site be chemically reproduced? A rational approach to a difficult problem....Pages 679-680
An HLA class II restricted T-cell is able to recognize about a million different peptides....Pages 681-682
Identification and optimization of antigens for T cell clones of clinical relevance using positional scanning combinatorial libraries....Pages 683-684
 In situ identification of T helper cell epitopes from a cellulose-bound peptide array....Pages 685-686
Cells activation modulates binding of an LFA-1 peptide to the T-cell adhesion receptors....Pages 687-688
A CD28 CDR3 peptide analog inhibits CD4+ T-cell proliferation in vitro ....Pages 689-690
Induction of an Ag-specific CTL response by a conformationally biased agonist of human C5a anaphylatoxin as a molecular adjuvant....Pages 691-692
Modulation of proteasomal activity in vitro induces the generation of an HLA-A✶0201 specific CTL-defined epitope derived from the melanoma-associated antigen MAGE-3....Pages 693-694
Evaluation of the immunogenicity of peptide and DNA constructs for HER-2/neu epitopes....Pages 695-696
Lipophilic modifications of peptide epitopes: T-cell response and susceptibility to peptidases....Pages 697-699
Peptide vaccine strategy for immunotherapy of HER-2/neu overexpressing cancers....Pages 700-701
Rational design of a subtype-specific peptide vaccine against Neisseria meningitis ....Pages 702-703
Front Matter....Pages 677-677
Immune response to a conformational peptide vaccine for HTLV-1....Pages 704-705
Synthetic peptide-based HIV vaccine induces protective immunity in SHIV-rhesus model....Pages 706-707
Recombinant MOG from baculovirus inhibits anti-hMOG(30-50) antibodies detected by the synthetic antigen [Asn 31 (Glc)]hMOG(30-50)....Pages 708-709
Front Matter....Pages 711-711
Design and synthesis of prion peptidyl mimetics for the detection and purification of prion proteins....Pages 713-714
Synthesis of amyloid β-peptides: Segment condensation of sparingly soluble protected peptides in chloroform-phenol mixed solvent....Pages 715-716
Conformational changes in native and HCHW A-D (E22Q) mutant forms β of-amyloid....Pages 717-718
Fibril formation and neurotoxicity by a herpes simplex virus glycoprotein B fragment with homology to Alzheimer’ β amyloid peptide....Pages 719-720
Amyloid fibril formation by partially unfolded islet amyloid polypeptide (IAPP)....Pages 721-723
Front Matter....Pages 725-725
Post-translational modification: A two-dimensional strategy for molecular diversity of Conus peptides....Pages 727-729
Structural studies on α-conotoxin SI....Pages 730-732
Antiamoebin: A polypeptide ion carrier and channel....Pages 733-735
Development of novel peptide antibiotics for vancomycin resistant infection using the “one-bead, one-compound” combinatorial library method....Pages 736-737
Can machine learning and combinatorial chemistry coexist? An antimicrobial peptide case study....Pages 738-739
Interaction of gramicidin S and its biologically active analogs with phospholipid bilayers....Pages 740-741
Biological activities of Polymyxin B nonapeptide analogs....Pages 742-743
Complexation analysis of the antimicrobial salivary histatin peptides....Pages 744-745
Design, synthesis, and antibacterial activity of a peptidomimetic library....Pages 746-747
 De novo design of small cyclic antimicrobial peptides....Pages 748-749
Cell lysis and its specificity induced by basic peptides are determined by difference of hydrophobicity....Pages 750-751
Modulation of specificity in cyclic antimicrobial peptides by amphipathicity....Pages 752-753
Front Matter....Pages 725-725
Effect of structural and chemico-physical factors on the biological activity of linear antimicrobial peptides....Pages 754-755
Synthesis of magainin 2 dimer and its interaction with phospholipid bilayer....Pages 756-757
SPC3, an HIV-derived multibranched peptide, triggers an ionic conductance in Xenopus oocytes....Pages 758-759
Role of disulfide bonds in the structure and activity of ShK toxin....Pages 760-761
Probing SAR of FLRF-NH 2 with its N - and C -terminally modified analogs and retro-inverso peptides....Pages 762-763
Front Matter....Pages 765-765
Chemical and biological consequences of sugar incorporation into a potential N -glycosylation site in the tubulin-binding repeat of tau protein....Pages 767-769
Practical glycopeptide analgesics: Blood-brain barrier transport and binding of glycosylated enkephalin analogs....Pages 770-772
Synthesis and application of a glycoprotein derived from the proteoglycan linkage structure....Pages 773-774
Synthesis of glycopeptide modified IgE epitopes....Pages 775-776
Lipoamino acid based glycoconjugates for peptide and drug delivery....Pages 77-78
Novel lipoamino acid and liposaccharide based peptide delivery system for tumor selective somatostatin analogs....Pages 779-781
Regioselective conjugation of chitosan with a peptide related to an active sequence of laminin....Pages 782-783
Fully automated synthesis of peptide-oligonucleotide conjugates....Pages 784-785
Chemical synthesis of cyclic peptide nucleic acid-peptide hybrids....Pages 786-787
Recognition of RNA and DNA targets by peptide nucleic acids....Pages 788-789
Synthesis of PNA-peptide conjugates and their interactions with DNA....Pages 790-791
A new Tc(I) radiolabeling method for peptides: Evaluation of neurotensin analogs for tumor targeting....Pages 792-793
Front Matter....Pages 795-795
Perspectives for the new peptide millennium....Pages 797-804