Peptide-Based Drug Design

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130 Hilpert et al. Table 1 (Continued) MIC (�g/mL) Name Source Sequence Remark E. coli S. aureus Ref. Unusual 200 3.1 (45,46) amino acid composition ILPWKWPWWPWRR-NH2 Unusual 7.7 3.8 (47,48) amino acid composition KCFQWQRNMRKVRGPPVSCI �–Hairpin 256 128 (49,50) peptide (amino acids 19–38 of Lactoferrin) KCRQWQSKIRRTNP IFCIRR �-Sheet (amino 64 32 (50) acids 18–37 of Lactoferrin) LLGDFFRKSKEKIGKEF �-Helical >32 (�M) >32 (�M) (51,52) KRIVQRIKDFLRNLVPRTES Bacillus brevis cyclo-((D)Phe-Pro-Val-Orn-Leu)2 (Orn is Ornithine) Gramicidin S Indolicidin Bovine neutrophil Human, derived from Lactoferrin Lactoferricin H-20 Porcine, derived from Lactoferrin Lactoferricin P-20 GIGKFLHSAKKFGKAFVGEIMNS �-Helical 11.6 64 (53–55) LL37 Human neutrophils and various epithelial cells Magainin2 Xenopus laevisskin
Cationic Antimicrobial <strong>Peptide</strong>s 131 A + HA + Unusual Inactive 2 (56–58) amino acid HVUK composition R-Dab-Thr-Dab-Dab-Dab-(D) Cyclic 1.8 26 (59–61) Phe-Leu-Dab-Dab-Thr (Dab is lipopeptide diaminobutyric acid) RRRPRPPYLPRPRPPPFF Unusual 4 250 (62,63) PPRLPPRIPPGFPPRF amino acid PPRFP-NH2 composition RGGRLCYCRRRFCVCVGR �-Sheet 0.75–11 1.7–8 (64–66) IOA*IULA*A + PGA + KA + GALMGA + NMKA + AA + Nisin Lactococcus lactis Polymyxin B Bacillus polymyxa PR-39 Pig intestine KWCFRVCYRGICYRRCR �-Sheet 6.3–12.5 3.1–6.3 (67,68) Protegrin-1 Porcine leukocyte Tachyplesin I Horseshoe crab A ∗ , part of lanthionine; A + , part of 3-methyllanthionine; U, dehydroalanine; O, dehydrobutyrine.
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Peptide-Based Drug Design
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METHODS IN MOLECULAR BIOLOGY TM Pep
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Preface Natural products chemistry
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Contents Preface...................
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Contributors Nikolinka Antcheva •
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Contributors xi Alessandro Tossi
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2 Otvos advance of computer power a
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4 Otvos see derivatives active in b
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6 Otvos was designed based on ligan
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8 Otvos 27. Borghouts, C., Kunz, C.
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10 Bulet Key Words: Invertebrate im
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12 Bulet 6. 5 �L or higher volume
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14 Bulet 2.5.2.1. MALDI-TOF-MS 1. M
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16 Bulet 7. Small-volume low-protei
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18 Bulet 3. Centrifuge between 8000
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20 Bulet internal diameter). Increa
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22 Bulet interest. As no instrument
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24 Bulet 3. Incubate the plates in
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26 Bulet bioactive peptides from th
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28 Bulet 21. Chernysh, S., Kim, S.I
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3 Sequence Analysis of Antimicrobia
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Sequence Analysis of Antimicrobial
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4 The Spot Technique: Synthesis and
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The Spot Technique 49 3. For amine
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The Spot Technique 51 2. Biotinylat
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The Spot Technique 53 the solutions
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The Spot Technique 55 solution. Ens
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The Spot Technique 57 (see Fig. 3)
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The Spot Technique 59 Fig. 5. Princ
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The Spot Technique 61 library, the
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The Spot Technique 63 7. Regenerati
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The Spot Technique 65 following rul
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The Spot Technique 67 20. Atherton,
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The Spot Technique 69 50. Bolger, G
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5 Analysis of A� Interactions Usi
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Analysis of Aβ Interactions 73 are
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Analysis of Aβ Interactions 75 Ana
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Analysis of Aβ Interactions 77 3.
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Page 98 and 99: 6 NMR in Peptide Drug Development J
Page 100 and 101: NMR of Peptides 89 usually require
Page 102 and 103: NMR of Peptides 91 limiting the siz
Page 104 and 105: NMR of Peptides 93 and STD NMR expe
Page 106 and 107: NMR of Peptides 95 The basis of the
Page 108 and 109: NMR of Peptides 97 Fig. 5. Overlay
Page 110 and 111: NMR of Peptides 99 Fig. 7. Schemati
Page 112 and 113: NMR of Peptides 101 4.4.2. Saturati
Page 114 and 115: NMR of Peptides 103 4.6. Diffusion
Page 116 and 117: NMR of Peptides 105 Fig. 13. Propos
Page 118 and 119: NMR of Peptides 107 protein prevent
Page 120 and 121: NMR of Peptides 109 6. Wuthrich, K.
Page 122 and 123: NMR of Peptides 111 45. Morris, K.
Page 124 and 125: NMR of Peptides 113 78. Aumailley,
Page 126 and 127: 116 Copps et al. Fig. 1. Potential
Page 128 and 129: 118 Copps et al. Fig. 2. Flowchart
Page 130 and 131: 120 Copps et al. 10. In accordance
Page 132 and 133: 122 Copps et al. Fig. 3. DSSP for g
Page 134 and 135: 124 Copps et al. ingly with the sam
Page 136 and 137: 126 Copps et al. 19. Essman, U., Pe
Page 138 and 139: 128 Hilpert et al. Key Words: Scree
Page 142 and 143: 132 Hilpert et al. different natura
Page 144 and 145: 134 Hilpert et al. wt A C D E F …
Page 146 and 147: 136 Hilpert et al. methods primaril
Page 148 and 149: 138 Hilpert et al. Table 2 (Continu
Page 154 and 155: 144 Hilpert et al. Table 3 Summary
Page 158 and 159: 148 Hilpert et al. of substituting
Page 160 and 161: 150 Hilpert et al. in models that c
Page 162 and 163: 152 Hilpert et al. than control. Gi
Page 164 and 165: 154 Hilpert et al. Table 4 Accuracy
Page 166 and 167: 156 Hilpert et al. 25. Pini, A., Gi
Page 168 and 169: 158 Hilpert et al. 55. Giacometti,
Page 170 and 171: 9 Investigating the Mode of Action
Page 172 and 173: Proline-Rich Antimicrobial Peptides
Page 186 and 187: 10 Serum Stability of Peptides Håv
Page 188 and 189: Serum Stability of Peptides 179 2.
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Serum Stability of Peptides 181 9.
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Serum Stability of Peptides 183 �
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Serum Stability of Peptides 185 13.
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11 Preparation of Glycosylated Amin
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Glycosylated Amino Acid Synthesis 1
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12 Synthesis of O-Phosphopeptides o
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Solid-Phase Synthesis of O-Phosphop
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13 Peptidomimetics: Fmoc Solid-Phas
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Peptidomimetics 225 O O R S N H Pep
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Peptidomimetics 227 not without its
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Peptidomimetics 229 Oxidation step:
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Peptidomimetics 231 of peptidosulfo
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Peptidomimetics 233 8. Allow the re
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Peptidomimetics 235 3.3.2. Solid-Ph
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Peptidomimetics 237 On the other ha
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Peptidomimetics 239 nitrogen (73).
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Peptidomimetics 241 3. Cover the re
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Peptidomimetics 243 efficient synth
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Peptidomimetics 245 55. Alsina, J.,
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14 Synthesis of Toll-Like Receptor-
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Lipopeptides 249 2. Materials 2.1.
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Lipopeptides 251 Fig. 1. Structural
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Lipopeptides 253 8. To enable lipid
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Lipopeptides 255 Representative res
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Lipopeptides 257 Fig. 2. Immunogeni
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Lipopeptides 259 8. A large plastic
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Lipopeptides 261 26. Nardin, E.H.,
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264 Otvos response, synthetic pepti
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266 Otvos Fig. 3. Schematic present
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268 Otvos 3. Methods The main goal
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270 Otvos 3.2.3. Purification and Q
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272 Otvos 6. Meyer, D., and Torres,
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16 Cysteine-Containing Fusion Tag f
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Targeted Therapeutic and Imaging Ag
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Index A A� peptides aggregation a
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Index 297 phosphopeptides influenci
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Index 299 for genetically synthetic
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Index 301 peptidosulfonamide, disad
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Index 303 solid phase, 180, 214 sul
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