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1 | (34) |
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1.1 Protein-Protein Interactions and Their Small-Molecule Modulators |
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1 | (7) |
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1.1.1 Characteristics of Protein-Protein Interactions |
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1 | (2) |
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1.1.2 Intervention of Protein-Protein Interactions Using Small Molecules |
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3 | (2) |
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1.1.2.1 Leukocyte Function-Associated Antigen-1 |
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5 | (1) |
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1.1.2.2 Inhibitor of Apoptosis Proteins |
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6 | (1) |
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6 | (1) |
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1.1.2.4 Human Immunodeficiency Virus Integrase |
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6 | (1) |
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1.1.2.5 B-Cell Lymphoma-2 Family/B-Cell Lymphoma-2 Homology 3 Proteins Interaction |
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7 | (1) |
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1.1.2.6 Mouse Double Minute 2-p53 Interaction |
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7 | (1) |
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1.2 Features of Peptide as Molecular Tools |
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8 | (4) |
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1.2.1 Advantages of Peptides as Molecular Tools |
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8 | (3) |
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1.2.2 Disadvantages of Peptides as Molecular Tools |
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11 | (1) |
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1.3 Helical Structures and Their Characterization |
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12 | (6) |
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1.3.1 Different Types of Helices |
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12 | (1) |
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12 | (1) |
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12 | (1) |
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13 | (2) |
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1.3.2 Characterization of Helical Peptides |
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15 | (1) |
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1.3.2.1 Circular Dichroism |
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15 | (1) |
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1.3.2.2 X-ray Crystallography |
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16 | (1) |
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1.3.2.3 Nuclear Magnetic Resonance (NMR) |
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17 | (1) |
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1.4 Stabilization of Peptides |
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18 | (9) |
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1.4.1 Peptide Stabilization via Cyclization |
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18 | (1) |
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18 | (1) |
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19 | (2) |
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1.4.2 Peptide Stabilization via Backbone Reconstruction |
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21 | (1) |
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21 | (2) |
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23 | (4) |
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27 | (8) |
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2 Construction of Constrained Helices |
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35 | (34) |
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2.1 Side-Chain Cross-linking |
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35 | (22) |
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35 | (2) |
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37 | (5) |
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2.1.3 All-Hydrocarbon Stapled Peptide |
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42 | (6) |
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48 | (8) |
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56 | (1) |
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57 | (5) |
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2.2.1 Macrocycle-Based N-cap Templates |
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58 | (2) |
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2.2.2 Hydrogen Bond Surrogate Approaches |
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60 | (1) |
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2.2.3 N-Terminal Side Chain Constrains as Helix-Nucleating Templates |
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61 | (1) |
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62 | (7) |
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3 Properties of Stabilized Peptides |
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69 | (38) |
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69 | (11) |
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69 | (5) |
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74 | (5) |
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79 | (1) |
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80 | (4) |
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80 | (1) |
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3.2.2 Cyclization Position |
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81 | (3) |
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84 | (1) |
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84 | (5) |
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3.3.1 Amphiphilicity: Hydrophobicity and Isoelectric Point |
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84 | (3) |
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87 | (2) |
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89 | (1) |
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89 | (8) |
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97 | (1) |
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3.5.1 Proteolytic Stability |
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91 | (4) |
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3.5.2 Pharmacokinetic Properties |
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95 | (3) |
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98 | (5) |
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103 | (4) |
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4 Applications of Constrained Helices |
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107 | (52) |
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107 | (36) |
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107 | (3) |
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4.1.2 B-Cell Lymphoma 2 (MCL-l/BCL-2/BCL-XL)-BID/Noxa/BAX/BIM/PUMA |
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110 | (4) |
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114 | (4) |
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4.1.4 Insulin Receptor Substrate 1 |
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118 | (2) |
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120 | (4) |
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124 | (2) |
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4.1.7 β-Catenin BCL-9/AXIN |
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126 | (4) |
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4.1.8 Epidermal Growth Factor Receptor |
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130 | (5) |
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4.1.9 Estrogen Receptor a |
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135 | (3) |
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4.1.10 Hypoxia-Inducible Factor |
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138 | (2) |
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4.1.11 Embryonic Ectoderm Development - Enhancer of Zeste Homolog 2 |
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140 | (3) |
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143 | (7) |
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143 | (5) |
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4.2.2 Respiratory Syncytial Virus F (RSV) |
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148 | (2) |
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150 | (2) |
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4.3.1 Glucokinase-Phospho-BAD |
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150 | (2) |
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152 | (7) |
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5 Stabilized Peptide Covalent Inhibitors |
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159 | (22) |
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5.1 Methodologies of Peptide Covalent Inhibitor |
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159 | (3) |
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160 | (2) |
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162 | (1) |
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162 | (15) |
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5.2.1 BCL-2 Family Proteins As Target |
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163 | (1) |
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5.2.2 MDM2 and MDM4 As Target |
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164 | (4) |
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5.2.3 Sulfonium Tethered Peptide |
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168 | (8) |
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176 | (1) |
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177 | (4) |
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6 Stabilized Peptide PROTAC |
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181 | (10) |
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6.1 Proteolysis-Targeting Chimera (PROTAC) |
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181 | (1) |
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6.2 Design of Peptide PROTAC |
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181 | (3) |
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6.2.1 Exploitation of E3 Ubiquitin Ligase-Recruiting Ligand |
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182 | (1) |
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6.2.2 Design of Stabilized Peptide Ligand |
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183 | (1) |
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184 | (1) |
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6.3 Therapeutic Applications of Stabilized Peptide PROTAC |
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184 | (4) |
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185 | (3) |
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6.3.2 Targeting β-Catenin |
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188 | (1) |
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188 | (3) |
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7 Stabilized Peptide for Drug Delivery |
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191 | (22) |
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7.1 Cell-Penetraying Peptides (CPPs) |
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191 | (5) |
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7.1.1 Classification of CPPs |
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192 | (1) |
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7.1.2 Mechanism of Cell Penetration of CPPs |
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193 | (1) |
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7.1.3 Applications of CPPs |
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194 | (2) |
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7.2 Cell-Permeable Cyclic Peptides (Cyclic CPPs) |
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196 | (8) |
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7.2.1 Cyclic CPPs-Mediated Drug Delivery |
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198 | (4) |
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202 | (2) |
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7.3 Co-assembly Nanocarrier System |
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204 | (2) |
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7.4 Examples of Stabilized Peptide Drugs |
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206 | (2) |
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208 | (5) |
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213 | (10) |
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8.1 The Development of Peptide-Stabilizing Methods |
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213 | (5) |
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8.2 Applications of Stabilized Helical Peptides |
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218 | (2) |
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220 | (3) |
Index |
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223 | |