Handbook of In Vivo Chemistry in Mice: From Lab to Living System

Cover......Page 1
Title Page......Page 5
Copyright......Page 6
Contents......Page 7
 1.1 Introduction......Page 17
 1.2 Origin and History of Laboratory Mice......Page 18
  1.3.1 Wild‐Derived Mice......Page 19
  1.3.3 Hybrid Mice......Page 20
  1.3.6 Congenic Mice......Page 24
  1.4.2 Transgenesis......Page 25
  1.4.3 Targeted Mutagenesis......Page 27
  1.4.5 Cre–loxP System......Page 29
  1.4.6 CRISPR/Cas9 System......Page 31
 1.6 Germ‐Free Mice......Page 32
 1.9 Immunocompetent and Immunodeficient Mice......Page 34
  1.11.2 Breeding Systems and Mating Schemes......Page 35
 1.15 Parental Behavior and Rearing Pups......Page 37
 1.16 Growth of Pups......Page 38
 1.18 Record Keeping and Colony Organization......Page 39
 1.20 Animal Models in Preclinical Research......Page 40
 References......Page 45
 2.1 Introduction......Page 49
  2.3.1 Substance Characteristics......Page 50
  2.3.2 Vehicle Characteristics......Page 51
  2.3.3 Frequency and Volume of Administration......Page 52
 2.4 Anesthesia......Page 53
  2.4.2 Injectable Agents......Page 54
 2.5 Euthanasia......Page 56
 2.6 Administration......Page 57
  2.6.2 Parenteral Administration......Page 58
   2.6.2.2 Intraperitoneal Administration......Page 60
   2.6.2.7 Epicutaneous Administration......Page 62
   2.6.2.9 Inhalational Administration......Page 67
   2.6.2.10 Retro‐orbital Administration......Page 68
 References......Page 69
  3.1.1 Basics of Luminescence......Page 71
  3.1.2 Appropriate Wavelengths for Live Animal Imaging......Page 72
  3.2.1 Fluorescent Molecules for Live Animal Imaging......Page 74
  3.2.2 How to Detect Fluorescence in Live Animals?......Page 77
  3.2.3 Activatable Probes......Page 78
  3.2.5 Application of Fluorescence Imaging to Drug Development......Page 84
 3.3 Luminescence Imaging in Live Animals......Page 85
   3.3.1.1 Firefly/Beetle Luciferin–Luciferase System......Page 86
   3.3.1.2 Coelenterazine‐Dependent Luciferase System......Page 92
   3.3.1.3 Chemiluminescence System......Page 98
  3.3.3 Luciferase‐Based Bioluminescence Probes for In Vivo Imaging......Page 100
 References......Page 103
 4.1 Introduction......Page 119
 4.2 High‐Frequency Ultrasound Imaging......Page 121
 4.3 Ultrasound Contrast Agents......Page 125
 4.4 Photoacoustic Imaging......Page 128
  4.5.1 Cardiovascular......Page 131
  4.5.2 Oncology......Page 136
  4.5.3 Developmental Biology......Page 137
 References......Page 139
 5.1 Introduction......Page 143
 5.2 Brief History of PET......Page 144
 5.3 Principles of PET......Page 145
 5.4 Small‐Animal PET Scanners......Page 149
  5.5.1 Metabolic Probe......Page 150
  5.5.2 Specific Receptor Targeting Probe......Page 151
  5.5.3 Gene Expression......Page 152
  5.5.5 Microenvironment Probe......Page 153
  5.5.6 Biological Processes......Page 154
  5.5.8 Nanoparticles......Page 156
  5.6.1 PET in Oncology Model......Page 157
   5.6.1.2 Personal Treatment Screening......Page 158
   5.6.1.3 Therapeutic Effect Monitoring......Page 159
   5.6.1.5 Drug Discovery......Page 160
  5.6.2 PET in Cardiology Model......Page 161
  5.6.3 PET in Neurology Model......Page 162
 5.7 PET Image Analysis......Page 163
 5.8 Outlook for the Future......Page 164
 Reference......Page 165
 6.1 Introduction......Page 167
 6.2 SPECT Devices Used in Small Animals......Page 168
  6.2.1 Innovative Preclinical Full‐Body SPECT Imager for Rats and Mice: γ‐CUBE......Page 171
  6.2.3 Innovative Preclinical Full‐Body CT Imager for Rats and Mice: X‐CUBE......Page 172
  6.2.5 Selected Applications Acquired on the CUBES......Page 173
   6.2.5.2 PET Imaging with β‐CUBE......Page 174
   6.2.5.3 CT Imaging with X‐CUBE......Page 177
  6.3.2 Characteristics of SPECT Imaging Probes......Page 178
 6.4 Radiolabeling......Page 179
  6.4.2 Radiolabeling with Technetium‐99m......Page 180
  6.4.5 Aromatic Electrophilic Substitution Reaction......Page 187
 6.5 In Vivo Imaging of Disease Models......Page 188
   6.5.1.1 Alzheimer\'s Disease......Page 189
   6.5.1.2 Parkinson\'s Disease......Page 190
   6.5.1.3 Cerebral Ischemia......Page 192
   6.5.2.2 Myocardial Ischemia......Page 193
   6.5.2.3 Imaging of Cancer......Page 194
 6.6 Conclusions......Page 195
 References......Page 196
 7.1 Introduction......Page 201
  7.2.1 Radiotherapy with β‐Emitting Nuclides......Page 202
  7.2.2 Radiotherapy Using α‐Emitting Nuclides......Page 204
  7.3.1 Labeled Target Compounds......Page 207
  7.3.2 211At‐Labeled Compounds......Page 208
  7.3.3 Chelating Agents for 90Y, 177Lu, 225Ac, 213Bi......Page 209
   7.3.4.1 Octreotate (TATE) and [Tyr3]‐Octreotide (TOC)......Page 211
   7.3.4.5 Minigastrin......Page 212
  7.3.6 Examples of Radiotherapeutic Agents and Target Diseases......Page 213
  7.4.1 Radiotheranostics Probe......Page 216
  7.4.3 Expectations and Challenges in Radiotheranostics......Page 218
  7.4.4 Boron Neutron Capture Therapy (BNCT)......Page 219
   7.4.5.2 Sodium Borocaptate (BSH)......Page 220
 References......Page 221
 8.1 Introduction......Page 225
  8.2.1 Origin of Metabolic Glycan Engineering......Page 226
  8.2.2 Expansion of the Methodology to Include Unnatural Functional Groups and Bio‐orthogonal Elaboration......Page 229
  8.3.1 Bio‐orthogonal Chemistries Amenable to Deployment in Live Animals......Page 232
  8.3.2 Bio‐orthogonal Chemistries Amenable to Deployment on Cells......Page 237
  8.4.1 Deployment of Unnatural Monosaccharides in Mammalian Cells......Page 239
  8.4.2 Unnatural Sugars that Label Glycans on Bacterial Cells......Page 241
 8.5 Cell‐ and Tissue‐Specific Delivery of Unnatural Sugars......Page 242
  8.5.2 Metabolically Label Cells Ex vivo Before Introducing Them In vivo......Page 243
  8.5.4 Employ Tissue‐Specific Enzymes to Release Monosaccharide Substrates......Page 245
  8.5.5 Deliver Monosaccharide Substrates via Liposomes......Page 247
  8.6.1 Imaging Glycans in Mice......Page 250
  8.6.2 Covalent Delivery of Therapeutics in Mice......Page 252
  8.7.1 Zebra Fish......Page 253
  8.7.2 Worms......Page 255
  8.8.1 Metabolic Glycan Engineering Offers a Test Bed for Bio‐orthogonal Chemistries......Page 256
 References......Page 257
  9.1.1 IEDDA Chemistry Between trans‐Cyclooctene and Tetrazine......Page 265
 9.2 In Vivo Applications of IEDDA Chemistry......Page 267
  9.2.1 Pretargeting Approach for Cell Imaging......Page 268
  9.2.2 Pretargeting Approach for In Vivo Imaging......Page 272
  9.2.3 Application of the Pretargeting Strategy for In Vivo Radio Imaging......Page 275
  9.2.4 In Vivo Drug Activation Using Bond‐cleaving Bio‐orthogonal Chemistry......Page 276
  9.2.5 Reloadable Materials Allow Local Prodrug Activation......Page 281
  9.2.6 Reloadable Materials Allow Local Prodrug Activation Using IEDDA Chemistry......Page 282
  9.2.7 Controlled Activation of siRNA Using IEDDA Chemistry......Page 288
 9.3 Future Outlook......Page 290
 References......Page 293
 10.1 Introduction......Page 297
  10.2.1 Ligand‐Directed Tosyl Chemistry......Page 298
  10.2.2 Ligand‐Directed Acyl Imidazole Chemistry......Page 300
 10.3 Labeling Chemistry of Targeted Covalent Inhibitors......Page 303
  10.3.1 Michael Acceptors......Page 306
  10.3.2 Haloacetamides......Page 309
  10.3.3 Activated Esters, Amides, Carbamates, and Ureas......Page 311
  10.3.4 Sulfur(VI) Fluorides......Page 313
  10.3.5 Other Warheads and Reactions......Page 316
 10.4 Conclusion......Page 317
 References......Page 318
 11.1 Introduction......Page 325
  11.2.1 Protein Decaging......Page 326
  11.2.2 Protein Bioconjugation......Page 327
  11.2.3 Small Molecule – Bond Formation......Page 335
  11.2.4 Small Molecule – Bond Cleavage......Page 340
  11.3.1 ArMs Utilizing Naturally Occurring Metals......Page 348
  11.3.2 ArMs Utilizing Abiotic Transition Metals......Page 351
 11.4 Concluding Remarks......Page 356
 References......Page 359
 12.1 Introduction......Page 371
 12.2 Catalytic Photo‐oxygenation of Aβ Using a Flavin–Peptide Conjugate......Page 373
 12.3 On–Off Switchable Photo‐oxygenation Catalysts that Sense Higher Order Amyloid Structures......Page 374
 12.4 Near‐Infrared Photoactivatable Oxygenation Catalysts: Application to Amyloid Disease Model Mice......Page 379
 12.5 Closing Remarks......Page 383
 References......Page 384
 13.1 Introduction......Page 389
  13.2.1 Physicochemical Properties of NPs......Page 391
  13.2.2 Surface Functionalization......Page 395
  13.2.3 Stimuli‐Responsive Nanomaterials......Page 397
  13.3.1 Lipidic Nanoplatforms......Page 400
  13.3.2 Polymer‐Based Nanoplatforms......Page 405
  13.3.3 Inorganic Nanoplatforms......Page 407
  13.3.4 Biomimetic Cell‐Derived Nanoplatforms......Page 409
 13.4 Conclusions......Page 410
 References......Page 411
 14.1 Introduction......Page 417
  14.2.1 UV Light‐Triggered Photocaged Strategy......Page 419
  14.2.2 UV Light‐Mediated Photoisomerization Strategy......Page 421
 14.3 Visible Light‐Responsive Theranostics......Page 424
 14.4 Near‐Infrared (NIR) Light‐Responsive Theranostics......Page 426
  14.4.1 NIR Light‐Mediated Drug Delivery Approach......Page 427
  14.4.2 NIR Light‐Mediated Photodynamic Therapy (PDT) Approach......Page 431
  14.4.3 NIR Light‐Mediated Photothermal Therapy (PTT) Approach......Page 435
 14.5 Conclusion and Prospects......Page 437
 References......Page 439
 15.1 Introduction......Page 449
  15.1.1 Light‐Sensitive Liposomes......Page 450
  15.2.1 Light‐Induced Oxidation......Page 451
  15.2.2 Photocrosslinking......Page 452
  15.2.3 Photoisomerization......Page 454
  15.2.4 Photocleavage......Page 456
  15.2.5 Photothermal Release......Page 458
 References......Page 460
 16.1 Introduction......Page 467
  16.2.1 Natural Ligands and Biomimetics......Page 468
  16.2.2 Phage Display Peptide Library Screening......Page 470
  16.2.3 Synthetic Peptide Library Screening......Page 474
  16.3.1 Therapeutic Peptides......Page 476
   16.3.1.2 Peptide Conjugates......Page 480
   16.3.2.1 Peptide–Drug Conjugates......Page 481
   16.3.2.2 Peptide‐Targeted Nanoparticles......Page 483
 16.4 Molecular Imaging Mediated by Targeting Peptides......Page 485
  16.4.1 Optical Imaging......Page 486
   16.4.1.2 Integrin αvβ3 – RGD Tripeptide Targeting Probes:......Page 487
  16.4.2 Positron Emission Tomography......Page 488
  16.4.3 Magnetic Resonance Imaging......Page 489
 16.5 Summary and Future Perspectives......Page 490
 References......Page 491
 17.1 Introduction......Page 505
 17.2 Liver and Liver‐Based Disease Targeting......Page 507
  17.2.1 Parenchymal Cell Targeting......Page 508
  17.2.2 Nonparenchymal Cell Targeting......Page 514
 17.3 Immune System Targeting......Page 517
  17.3.2 Peritoneal Macrophage Targeting......Page 519
  17.3.4 Brain Macrophage Targeting......Page 520
 17.4 Bacterial Cell Targeting......Page 521
  17.5.1 Natural Monosaccharide‐Based Methods......Page 522
  17.5.2 Synthetic Sugars......Page 524
  17.5.3 Complex Glycan Scaffold......Page 527
 References......Page 530
Index......Page 547
EULA......Page 563