Chapter
1.3.3 Polyplex Micelles for Safe Endosome Escape
1.3.4 Polyplex Micelles for Nuclear Translocation
1.3.5 Polyplex Micelles for Efficient Transcription
1.4 Design Criteria of Block Catiomers Toward Systemic Gene Therapy
1.5 Rod Shape or Toroid Shape
Chapter 2 Manipulation of Molecular Architecture with DNA
2.2 Molecular Structure of DNA
2.3 Immobile DNA Junctions
2.4 Topologically Unique DNA Molecules
2.5 DNA Tiles and Their Assemblies
2.7 DNA Origami as a Molecular Peg Board
2.8 Molecular Machines Made of DNA Origami
2.9 DNA Origami Pinching Devices
2.10 Novel Design Principles
2.11 DNA‐PAINT: An Application of DNA Devices
Chapter 3 Chemical Assembly Lines for Skeletally Diverse Indole Alkaloids
3.2 Macmillan's Collective Total Synthesis by Means of Organocascade Catalysis
3.3 Systematic Synthesis of Indole Alkaloids Employing Cyclopentene Intermediates by the Zhu Group
3.4 Biogenetically Inspired Synthesis Employing a Multipotent Intermediate by the Oguri Group
Chapter 4 Molecular Technology for Injured Brain Regeneration
4.2 Biology of Angiogenesis
4.3 Angiogenesis for Injured Brain Regeneration
4.4 Molecular Technology to Promote Angiogenesis
4.5 Biology of Cell Cycle
4.6 Biology of Neurogenesis
4.7 Molecular Technology to Promote Neuron Regeneration
Chapter 5 Engineering the Ribosomal Translation System to Introduce Non‐proteinogenic Amino Acids into Peptides
5.2 Decoding the Genetic Code
5.3 Aminoacylation of tRNA by Aminoacyl‐tRNA Synthetases
5.4 Methods for Preparing Noncanonical Aminoacyl‐tRNAs
5.4.1 Ligation of Aminoacyl‐pdCpA Dinucleotide with tRNA Lacking the 3′‐Terminal CA
5.4.2 Post‐aminoacylation Modification of Aminoacyl‐tRNA
5.4.3 Misacylation of Non‐proteinogenic Amino Acids by ARSs
5.4.4 Flexizyme, an Aminoacylation Ribozyme
5.5 Methods for Assigning Non‐proteinogenic Amino Acids to the Genetic Code
5.5.1 The Nonsense Codon Method
5.5.2 Genetic Code Reprogramming
5.5.3 The Four‐base Codon Method
5.5.4 The Nonstandard Base Method
5.6 Limitation of the Incorporation of Noncanonical Amino Acids: Substrate Scope
5.7 Improvement of the Substrate Tolerance of Ribosomal Translation
5.8 Ribosomally Synthesized Noncanonical Peptides as Drug Discovery Platforms
Chapter 6 Development of Functional Nanoparticles and Their Systems Capable of Accumulating to Tumors
6.2 Accumulation Based on Aberrant Morphology and Size
6.3 Accumulation Based on Aberrant pH Microenvironment
6.4 Accumulation Based on Temperature of Tumor Microenvironment
Chapter 7 Glycan Molecular Technology for Highly Selective In Vivo Recognition
7.1 Molecular Technology for Chemical Glycan Conjugation
7.1.1 Conjugation to Lysine
7.1.2 Conjugation to Cysteine
7.1.3 Bioorthogonal Conjugation
7.1.4 Enzymatic Glycosylation
7.2 In Vivo Kinetic Studies of Monosaccharide‐Modified Proteins
7.2.1 Dissection‐Based Kinetic and Biodistribution Studies: Effects of Protein Modification by Galactose, Mannose, and Fucose
7.2.2 Noninvasive Imaging of In Vivo Kinetic and Organ‐Specific Accumulation of Monosaccharide‐Modified Proteins
7.3 In Vivo Kinetic Studies of Oligosaccharide‐Modified Proteins
7.3.1 In Vivo Kinetics of Proteins Modified by a Few Molecules of N‐glycans
7.3.2 In Vivo Kinetics of Proteins Modified by Many N‐glycans: Homogeneous N‐glycoalbumins
7.3.3 In Vivo Kinetics of Proteins Modified by Many N‐glycans: Heterogeneous N‐glycoalbumins
7.3.4 Tumor Targeting by N‐glycoalbumins
7.3.5 Glycan Molecular Technology on Live Cells: Tumor Targeting by N‐glycan‐Engineered Lymphocytes
7.4 Glycan Molecular Technology Adapted as Metal Carriers: In Vivo Metal‐Catalyzed Reactions within Live Animals
Chapter 8 Molecular Technology Toward Expansion of Nucleic Acid Functionality
8.2 Molecular Technologies that Enable Genetic Alphabet Expansion
8.2.1 Nucleotide Modification
8.2.2 Unnatural Base Pairs (UBPs) as Third Base Pairs Toward Expansion of Nucleic Acid Functionality
8.2.3 High‐Affinity DNA Aptamer Generation Using the Expanded Genetic Alphabet
8.3 Molecular Technologies that Enable Fluorescence Blinking Control
8.3.1 Single Molecule Detection Based on Blinking Observations
8.3.3 Control of Fluorescence Blinking by DNA Structure
8.3.3.3 Isomerization Blinking
Chapter 9 Molecular Technology for Membrane Functionalization
9.2 Synthetic Approach for Membrane Functionalization
9.2.1 Formation of Multipass Transmembrane Structure
9.2.2 Formation of Supramolecular Ion Channels
9.2.3 Demonstration of Ligand‐Gated Ion Transportation
9.2.4 Light‐Triggered Membrane Budding
9.3 Semi‐biological Approach for Membrane Functionalization
9.3.1 Mechanical Analysis of the Transmembrane Structure of Membrane Proteins
9.3.2 Development of the Nanobiodevice Using a Membrane Protein Expressing in the Inner Ear
9.3.3 Improvement of Protein Performance by Genetic Engineering
Chapter 10 Molecular Technology for Degradable Synthetic Hydrogels for Biomaterials
10.1 Degradation Behavior of Hydrogels
10.2 Polylactide Copolymer
10.3 Trimethylene Carbonate Derivatives
Chapter 11 Molecular Technology for Epigenetics Toward Drug Discovery
11.3 Isozyme‐Selective Histone Deacetylase (HDAC) Inhibitors
11.3.1 Identification of HDAC3‐Selective Inhibitors by Click Chemistry Approach
11.3.2 Identification of HDAC8‐Selective Inhibitors by Click Chemistry Approach and Structure‐Based Drug Design
11.3.3 Identification of HDAC6‐Insensitive Inhibitors Using C–H Activation Reaction
11.3.4 Identification of HDAC6‐Selective Inhibitors by Substrate‐Based Drug Design
11.3.5 Identification of SIRT1‐Selective Inhibitors by Target‐Guided Synthesis
11.3.6 Identification of SIRT2‐Selective Inhibitors by Structure‐Based Drug Design and Click Chemistry Approach
11.4 Histone Lysine Demethylase (KDM) Inhibitors
11.4.1 Identification of KDM4C Inhibitors by Structure‐Based Drug Design
11.4.2 Identification of KDM5A Inhibitors by Structure‐Based Drug Design
11.4.3 Identification of KDM7B Inhibitors by Structure‐Based Drug Design
11.4.4 Identification of LSD1 Inhibitors by Target‐Guided Synthesis
11.4.5 Small‐Molecule‐Based Drug Delivery System Using LSD1 and its Inhibitor
Chapter 12 Molecular Technology for Highly Efficient Gene Silencing: DNA/RNA Heteroduplex Oligonucleotides
12.2 Therapeutic Oligonucleotides
12.3 Chemical Modifications of Therapeutic Oligonucleotide
12.3.1 Modifications of Internucleotide Linkage
12.3.2 Modifications of Sugar Moiety
12.4 Ligand Conjugation for DDS
12.4.1 Development of Ligand Molecules for Therapeutic Oligonucleotides
12.4.2 Vitamin E for Ligand Molecule
12.4.3 siRNA Conjugated with Tocopherol
12.4.4 ASO Conjugated with Tocopherol
12.5 DNA/RNA Heteroduplex Oligonucleotide
12.5.1 Basic Concept of Heteroduplex Oligonucleotide
12.5.2 HDO Conjugated with Tocopherol (Toc‐HDO)
12.5.2.1 Design of Toc‐HDO
12.5.2.2 Potency of Toc‐HDO
12.5.2.3 Adverse Effect of Toc‐HDO
12.5.2.4 Mechanism of Toc‐HDO
Chapter 13 Molecular Technology for Highly Sensitive Biomolecular Analysis: Hyperpolarized NMR/MRI Probes
13.2 Requirements for HP Molecular Imaging Probes
13.3 HP 13C Molecular Probes for Analysis of Enzymatic Activity
13.3.2 HP 13C Probes for Analysis of Glycolysis and Tricarboxylic Acid Cycle
13.3.3 𝛄‐Glutamyl‐[1‐13C]glycine: HP 13C Probe for Analysis of 𝛄‐glutamyl Transpeptidase
13.3.4 [1‐13C]Alanine‐NH2: HP 13C Probes for Analysis of Aminopeptidase N
13.4 HP 13C Molecular Probes for Analysis of the Chemical Environment
13.4.1 [1‐13C]Bicarbonate
13.4.2 [1‐13C]Ascorbate and Dehydroascorbate
13.4.3 [13C]Benzoylformic Acid for Sensing H2O2
13.4.4 [13C,D3]‐p‐Anisidine for Sensing of HOCl
13.4.5 [13C,D]EDTA for Sensing of Metal Ions
13.5 HP 15N Molecular Probes
13.6 A Strategy for Designing HP Molecular Probes
13.6.1 Scaffold Structure for Design of 15N HP Probes: [15N,D9]TMPA
13.6.2 Scaffold Structure for Designing 13C Hyperpolarized Probes
Chapter 14 Molecular Technologies in Life Innovation: Novel Molecular Technologies for Labeling and Functional Control of Proteins Under Live Cell Conditions
14.1 General Introduction
14.2 Ligand‐Directed Chemistry for Neurotransmitter Receptor Proteins Under Live Cell Condition and its Application
14.3 Affinity‐Guided DMAP Reaction for Analysis of Live Cell Surface Proteins
14.4 Coordination Chemistry‐Based Chemogenetic Approach to Switch the Activity of Glutamate Receptors in Live Cells
Chapter 15 Molecular Technologies for Pseudo‐natural Peptide Synthesis and Discovery of Bioactive Compounds Against Undruggable Targets
15.2 Peptides Could Target Undruggable Targets
15.2.1 Druggable Proteins
15.2.2 Undruggable Proteins
15.2.3 Natural Peptides as Drugs
15.2.4 Modification to Peptides can Improve Their Drug‐Like Characteristics
15.2.4.1 Macrocyclization
15.2.4.2 Amino Acids with Unnatural Side Chains
15.2.4.3 Backbone Modifications Including N‐Methylation
15.2.4.4 Cyclosporin – A Membrane‐Permeable Anomaly
15.2.4.5 Membrane Permeability Cannot be Calculated from Amino Acid Content
15.2.5 Cyclosporin – The Inspiration for the Cyclic Peptide Approach to Undruggable Targets
15.3 Molecular Technologies to Discover Functional Peptides
15.3.1 Ribosomal Synthesis of Peptides
15.3.2 Natural Peptide Synthesis is an Efficient Method to Generate Huge Libraries
15.3.3.1 Intracellular Peptide Selection
15.3.3.3 A Cell‐Free Display, mRNA Display
15.3.4 Other Methods of Selection
15.4 Molecular Technology for Pseudo‐natural Peptide Synthesis and Its Use in Peptide Drug Discovery
15.4.1 The Need for Pseudo‐natural Synthesis – The Limitations of SPPS
15.4.2 Intein Cyclization and SICLOPPS
15.4.3 Post‐translation Modification
15.4.4 Genetic Code Expansion
15.4.5 Replacing Amino Acids in Translation
15.4.6 Genetic Code Reprogramming
Molecular Technology
：Life Innovation
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