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by Natanya Civjan
Chemical Biology: Approaches to Drug Discovery and Development to Targeting Disease
Cover
Copyright
Title Page
Preface
Contributors
Part I: Drug Discovery and Development
Chapter 1: The Role of Chemical Biology in Drug Discovery
1.1 Introduction
1.2 Target Identification and Validation
1.3 Reagent and Assay Development
1.4 Lead Discovery
1.5 Hit to Lead/Probe
1.6 Lead Optimization
1.7 Conclusions
Chapter 2: Computational Approaches to Drug Discovery and Development
2.1 Target Identification
2.2 Lead Discovery
2.3 ADME/T Optimization
2.4 The Future
Chapter 3: Design and Selection of Small Molecule Inhibitors
3.1 Virtual Screening in Selecting Small Molecule Inhibitors
3.2 Receptor-Based VLS
3.3 Ligand-Based Virtual Screening (2-D Similarity Search, 3-D Pharmacophore Search)
3.4 Design of Small Molecule Inhibitors
3.5 Scaffolds and Fragments-Based Lead Design
3.6 Hybrid Design Based on Known Inhibitors
3.7 De Novo Design
3.8 Hit and Lead Optimization
3.9 Structure Based
3.10 Qsar Based
3.11 Design of Selective Small Molecule Inhibitors
3.12 Targeting the Differences in the Binding Pocket
3.13 Engineering Selectivity Using Chemical Genetics
3.14 Summary
Chapter 4: Lead Optimization in Drug Discovery
4.1 Advances in High-Throughput Screening Technologies
4.2 Solution-Phase Parallel Synthesis for Lead Optimization
4.3 Expedited Drug Metabolism and Pharmacokinetics
4.4 Expedited, “Closed-Loop” Work Flow for Lead Optimization
Chapter 5: Pharmacokinetics of Drug Candidates
5.1 Clinical Pharmacokinetics
5.2 Role of PK in the Drug Discovery and Development Process
5.3 Summary
Chapter 6: ADME Properties of Drugs
6.1 Solubility
6.2 Permeability
6.3 Stability
6.4 Cytochrome P450 Inhibition
6.5 Other ADME/TOX Properties
Chapter 7: Drug Transport in Living Systems
7.1 Multidrug Transporters (MDTs)
7.2 Insights Into Structures of MDTs
7.3 Substrate Recognition: Multiple Drug Binding Proteins
7.4 Transport Mechanisms of MDTs
7.5 Physiologic Roles and Natural Substrates
Acknowledgment
Chapter 8: Blood-Brain Barrier: Considerations in Drug Development and Delivery
8.1 Cellular Physiology of the Blood-Brain Barrier
8.2 Drug Delivery to the Brain
8.3 Strategies to Improve CNS Drug Delivery
Acknowledgments
Chapter 9: Pharmacokinetic Considerations: Methods and Systems of Controlled Drug Delivery
9.1 General Introduction of Pharmacokinetics/ Pharmacodynamics
9.2 Pharmacokinetic/Pharmaceutical Dosage Form/Pharmacodynamic Considerations in the Design of A Controlled Drug Delivery System
9.3 Methods and Systems of Controlled Drug Delivery
9.4 Summary
Chapter 10: Pharmaceuticals: Natural Products and Natural Product Models
10.1 Introduction
10.2 Antibacterial Agents
10.3 Antifungal Agents
10.4 Antimalarials
10.5 Antivirals
10.6 Antipain Agents
10.7 Antiobesity
10.8 Alzheimer's Agents
10.9 Antineoplastic Agents
10.10 Immunosuppressant Agents
10.11 Cardiovascular Agents
10.12 Antiparasitic Agents
10.13 Pharmaceutical Models
Part II: Chemical Biology to Understand And Target Disease
Chapter 11: The Role of Chemical Biology in Understanding and Treating Disease—Are Small Molecule “Correctors” the Way of the Future?
11.1 The Potential for Small-Molecule Correctors
Chapter 12: Anxiety Disorders
12.1 Neuroticism and Anxiety
12.2 Genes, Their Protein Products, and Associated Biological Pathways Implicated in Anxiety and Anxiety-Like Behavior
12.3 Environmental Factors and Related Biological Pathways Involved in Anxiety
12.4 Interaction Between Genetic and Environmental Factors
12.5 Convergence of Anxiety-Related Pathways and Mechanisms
Chapter 13: Chronic Obstructive Pulmonary Disease (COPD)
13.1 COPD as an Inflammatory Disease
13.2 Inflammatory Cells
13.3 T-Lymphocytes
13.4 Mediators of Inflammation
13.5 Conclusions
Chapter 14: Depression
14.1 Introduction
14.2 Biogenic Amines
14.3 Classes of Antidepressants
14.4 Beyond Biogenic Amines
14.5 Other Antidepressant Approaches and Targets
14.6 Concluding Remarks
Acknowledgments
Chapter 15: Osteoarthritis
15.1 Biological and Biophysical Background of Osteoarthritis
15.2 Biochemistry and Molecular Mechanism Involved in Osteoarthritis
15.3 Tools and Methods for Studying Osteoarthritis
15.4 Therapeutic Management of Osteoarthritis
Chapter 16: Human Immunodeficiency Virus (HIV)
16.1 Introduction
16.2 The Mechanism of Viral Infection
16.3 Conclusion
Chapter 17: Allergy and Asthma
17.1 Biological Background
17.2 Small Molecules in Asthma
17.3 Targeting Inflammatory Cell Accumulation
17.4 Immunotherapy
Chapter 18: Schizophrenia
18.1 Neurobiology (Neurochemistry) of Schizophrenia
18.2 Antipsychotics
18.3 Behavioral Phenotype
18.4 Antipsychotics Clinical Efficacy Profile
18.5 Adverse Effects Associated with Antipsychotic Treatments
18.6 Cholinergic Drugs (Positive Modulators of Muscarinic Receptors)
18.7 Gulatamatergic Drugs in the Treatment of Schizophrenia
Chapter 19: Protein Misfolding and Disease
19.1 Introduction
19.2 Biological Background of Protein Misfolding Diseases
19.3 Biophysical Characterization of Fibrils and Molecular Mechanism of their Formation
19.4 Methods Used for Fibril Structure Determination and Aggregation Assays
Chapter 20: Protein Trafficking Diseases
20.1 Quality Control in the ER
20.2 Protein Trafficking Diseases
20.3 Correctors of Protein Trafficking
20.4 Conclusions
Acknowledgments
Chapter 21: Metabolic Diseases
21.1 The Global Crisis in Obesity, Diabetes, and CV Risk
21.2 Underlying Mechanisms that Lead to Insulin Resistance and CVD
21.3 Current and Next Generation Therapeutics
Chapter 22: Mitochondrial Medicine
22.1 Biological Background
22.2 The Chemistry of the OXPHOS System
22.3 Tools and Techniques to Study the OXPHOS System
22.4 Diagnostic Biochemical Analysis of the Mitochondrial Energy Generating System
Chapter 23: Lysosomal Disorders
23.1 Endosomes and Lysosomes
23.2 Components of Endosomes and Lysosomes
23.3 Targeting of Protein Constituents to Lysosomes
23.4 Interaction of Endosomes and Lysosomes and the Site of Substrate Hydrolysis
23.5 Commonalities for Lysosomal Storage Disorders in Terms of Clinical Phenotype and Vesicular Pathology
23.6 Primary and Secondary Storage Materials
23.7 Impact of Storage on Vesicular Structure and Traffic
23.8 Treatment Strategies and Ability to Correct Residual Pathology
Index
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