Drug Metabolism Handbook 2nd Edition by Ala F Nassar, Paul F Hollenberg, Joann Scatina, Soumen Kanti Manna, Su Zeng – Ebook PDF Instant Download/Delivery: 1119851017 ,9781119851011
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ISBN 10: 1119851017
ISBN 13: 9781119851011
Author: Ala F Nassar, Paul F Hollenberg, Joann Scatina, Soumen Kanti Manna, Su Zeng
A comprehensive explanation of drug metabolism concepts and applications in drug development and cancer treatment
In the newly revised second edition of Drug Metabolism Handbook: Concepts and Applications in Cancer Research, a distinguished team of researchers delivers an incisive and robust exploration of the drug metabolism system and a well-illustrated and detailed explanation of the latest tools and techniques used in the research, pharmacology, and medicine. The book discusses the creation of new molecular entities, drug development, troubleshooting, and other highly relevant concepts, guiding readers through new applications in pharmaceutical research, development, and assessment.
The latest edition offers updated content on metabolism basics and the application of a variety of new techniques to cancer treatment, including mass spectrometry, imaging, metabolomics, and immunotherapy. It also offers in-depth case studies highlighting the role of metabolism in drug development.
Readers will also benefit from:
- A thorough introduction to drug metabolism, including a historical perspective, factors affecting metabolism, and biotransformations in drug metabolism
- Comprehensive discussions of technologies for in vitro and in vivo studies, including mass spectrometry and accelerating metabolite identification with mass spectrometry
- In-depth explorations of drug interactions, including discussions of enzyme inhibition and the characterization of cytochrome P450 mechanism-based inhibition
- Fulsome treatments of drug toxicity, including the role of drug metabolism in toxicity, and allergic reactions to drugs
Perfect for medicinal chemists, pharmaceutical scientists, and toxicologists, Drug Metabolism Handbook: Concepts and Applications in Cancer Research, Second Edition will also earn a place in the libraries of analytical chemists and drug discovery professionals.
Drug Metabolism Handbook 2nd Edition Table of contents:
VOLUME 1
PART I: INTRODUCTION
CHAPTER 1: Historical Perspective
1.1 CONTROVERSIES SPANNING PAST, PRESENT, AND FUTURE
1.2 1800S: DISCOVERY OF MAJOR DRUG METABOLISM PATHWAYS (CONTI AND BICKEL, 1977)
1.3 1900–1950S: CONFIRMATION OF MAJOR PATHWAYS AND MECHANISTIC STUDIES
1.4 1950S–1980: MODERN DRUG METABOLISM EMERGES, WITH ENZYMATIC BASIS
1.5 1980–2005: FIELD DRIVEN BY IMPROVED TECHNOLOGIES
1.6 2005+: HIGH TECHNOLOGY
REFERENCES
CHAPTER 2: Factors Affecting Metabolism
REFERENCES
CHAPTER 3: Biotransformations in Drug Metabolism
3.1 DRUG METABOLISM IN DRUG DEVELOPMENT AND DRUG THERAPY
3.2 PREDICTION OF METABOLITE AND ENZYME RESPONSIBLE
3.3 FUNCTIONAL GROUP BIOTRANSFORMATIONS: PHASE I, PHASE II, AND CATALYSIS
3.4 OXIDATIONS AND CYTOCHROME P450
3.5 ENZYMOLOGY AND MODIFIERS OF CYTOCHROME P450S
REFERENCES
CHAPTER 4: A Comprehensive Picture of Biotransformation in Drug Discovery
4.1 INTRODUCTION
4.2 RATE OF METABOLISM
4.3 METABOLISM OF SMALL MOLECULES
4.4 ANALYTICAL TECHNOLOGIES IN DRUG METABOLISM
4.5 BIOTRANSFORMATION FOR NOVEL MODALITIES – PEPTIDES AND PROTEIN DEGRADERS
4.6 CONCLUSION
REFERENCES
CHAPTER 5: In Vivo Drug Metabolite Kinetics
5.1 INTRODUCTION
5.2 IN VIVO DRUG METABOLITE KINETIC CONCEPTS AND PRINCIPLES
5.3 EFFECT OF INHIBITION AND INDUCTION ON METABOLITE KINETICS
5.4 DETERMINATION OF FORMATION AND ELIMINATION CLEARANCE OF METABOLITE
5.5 INCORPORATION OF PHARMACOLOGICALLY ACTIVE METABOLITE(S) IN PHARMACOKINETIC/PHARMACODYNAMIC MODELING
5.6 SUMMARY
ABBREVIATIONS
REFERENCES
CHAPTER 6: LC-MS/MS-Based Proteomics Methods for Quantifying Drug-Metabolizing Enzymes and Transporters
6.1 INTRODUCTION
6.2 MASS SPECTROMETRY VERSUS ALTERNATIVE PROTEIN QUANTIFICATION METHODS
6.3 MASS SPECTROMETRY DATA ACQUISITION METHODS FOR PROTEOMICS ANALYSIS
6.4 TARGETED APPROACHES
6.5 UNTARGETED PROTEOMICS APPROACHES
6.6 RELATIVE QUANTIFICATION VERSUS ABSOLUTE QUANTIFICATION
6.7 LABEL-BASED PROTEOMICS
6.8 LABEL-FREE PROTEOMICS
6.9 DMET PROTEIN QUANTIFICATION USING LC-MS/MS-BASED PROTEOMICS
6.10 POTENTIAL APPLICATION OF DMET EXPRESSION STUDIES
6.11 CONSIDERATIONS OF DMET PROTEIN QUANTIFICATION UTILIZING LC-MS/MS METHODS
6.12 CONCLUSION
REFERENCES
PART II: TECHNOLOGIES FOR IN VITRO AND IN VIVO STUDIES
CHAPTER 7: Mass Spectrometry
7.1 INTRODUCTION
7.2 A BRIEF HISTORY
7.3 THE MASS SPECTROMETRY LITERATURE
7.4 MASS SPECTROMETRY INSTRUMENTATION
7.5 INTERPRETATION: WHAT DOES IT MEAN
7.6 CONCLUSIONS
REFERENCES
NOTES
CHAPTER 8: Accelerating Metabolite Identification Mass Spectrometry Technology Drives Metabolite Identification Studies Forward
8.1 INTRODUCTION
8.2 CRITERIA FOR LC-MS METHODS
8.3 MATRICES EFFECT
8.4 TOOL OF CHOICE FOR METABOLITE CHARACTERIZATION
8.5 STRATEGIES FOR IDENTIFYING UNKNOWN METABOLITES
8.6 ONLINE HD-LC-MS
8.7 “ALL-IN-ONE” RADIOACTIVITY DETECTOR, STOP FLOW, AND DYNAMIC FLOW FOR METABOLITE IDENTIFICATION
8.8 METABOLIC ACTIVATION STUDIES BY MASS SPECTROMETRY
8.9 STRATEGIES TO SCREEN FOR REACTIVE METABOLITES
8.10 SUMMARY
ABBREVIATIONS AND GLOSSARY
REFERENCES
CHAPTER 9: Role of Structural Modifications of Drug Candidates to Enhance Metabolic Stability
9.1 BACKGROUND
9.2 INTRODUCTION
9.3 SIGNIFICANCE OF METABOLITE CHARACTERIZATION AND STRUCTURE MODIFICATION
9.4 ENHANCE METABOLIC STABILITY
9.5 METABOLIC STABILITY AND INTRINSIC METABOLIC CLEARANCE
9.6 ADVANTAGES OF ENHANCING METABOLIC STABILITY
9.7 STRATEGIES TO ENHANCE METABOLIC STABILITY
9.8 ANALYTICAL TOOLS
9.9 CASE STUDIES
9.10 CONCLUSIONS
REFERENCES
CHAPTER 10: Drug Design Strategies: Role of Structural Modifications of Drug Candidates to Improve PK Parameters of New Drugs
10.1 ACTIVE METABOLITES
10.2 ORAL ABSORPTION AND INTRAVENOUS DOSE
10.3 PK ANALYSIS
10.4 CASE STUDIES
10.5 PRODRUGS TO INCREASE WATER SOLUBILITY
10.6 CONCLUSION
REFERENCES
CHAPTER 11: Chemical Structural Alert and Reactive Metabolite Concept as Applied in Medicinal Chemistry to Minimize the Toxicity of Drug Candidates
11.1 IMPORTANCE OF REACTIVE INTERMEDIATES IN DRUG DISCOVERY AND DEVELOPMENT
11.2 IDIOSYNCRATIC DRUG TOXICITY AND MOLECULAR MECHANISMS
11.3 KEY TOOLS AND STRATEGIES TO IMPROVE DRUG SAFETY
11.4 PEROXIDASES
11.5 ACYL GLUCURONIDATION AND S-Acyl-CoA Thioesters
11.6 COVALENT BINDING
11.7 MECHANISTIC STUDIES
11.8 PRECLINICAL DEVELOPMENT
11.9 CLINICAL DEVELOPMENT: STRATEGY
11.10 CASE STUDIES
11.11 CONCLUSION AND FUTURE POSSIBILITIES
REFERENCES
CHAPTER 12: Studies of Reactive Metabolites using Genotoxicity Arrays and Enzyme/DNA Biocolloids – 2021
12.1 INTRODUCTION
12.2 ON DEMAND METABOLIC REACTIONS
12.3 ARRAYS WITH ELECTROCHEMICAL DETECTION
12.4 ELECTROCHEMILUMINESCENT ARRAYS
12.5 ECL ARRAYS CAN MEASURE BOTH DNA OXIDATION AND NUCLEOBASE ADDUCTION
12.6 DETECTING SITE-SPECIFIC DAMAGE TO TUMOR SUPPRESSOR GENES
12.7 EMERGING TECHNOLOGIES AND METHODS
12.8 CONCLUSIONS AND FUTURE OUTLOOK
ACKNOWLEDGMENTS
BIOGRAPHIES
REFERENCES
PART III: DRUG INTERACTIONS
CHAPTER 13: Enzyme Inhibition
13.1 INTRODUCTION
13.2 MECHANISMS OF ENZYME INHIBITION
13.3 COMPETITIVE INHIBITION
13.4 NONCOMPETITIVE INHIBITION
13.5 UNCOMPETITIVE INHIBITION
13.6 PRODUCT INHIBITION
13.7 TRANSITION-STATE ANALOGS
13.8 SLOW, TIGHT-BINDING INHIBITORS
13.9 MECHANISM-BASED INACTIVATORS
13.10 INHIBITORS THAT ARE METABOLIZED TO REACTIVE PRODUCTS THAT COVALENTLY ATTACH TO THE ENZYME
13.11 SUBSTRATE INHIBITION
13.12 PARTIAL INHIBITION
13.13 INHIBITION OF CYTOCHROME P450 ENZYMES
13.14 REVERSIBLE INHIBITORS
13.15 QUASI-IRREVERSIBLE INHIBITORS
13.16 MECHANISM-BASED INACTIVATORS
REFERENCES
CHAPTER 14: Xenobiotic Receptor-Mediated Gene Regulation in Drug Metabolism and Disposition
14.1 INTRODUCTION
14.2 PREGNANE X RECEPTOR
14.3 CONSTITUTIVE ANDROSTANE/ACTIVATED RECEPTOR (CAR)
14.4 CLOSING REMARKS AND PERSPECTIVES
ACKNOWLEDGMENTS
REFERENCES
CHAPTER 15: Characterization of Cytochrome P450 Mechanism Based Inhibition
15.1 INTRODUCTION
15.2 INHIBITORS THAT UPON ACTIVATION BIND COVALENTLY TO THE P450 APOPROTEIN
15.3 INHIBITORS THAT INTERACT IN A PSEUDOIRREVERSIBLE MANNER WITH HEME IRON
15.4 INACTIVATION THAT CAUSE DESTRUCTION OF THE PROSTHETIC HEME GROUP, OFTEN TIMES LEADING TO HEME-DERIVED PRODUCTS THAT COVALENTLY MODIFY THE APOPROTEIN
REFERENCES
CHAPTER 16: An Introduction to Metabolic Reaction-Phenotyping
16.1 INTRODUCTION
16.2 SIGNIFICANT DRUG-METABOLIZING ENZYMES
16.3 COMMON IN VITRO METHODS TO ASSESS DRUG METABOLISM
16.4 IN VITRO TO IN VIVO EXTRAPOLATION OF METABOLIC CLEARANCE
16.5 SUMMARY
REFERENCES
CHAPTER 17: Epigenetic Regulation of Drug-Metabolizing Enzymes in Cancer
17.1 INTRODUCTION
17.2 DNA METHYLATION OF DME
17.3 HISTONE MODIFICATION
17.4 NONCODING RNA
17.5 RNA METHYLATION
17.6 CLOSING REMARKS AND PERSPECTIVES
ACKNOWLEDGMENTS
REFERENCES
CHAPTER 18: Epigenetic Regulation of Drug Transporters in Cancer
18.1 INTRODUCTION
18.2 DNA METHYLATION
18.3 HISTONE MODIFICATIONS
18.4 NONCODING RNA
18.5 Closing Remarks and Perspectives
ACKNOWLEDGMENTS
REFERENCES
VOLUME 2
PART IV: TOXICITY
CHAPTER 19: The Role of Drug Metabolism in Toxicity
19.1 INTRODUCTION
19.2 DRUG METABOLIZING ENZYMES
19.3 CLASSIFICATION OF TOXICITY
19.4 MOLECULAR MECHANISMS OF TOXICITY
19.5 ORGAN SYSTEMS TOXICOLOGY
19.6 CARCINOGENESIS
19.7 TERATOGENESIS
19.8 ABROGATION/MITIGATION OF BIOACTIVATION – CASE EXAMPLES
19.9 EXPERIMENTAL METHODS FOR SCREENING
19.10 SUMMARY
ACKNOWLEDGMENT
References
CHAPTER 20: Allergic Reactions to Drugs
20.1 INTRODUCTION
20.2 IMMUNE SYSTEM: A BRIEF OVERVIEW
20.3 DRUG METABOLISM AND THE HAPTEN HYPOTHESIS
20.4 ALLERGIC REACTIONS TO DRUGS (EXAMPLES)
20.5 CONCLUSION
ACKNOWLEDGMENTS
REFERENCES
NOTE
CHAPTER 21: Chemical Mechanisms in Toxicology
21.1 INTRODUCTION
21.2 GLUTATHIONE ADDUCTS
21.3 COVALENT BINDING
21.4 STRUCTURAL ALERTS
21.5 EXAMPLES OF METABOLIC ACTIVATION
21.6 CONCLUSION
ACKNOWLEDGMENTS
REFERENCES
NOTE
CHAPTER 22: Role of Bioactivation Reactions in Chemically Induced Nephrotoxicity
22.1 TOXICOLOGICAL IMPLICATIONS OF RENAL STRUCTURE AND FUNCTION
22.2 INTERORGAN AND INTRARENAL BIOACTIVATION PATHWAYS
22.3 CYTOCHROME P450 (CYP)-DEPENDENT BIOACTIVATION IN THE RENAL PROXIMAL TUBULE
22.4 FLAVIN-CONTAINING MONOOXYGENASE (FMO)-DEPENDENT BIOACTIVATION IN THE RENAL PROXIMAL TUBULE
22.5 GLUTATHIONE (GSH)-DEPENDENT BIOACTIVATION IN THE RENAL PROXIMAL TUBULE
22.6 RENAL METABOLISM OF ACETAMINOPHEN (PARACETAMOL) BY THE KIDNEYS
22.7 IMPACT OF CHRONIC KIDNEY DISEASE ON DRUG METABOLISM
22.8 SUMMARY AND CONCLUSION
REFERENCES
PART V: APPLICATIONS
CHAPTER 23: Mapping the Heterogeneous Distribution of Cancer Drugs by Imaging Mass Spectrometry
23.1 INTRODUCTION
23.2 MSI INSTRUMENTATION
23.3 IMAGE ANALYSIS
23.4 SAMPLE PREPARATION
23.5 QUANTITATIVE MSI
23.6 MSI IN STUDYING THE DISTRIBUTION OF CANCER DRUGS
23.7 EMERGING IN VITRO APPLICATIONS
23.8 CLINICAL TRANSLATION
23.9 CONCLUSION AND PERSPECTIVES
REFERENCES
CHAPTER 24: Systemic Metabolomic Changes Associated with Chemotherapy: Role in Personalized Therapy
24.1 INTRODUCTION
24.2 METABOLOMICS: MAPPING METABOLOMIC ALTERATIONS IN CANCER
24.3 ANALYTICAL METHODS IN CANCER METABOLOMICS: GLOBAL AND TARGETED STRATEGIES
24.4 METABOLOMICS IN CANCER: EXPLORATION OF METABOLIC ALTERATIONS DURING DISEASE DEVELOPMENT, CHEMOTHERAPY AND DRUG RESISTANCE
24.5 CHALLENGES AND PROGRESS IN THE APPLICATION OF METABOLOMICS FOR THE DEVELOPMENT OF PERSONALIZED CANCER MEDICINE
24.6 FUTURE PERSPECTIVES AND FURTHER SCOPE OF IMPROVEMENT IN METABOLOMICS-ASSISTED CANCER THERAPY
24.7 CONCLUDING REMARKS
REFERENCES
CHAPTER 25: Metabolic Reprogramming in Cancer
25.1 INTRODUCTION
25.2 REPROGRAMMING OF CENTRAL CARBON METABOLISM (CCM)
25.3 GLUTAMINE ADDICTION OF CANCER CELLS
25.4 ARGININE AND POLYAMINE METABOLISM
25.5 SERINE, METHIONINE AND ONE CARBON METABOLISM
25.6 BRANCHED-CHAIN AMINO ACID (BCAA) METABOLISM
25.7 REPROGRAMMING OF OXIDATIVE STRESS RESPONSE MACHINERY
25.8 BIOSYNTHESIS OF PURINE AND PYRIMIDINE NUCLEOTIDES IN CANCER
25.9 REPROGRAMMING OF LIPID METABOLISM IN CANCER
25.10 METABOLIC REWIRING IN CANCER STEM CELLS (CSC)
25.11 FUTURE PERSPECTIVES
REFERENCES
CHAPTER 26: Case Study: Metabolism and Reactions of Alkylating Agents in Cancer Therapy
26.1 INTRODUCTION
26.2 IN VITRO STUDIES
26.3 NOVEL REARRANGEMENT
26.4 IDENTIFICATION AND CHARACTERIZATION OF IN VITRO METABOLITE/DECOMPOSITION PRODUCTS OF LAROMUSTINE IN HLM
26.5 IDENTIFICATION AND CHARACTERIZATION OF IN VITRO CONJUGATION REACTIONS OF LAROMUSTINE
26.6 DISCUSSION
REFERENCES
CHAPTER 27: Rewiring of Drug Metabolism and Its Cross-talk with Metabolic Reprogramming in Cancer
27.1 INTRODUCTION
27.2 PATHWAYS INVOLVED IN ANTICANCER DRUG METABOLISM
27.3 ALTERATIONS IN DRUG METABOLISM IN CANCER
27.4 REWIRING OF DRUG METABOLISM IN RESPONSE TO ANTICANCER AGENTS
27.5 CROSS-TALK BETWEEN ENDOGENOUS AND DRUG METABOLISM IN CANCER
27.6 ROLE OF MICROENVIRONMENT IN DRUG METABOLISM
27.7 FUTURE PERSPECTIVES
ACKNOWLEDGMENT
REFERENCES
CHAPTER 28: Principles of Drug Metabolism and Interactions in Cardio-Oncology
28.1 INTRODUCTION
28.2 EXPRESSION OF CYP450 IN CANCER
28.3 EXPRESSION OF P-GLYCOPROTEIN IN CANCER
28.4 INTERACTIONS BETWEEN DRUG CLASSES IN CARDIO-ONCOLOGY BY CYP450 OR P-G
28.5 IMPACT OF GENOMIC VARIATION AND OTHER FORMS OF REGULATION
28.6 MULTIDISCIPLINARY TEAM APPROACH
28.7 CONCLUSION
REFERENCES
INDEX
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Tags: Ala F Nassar, Paul F Hollenberg, Joann Scatina, Soumen Kanti Manna, Su Zeng, Drug Metabolism