Drug metabolism in drug design and development [[electronic resource] ] : basic concepts and practice / / edited by Donglu Zhang, Mingshe Zhu, W. Griffith Humphreys |
Pubbl/distr/stampa | Hoboken, N.J., : Wiley-Interscience, c2008 |
Descrizione fisica | 1 online resource (633 p.) |
Disciplina |
615.7
615/.7 |
Altri autori (Persone) |
ZhangDonglu
ZhuMingshe HumphreysW. Griffith |
Soggetto topico |
Drugs - Metabolism
Drugs - Design Drug development |
ISBN |
1-281-09423-4
9786611094232 0-470-19169-4 0-470-19168-6 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto |
DRUG METABOLISM IN DRUG DESIGN AND DEVELOPMENT; CONTENTS; Preface; Contributors; PART I BASIC CONCEPTS OF DRUG METABOLISM; 1 Overview: Drug Metabolism in the Modern Pharmaceutical Industry; 1.1 Introduction; 1.2 Technology; 1.3 Breadth of Science; 1.3.1 Chemistry; 1.3.2 Enzymology and Molecular Biology; 1.4 Impact of Drug Metabolism on Efficacy and Safety; 1.4.1 Efficacy; 1.4.2 Safety; 1.5 Regulatory Impact and IP Position; 1.6 Summary; References; 2 Oxidative, Reductive, and Hydrolytic Metabolism of Drugs; 2.1 Introduction; 2.2 Nomenclature and Terminology
2.3 General Features of the Enzymes2.4 Fractional Contributions of Different Enzymes; 2.5 Oxidation Enzymes; 2.5.1 Cytochrome P450 (P450, CYP); 2.5.2 Flavin-Containing Monooxygenase (FMO); 2.5.3 Monoamine Oxidase (MAO); 2.5.4 Aldehyde Oxidase and Xanthine Dehydrogenase; 2.5.5 Peroxidases; 2.5.6 Alcohol Dehydrogenases (ADH); 2.5.7 Aldehyde Dehydrogenases (ALDH); 2.6 Reduction; 2.6.1 P450, ADH; 2.6.2 NADPH-P450 Reductase; 2.6.3 Aldo-Keto Reductases (AKR); 2.6.4 Quinone Reductase (NQO); 2.6.5 Glutathione Peroxidase (GPX); 2.7 Hydrolysis; 2.7.1 Epoxide Hydrolase; 2.7.2 Esterases and Amidases 2.8 SummaryReferences; 3 Conjugative Metabolism of Drugs; 3.1 UDP-Glucuronosyltransferases; 3.1.1 Location Within the Cell; 3.1.2 Endogenous Substrates; 3.1.3 Enzyme Multiplicity; 3.1.4 Inducibility; 3.1.5 Pharmacogenetics; 3.1.6 Experimental Considerations; 3.1.7 Enzyme Selective Substrates and Inhibitors; 3.1.8 Drug-Drug Interactions and Glucuronidation; 3.1.9 Summary; 3.2 Cytosolic Sulfotransferases; 3.2.1 Cellular Location and Tissue Expression; 3.2.2 The SULT Superfamily of Cytosolic Enzymes; 3.2.3 Inducibility; 3.2.4 SULT Pharmacogenetics 3.2.5 Analytical Detection of Sulfonated Metabolites3.2.6 SULT Inhibitors (Pacifici and Coughtrie, 2005); 3.2.7 Drug-Drug Interactions and Sulfonation; 3.2.8 Summary; 3.3 Glutathione-S-Transferases; 3.3.1 General Overview; 3.3.2 Classification of the GST Enzymes; 3.3.3 Localization and Expression; 3.3.4 Reactions Catalyzed by GSTs; 3.3.5 Regulation of GSTs; 3.3.6 GST Alpha Class; 3.3.7 GST Mu Class; 3.3.8 GST Pi Class; 3.3.9 GST Theta Class; 3.3.10 GST Zeta Class; 3.3.11 Incubation Conditions and Analytical Methods; 3.3.12 Glutathione Conjugate Metabolism (Mercapturic Acid Pathway) References4 Enzyme Kinetics; 4.1 Introduction; 4.2 Enzyme Catalysis; 4.3 Michaelis-Menten Kinetics; 4.3.1 Meanings of K(m), V(max) and Their Clinical Relevance; 4.4 Graphical Kinetic Plots; 4.5 Atypical Kinetics-Allosteric Effects; 4.5.1 Overview of Atypical Kinetic Phenomena; 4.5.2 Homotropic Cooperativity; 4.5.3 Heterotropic Cooperativity; 4.6 Graphical Analysis of Atypical Kinetic Data; 4.7 Enzyme Inhibition Kinetics; 4.7.1 Overview; 4.7.2 Competitive Inhibition; 4.7.3 Mixed Inhibition; 4.7.4 Noncompetitive Inhibition; 4.7.5 Uncompetitive Inhibition 4.7.6 Summary of Effects of Various Inhibition Types of Kinetic Parameters |
Record Nr. | UNINA-9910143981703321 |
Hoboken, N.J., : Wiley-Interscience, c2008 | ||
![]() | ||
Lo trovi qui: Univ. Federico II | ||
|
Drug metabolism in drug design and development [[electronic resource] ] : basic concepts and practice / / edited by Donglu Zhang, Mingshe Zhu, W. Griffith Humphreys |
Pubbl/distr/stampa | Hoboken, N.J., : Wiley-Interscience, c2008 |
Descrizione fisica | 1 online resource (633 p.) |
Disciplina |
615.7
615/.7 |
Altri autori (Persone) |
ZhangDonglu
ZhuMingshe HumphreysW. Griffith |
Soggetto topico |
Drugs - Metabolism
Drugs - Design Drug development |
ISBN |
1-281-09423-4
9786611094232 0-470-19169-4 0-470-19168-6 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto |
DRUG METABOLISM IN DRUG DESIGN AND DEVELOPMENT; CONTENTS; Preface; Contributors; PART I BASIC CONCEPTS OF DRUG METABOLISM; 1 Overview: Drug Metabolism in the Modern Pharmaceutical Industry; 1.1 Introduction; 1.2 Technology; 1.3 Breadth of Science; 1.3.1 Chemistry; 1.3.2 Enzymology and Molecular Biology; 1.4 Impact of Drug Metabolism on Efficacy and Safety; 1.4.1 Efficacy; 1.4.2 Safety; 1.5 Regulatory Impact and IP Position; 1.6 Summary; References; 2 Oxidative, Reductive, and Hydrolytic Metabolism of Drugs; 2.1 Introduction; 2.2 Nomenclature and Terminology
2.3 General Features of the Enzymes2.4 Fractional Contributions of Different Enzymes; 2.5 Oxidation Enzymes; 2.5.1 Cytochrome P450 (P450, CYP); 2.5.2 Flavin-Containing Monooxygenase (FMO); 2.5.3 Monoamine Oxidase (MAO); 2.5.4 Aldehyde Oxidase and Xanthine Dehydrogenase; 2.5.5 Peroxidases; 2.5.6 Alcohol Dehydrogenases (ADH); 2.5.7 Aldehyde Dehydrogenases (ALDH); 2.6 Reduction; 2.6.1 P450, ADH; 2.6.2 NADPH-P450 Reductase; 2.6.3 Aldo-Keto Reductases (AKR); 2.6.4 Quinone Reductase (NQO); 2.6.5 Glutathione Peroxidase (GPX); 2.7 Hydrolysis; 2.7.1 Epoxide Hydrolase; 2.7.2 Esterases and Amidases 2.8 SummaryReferences; 3 Conjugative Metabolism of Drugs; 3.1 UDP-Glucuronosyltransferases; 3.1.1 Location Within the Cell; 3.1.2 Endogenous Substrates; 3.1.3 Enzyme Multiplicity; 3.1.4 Inducibility; 3.1.5 Pharmacogenetics; 3.1.6 Experimental Considerations; 3.1.7 Enzyme Selective Substrates and Inhibitors; 3.1.8 Drug-Drug Interactions and Glucuronidation; 3.1.9 Summary; 3.2 Cytosolic Sulfotransferases; 3.2.1 Cellular Location and Tissue Expression; 3.2.2 The SULT Superfamily of Cytosolic Enzymes; 3.2.3 Inducibility; 3.2.4 SULT Pharmacogenetics 3.2.5 Analytical Detection of Sulfonated Metabolites3.2.6 SULT Inhibitors (Pacifici and Coughtrie, 2005); 3.2.7 Drug-Drug Interactions and Sulfonation; 3.2.8 Summary; 3.3 Glutathione-S-Transferases; 3.3.1 General Overview; 3.3.2 Classification of the GST Enzymes; 3.3.3 Localization and Expression; 3.3.4 Reactions Catalyzed by GSTs; 3.3.5 Regulation of GSTs; 3.3.6 GST Alpha Class; 3.3.7 GST Mu Class; 3.3.8 GST Pi Class; 3.3.9 GST Theta Class; 3.3.10 GST Zeta Class; 3.3.11 Incubation Conditions and Analytical Methods; 3.3.12 Glutathione Conjugate Metabolism (Mercapturic Acid Pathway) References4 Enzyme Kinetics; 4.1 Introduction; 4.2 Enzyme Catalysis; 4.3 Michaelis-Menten Kinetics; 4.3.1 Meanings of K(m), V(max) and Their Clinical Relevance; 4.4 Graphical Kinetic Plots; 4.5 Atypical Kinetics-Allosteric Effects; 4.5.1 Overview of Atypical Kinetic Phenomena; 4.5.2 Homotropic Cooperativity; 4.5.3 Heterotropic Cooperativity; 4.6 Graphical Analysis of Atypical Kinetic Data; 4.7 Enzyme Inhibition Kinetics; 4.7.1 Overview; 4.7.2 Competitive Inhibition; 4.7.3 Mixed Inhibition; 4.7.4 Noncompetitive Inhibition; 4.7.5 Uncompetitive Inhibition 4.7.6 Summary of Effects of Various Inhibition Types of Kinetic Parameters |
Record Nr. | UNINA-9910830456403321 |
Hoboken, N.J., : Wiley-Interscience, c2008 | ||
![]() | ||
Lo trovi qui: Univ. Federico II | ||
|
Drug metabolism in drug design and development [[electronic resource] ] : basic concepts and practice / / edited by Donglu Zhang, Mingshe Zhu, W. Griffith Humphreys |
Pubbl/distr/stampa | Hoboken, N.J., : Wiley-Interscience, c2008 |
Descrizione fisica | 1 online resource (633 p.) |
Disciplina |
615.7
615/.7 |
Altri autori (Persone) |
ZhangDonglu
ZhuMingshe HumphreysW. Griffith |
Soggetto topico |
Drugs - Metabolism
Drugs - Design Drug development |
ISBN |
1-281-09423-4
9786611094232 0-470-19169-4 0-470-19168-6 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto |
DRUG METABOLISM IN DRUG DESIGN AND DEVELOPMENT; CONTENTS; Preface; Contributors; PART I BASIC CONCEPTS OF DRUG METABOLISM; 1 Overview: Drug Metabolism in the Modern Pharmaceutical Industry; 1.1 Introduction; 1.2 Technology; 1.3 Breadth of Science; 1.3.1 Chemistry; 1.3.2 Enzymology and Molecular Biology; 1.4 Impact of Drug Metabolism on Efficacy and Safety; 1.4.1 Efficacy; 1.4.2 Safety; 1.5 Regulatory Impact and IP Position; 1.6 Summary; References; 2 Oxidative, Reductive, and Hydrolytic Metabolism of Drugs; 2.1 Introduction; 2.2 Nomenclature and Terminology
2.3 General Features of the Enzymes2.4 Fractional Contributions of Different Enzymes; 2.5 Oxidation Enzymes; 2.5.1 Cytochrome P450 (P450, CYP); 2.5.2 Flavin-Containing Monooxygenase (FMO); 2.5.3 Monoamine Oxidase (MAO); 2.5.4 Aldehyde Oxidase and Xanthine Dehydrogenase; 2.5.5 Peroxidases; 2.5.6 Alcohol Dehydrogenases (ADH); 2.5.7 Aldehyde Dehydrogenases (ALDH); 2.6 Reduction; 2.6.1 P450, ADH; 2.6.2 NADPH-P450 Reductase; 2.6.3 Aldo-Keto Reductases (AKR); 2.6.4 Quinone Reductase (NQO); 2.6.5 Glutathione Peroxidase (GPX); 2.7 Hydrolysis; 2.7.1 Epoxide Hydrolase; 2.7.2 Esterases and Amidases 2.8 SummaryReferences; 3 Conjugative Metabolism of Drugs; 3.1 UDP-Glucuronosyltransferases; 3.1.1 Location Within the Cell; 3.1.2 Endogenous Substrates; 3.1.3 Enzyme Multiplicity; 3.1.4 Inducibility; 3.1.5 Pharmacogenetics; 3.1.6 Experimental Considerations; 3.1.7 Enzyme Selective Substrates and Inhibitors; 3.1.8 Drug-Drug Interactions and Glucuronidation; 3.1.9 Summary; 3.2 Cytosolic Sulfotransferases; 3.2.1 Cellular Location and Tissue Expression; 3.2.2 The SULT Superfamily of Cytosolic Enzymes; 3.2.3 Inducibility; 3.2.4 SULT Pharmacogenetics 3.2.5 Analytical Detection of Sulfonated Metabolites3.2.6 SULT Inhibitors (Pacifici and Coughtrie, 2005); 3.2.7 Drug-Drug Interactions and Sulfonation; 3.2.8 Summary; 3.3 Glutathione-S-Transferases; 3.3.1 General Overview; 3.3.2 Classification of the GST Enzymes; 3.3.3 Localization and Expression; 3.3.4 Reactions Catalyzed by GSTs; 3.3.5 Regulation of GSTs; 3.3.6 GST Alpha Class; 3.3.7 GST Mu Class; 3.3.8 GST Pi Class; 3.3.9 GST Theta Class; 3.3.10 GST Zeta Class; 3.3.11 Incubation Conditions and Analytical Methods; 3.3.12 Glutathione Conjugate Metabolism (Mercapturic Acid Pathway) References4 Enzyme Kinetics; 4.1 Introduction; 4.2 Enzyme Catalysis; 4.3 Michaelis-Menten Kinetics; 4.3.1 Meanings of K(m), V(max) and Their Clinical Relevance; 4.4 Graphical Kinetic Plots; 4.5 Atypical Kinetics-Allosteric Effects; 4.5.1 Overview of Atypical Kinetic Phenomena; 4.5.2 Homotropic Cooperativity; 4.5.3 Heterotropic Cooperativity; 4.6 Graphical Analysis of Atypical Kinetic Data; 4.7 Enzyme Inhibition Kinetics; 4.7.1 Overview; 4.7.2 Competitive Inhibition; 4.7.3 Mixed Inhibition; 4.7.4 Noncompetitive Inhibition; 4.7.5 Uncompetitive Inhibition 4.7.6 Summary of Effects of Various Inhibition Types of Kinetic Parameters |
Record Nr. | UNINA-9910840505403321 |
Hoboken, N.J., : Wiley-Interscience, c2008 | ||
![]() | ||
Lo trovi qui: Univ. Federico II | ||
|
Mass spectrometry in drug metabolism and disposition [[electronic resource] ] : basic principles and applications / / edited by Mike S. Lee, Mingshe Zhu |
Pubbl/distr/stampa | Hoboken, N.J., : John Wiley & Sons, c2011 |
Descrizione fisica | 1 online resource (776 p.) |
Disciplina | 615/.7 |
Altri autori (Persone) |
LeeMike S. <1960->
ZhuMingshe |
Collana | Wiley series on pharmaceutical science and biotechnology: practices, applications and methods |
Soggetto topico |
Drugs - Metabolism - Analysis
Metabolites - Spectra Mass spectrometry |
ISBN |
0-470-93469-7
1-283-05232-6 9786613052322 0-470-92926-X 0-470-92927-8 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto | (Publisher-supplied data) Part I Basic Concepts of Drug Metabolism and Disposition -- The Progression of Drug Metabolism -- Common Biotransformation Reactions -- Metabolic Activation of Organic Functional Groups Utilized in Medicinal Chemistry -- Drug Metabolizing Enzymes, Transporters and Drug-Drug Interactions -- Experimental Models of Drug Metabolism and Disposition -- Principles of Pharmacokinetics: Predicting Human Pharmacokinetics -- Drug Metabolism Research as an Integral Part of the Drug Discovery and Development Processes -- Part II Mass Spectrometry in Drug Metabolism: Principles and Common Practice -- Theory and Instrumentation of Mass Spectrometry -- Common Liquid Chromatography-Mass Spectrometry (LC-MS) Methodology for Metabolite Identification -- Mass Spectral Interpretation -- Techniques to Facilitate the Performance of Mass Spectrometry: Sample Preparation, Liquid Chromatography and Non-Mass Spectrometric Detection -- Part III Applications of New LC/MS Techniques in Drug Metabolism and Disposition -- Quantitative In Vitro ADME Assays using LC-MS as a Part of Early Drug Metabolism Screening -- High Resolution Mass Spectrometry and Drug Metabolite Identification -- Distribution Studies of Drugs and Metabolites in Tissue by Mass Spectrometric Imaging -- Use of Triple Quadrupole-Linear Ion Trap Mass Spectrometry as a Single LC/MS Platform in Drug Metabolism and Pharmacokinetics Studies -- Quantitative Drug Metabolism with Accelerator Mass Spectrometry -- Standard-Free Estimation of Metabolite Levels Using Nanospray Mass Spectrometry: Current Statutes and Future Directions -- Profiling and Characterization of Herbal Medicine and their Metabolites using LC-MS -- Liquid Chromatography Mass Spectrometry Bioanalysis of Proteins in Biological Matrices -- Mass Spectrometry in the Analysis of DNA, Protein, Peptide, and Lipid Biomarkers of Oxidative Stress -- LC-MS in Endogenous Metabolite Profiling and Small Molecule Biomarker Discovery. |
Record Nr. | UNINA-9910133582603321 |
Hoboken, N.J., : John Wiley & Sons, c2011 | ||
![]() | ||
Lo trovi qui: Univ. Federico II | ||
|
Mass spectrometry in drug metabolism and disposition [[electronic resource] ] : basic principles and applications / / edited by Mike S. Lee, Mingshe Zhu |
Pubbl/distr/stampa | Hoboken, N.J., : John Wiley & Sons, c2011 |
Descrizione fisica | 1 online resource (776 p.) |
Disciplina | 615/.7 |
Altri autori (Persone) |
LeeMike S. <1960->
ZhuMingshe |
Collana | Wiley series on pharmaceutical science and biotechnology: practices, applications and methods |
Soggetto topico |
Drugs - Metabolism - Analysis
Metabolites - Spectra Mass spectrometry |
ISBN |
0-470-93469-7
1-283-05232-6 9786613052322 0-470-92926-X 0-470-92927-8 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto | (Publisher-supplied data) Part I Basic Concepts of Drug Metabolism and Disposition -- The Progression of Drug Metabolism -- Common Biotransformation Reactions -- Metabolic Activation of Organic Functional Groups Utilized in Medicinal Chemistry -- Drug Metabolizing Enzymes, Transporters and Drug-Drug Interactions -- Experimental Models of Drug Metabolism and Disposition -- Principles of Pharmacokinetics: Predicting Human Pharmacokinetics -- Drug Metabolism Research as an Integral Part of the Drug Discovery and Development Processes -- Part II Mass Spectrometry in Drug Metabolism: Principles and Common Practice -- Theory and Instrumentation of Mass Spectrometry -- Common Liquid Chromatography-Mass Spectrometry (LC-MS) Methodology for Metabolite Identification -- Mass Spectral Interpretation -- Techniques to Facilitate the Performance of Mass Spectrometry: Sample Preparation, Liquid Chromatography and Non-Mass Spectrometric Detection -- Part III Applications of New LC/MS Techniques in Drug Metabolism and Disposition -- Quantitative In Vitro ADME Assays using LC-MS as a Part of Early Drug Metabolism Screening -- High Resolution Mass Spectrometry and Drug Metabolite Identification -- Distribution Studies of Drugs and Metabolites in Tissue by Mass Spectrometric Imaging -- Use of Triple Quadrupole-Linear Ion Trap Mass Spectrometry as a Single LC/MS Platform in Drug Metabolism and Pharmacokinetics Studies -- Quantitative Drug Metabolism with Accelerator Mass Spectrometry -- Standard-Free Estimation of Metabolite Levels Using Nanospray Mass Spectrometry: Current Statutes and Future Directions -- Profiling and Characterization of Herbal Medicine and their Metabolites using LC-MS -- Liquid Chromatography Mass Spectrometry Bioanalysis of Proteins in Biological Matrices -- Mass Spectrometry in the Analysis of DNA, Protein, Peptide, and Lipid Biomarkers of Oxidative Stress -- LC-MS in Endogenous Metabolite Profiling and Small Molecule Biomarker Discovery. |
Record Nr. | UNINA-9910816941903321 |
Hoboken, N.J., : John Wiley & Sons, c2011 | ||
![]() | ||
Lo trovi qui: Univ. Federico II | ||
|