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ADME-enabling technologies for drug design and development [[electronic resource] /] / edited by Donglu Zhang, Sekhar Surapaneni
| ADME-enabling technologies for drug design and development [[electronic resource] /] / edited by Donglu Zhang, Sekhar Surapaneni |
| Pubbl/distr/stampa | Hoboken, N.J., : Wiley, c2012 |
| Descrizione fisica | 1 online resource (623 p.) |
| Disciplina | 615.1/9 |
| Altri autori (Persone) |
ZhangDonglu
SurapaneniSekhar |
| Soggetto topico |
Drugs - Design
Drug development Drugs - Metabolism Pharmaceutical chemistry Pharmacokinetics Pharmaceutical technology |
| ISBN |
1-280-59257-5
9786613622402 1-118-18076-3 1-118-18077-1 1-118-18074-7 |
| Formato | Materiale a stampa  |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
ADME-Enabling Technologies in Drug Design and Development; CONTENTS; FOREWORD; PREFACE; CONTRIBUTORS; PART A: ADME: OVERVIEW AND CURRENT TOPICS; 1: REGULATORY DRUG DISPOSITION AND NDA PACKAGE INCLUDING MIST; 1.1 INTRODUCTION; 1.2 NONCLINICAL OVERVIEW; 1.3 PK; 1.4 ABSORPTION; 1.5 DISTRIBUTION; 1.5.1 Plasma Protein Binding; 1.5.2 Tissue Distribution; 1.5.3 Lacteal and Placental Distribution Studies; 1.6 METABOLISM; 1.6.1 In vitro Metabolism Studies; 1.6.2 Drug-Drug Interaction Studies; 1.6.3 In vivo Metabolism (ADME) Studies; 1.7 EXCRETION; 1.8 IMPACT OF METABOLISM INFORMATION ON LABELING
1.9 CONCLUSIONSREFERENCES; 2: OPTIMAL ADME PROPERTIES FOR CLINICAL CANDIDATE AND INVESTIGATIONAL NEW DRUG (IND) PACKAGE; 2.1 INTRODUCTION; 2.2 NCE AND INVESTIGATIONAL NEW DRUG (IND) PACKAGE; 2.3 ADME OPTIMIZATION; 2.3.1 Absorption; 2.3.2 Metabolism; 2.3.3 PK; 2.4 ADME OPTIMIZATION FOR CNS DRUGS; 2.5 SUMMARY; REFERENCES; 3: DRUG TRANSPORTERS IN DRUG INTERACTIONS AND DISPOSITION; 3.1 INTRODUCTION; 3.2 ABC TRANSPORTERS; 3.2.1 Pgp (MDR1, ABCB1); 3.2.2 BCRP (ABCG2); 3.2.3 MRP2 (ABCC2); 3.3 SLC TRANSPORTERS; 3.3.1 OCT1 (SLC22A1) and OCT2 (SLC22A2); 3.3.2 MATE1 (SLC47A1) and MATE2K (SLC47A2) 3.3.3 OAT1 (SLC22A6) and OAT3 (SLC22A8)3.3.4 OATP1B1 (SLCO1B1, SLC21A6), OATP1B3 (SLCO1B3, SLC21A8), and OATP2B1 (SLCO2B1, SLC21A9); 3.4 IN VITRO ASSAYS IN DRUG DEVELOPMENT; 3.4.1 Considerations for Assessing Candidate Drugs as Inhibitors; 3.4.2 Considerations for Assessing Candidate Drugs as Substrates; 3.4.3 Assay Systems; 3.5 CONCLUSIONS AND PERSPECTIVES; REFERENCES; 4: PHARMACOLOGICAL AND TOXICOLOGICAL ACTIVITY OF DRUG METABOLITES; 4.1 INTRODUCTION; 4.2 ASSESSMENT OF POTENTIAL FOR ACTIVE METABOLITES; 4.2.1 Detection of Active Metabolites during Drug Discovery 4.2.2 Methods for Assessing and Evaluating the Biological Activity of Metabolite Mixtures4.2.3 Methods for Generation of Metabolites; 4.3 ASSESSMENT OF THE POTENTIAL TOXICOLOGY OF METABOLITES; 4.3.1 Methods to Study the Formation of Reactive Metabolites; 4.3.2 Reactive Metabolite Studies: In vitro; 4.3.3 Reactive Metabolite Studies: In vivo; 4.3.4 Reactive Metabolite Data Interpretation; 4.3.5 Metabolite Contribution to Off-Target Toxicities; 4.4 SAFETY TESTING OF DRUG METABOLITES; 4.5 SUMMARY; REFERENCES 5: IMPROVING THE PHARMACEUTICAL PROPERTIES OF BIOLOGICS IN DRUG DISCOVERY: UNIQUE CHALLENGES AND ENABLING SOLUTIONS5.1 INTRODUCTION; 5.2 PHARMACOKINETICS; 5.3 METABOLISM AND DISPOSITION; 5.4 IMMUNOGENICITY; 5.5 TOXICITY AND PRECLINICAL ASSESSMENT; 5.6 COMPARABILITY; 5.7 CONCLUSIONS; REFERENCES; 6: CLINICAL DOSE ESTIMATION USING PHARMACOKINETIC/PHARMACODYNAMIC MODELING AND SIMULATION; 6.1 INTRODUCTION; 6.2 BIOMARKERS IN PK AND PD; 6.2.1 PK; 6.2.2 PD; 6.2.3 Biomarkers; 6.3 MODEL-BASED CLINICAL DRUG DEVELOPMENT; 6.3.1 Modeling; 6.3.2 Simulation; 6.3.3 Population Modeling 6.3.4 Quantitative Pharmacology (QP) and Pharmacometrics |
| Record Nr. | UNINA-9910141254203321 |
| Hoboken, N.J., : Wiley, c2012 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
ADME-enabling technologies for drug design and development / / edited by Donglu Zhang, Sekhar Surapaneni
| ADME-enabling technologies for drug design and development / / edited by Donglu Zhang, Sekhar Surapaneni |
| Edizione | [1st ed.] |
| Pubbl/distr/stampa | Hoboken, N.J., : Wiley, c2012 |
| Descrizione fisica | 1 online resource (623 p.) |
| Disciplina | 615.1/9 |
| Altri autori (Persone) |
ZhangDonglu
SurapaneniSekhar |
| Soggetto topico |
Drugs - Design
Drug development Drugs - Metabolism Pharmaceutical chemistry Pharmacokinetics Pharmaceutical technology |
| ISBN |
1-280-59257-5
9786613622402 1-118-18076-3 1-118-18077-1 1-118-18074-7 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
ADME-Enabling Technologies in Drug Design and Development; CONTENTS; FOREWORD; PREFACE; CONTRIBUTORS; PART A: ADME: OVERVIEW AND CURRENT TOPICS; 1: REGULATORY DRUG DISPOSITION AND NDA PACKAGE INCLUDING MIST; 1.1 INTRODUCTION; 1.2 NONCLINICAL OVERVIEW; 1.3 PK; 1.4 ABSORPTION; 1.5 DISTRIBUTION; 1.5.1 Plasma Protein Binding; 1.5.2 Tissue Distribution; 1.5.3 Lacteal and Placental Distribution Studies; 1.6 METABOLISM; 1.6.1 In vitro Metabolism Studies; 1.6.2 Drug-Drug Interaction Studies; 1.6.3 In vivo Metabolism (ADME) Studies; 1.7 EXCRETION; 1.8 IMPACT OF METABOLISM INFORMATION ON LABELING
1.9 CONCLUSIONSREFERENCES; 2: OPTIMAL ADME PROPERTIES FOR CLINICAL CANDIDATE AND INVESTIGATIONAL NEW DRUG (IND) PACKAGE; 2.1 INTRODUCTION; 2.2 NCE AND INVESTIGATIONAL NEW DRUG (IND) PACKAGE; 2.3 ADME OPTIMIZATION; 2.3.1 Absorption; 2.3.2 Metabolism; 2.3.3 PK; 2.4 ADME OPTIMIZATION FOR CNS DRUGS; 2.5 SUMMARY; REFERENCES; 3: DRUG TRANSPORTERS IN DRUG INTERACTIONS AND DISPOSITION; 3.1 INTRODUCTION; 3.2 ABC TRANSPORTERS; 3.2.1 Pgp (MDR1, ABCB1); 3.2.2 BCRP (ABCG2); 3.2.3 MRP2 (ABCC2); 3.3 SLC TRANSPORTERS; 3.3.1 OCT1 (SLC22A1) and OCT2 (SLC22A2); 3.3.2 MATE1 (SLC47A1) and MATE2K (SLC47A2) 3.3.3 OAT1 (SLC22A6) and OAT3 (SLC22A8)3.3.4 OATP1B1 (SLCO1B1, SLC21A6), OATP1B3 (SLCO1B3, SLC21A8), and OATP2B1 (SLCO2B1, SLC21A9); 3.4 IN VITRO ASSAYS IN DRUG DEVELOPMENT; 3.4.1 Considerations for Assessing Candidate Drugs as Inhibitors; 3.4.2 Considerations for Assessing Candidate Drugs as Substrates; 3.4.3 Assay Systems; 3.5 CONCLUSIONS AND PERSPECTIVES; REFERENCES; 4: PHARMACOLOGICAL AND TOXICOLOGICAL ACTIVITY OF DRUG METABOLITES; 4.1 INTRODUCTION; 4.2 ASSESSMENT OF POTENTIAL FOR ACTIVE METABOLITES; 4.2.1 Detection of Active Metabolites during Drug Discovery 4.2.2 Methods for Assessing and Evaluating the Biological Activity of Metabolite Mixtures4.2.3 Methods for Generation of Metabolites; 4.3 ASSESSMENT OF THE POTENTIAL TOXICOLOGY OF METABOLITES; 4.3.1 Methods to Study the Formation of Reactive Metabolites; 4.3.2 Reactive Metabolite Studies: In vitro; 4.3.3 Reactive Metabolite Studies: In vivo; 4.3.4 Reactive Metabolite Data Interpretation; 4.3.5 Metabolite Contribution to Off-Target Toxicities; 4.4 SAFETY TESTING OF DRUG METABOLITES; 4.5 SUMMARY; REFERENCES 5: IMPROVING THE PHARMACEUTICAL PROPERTIES OF BIOLOGICS IN DRUG DISCOVERY: UNIQUE CHALLENGES AND ENABLING SOLUTIONS5.1 INTRODUCTION; 5.2 PHARMACOKINETICS; 5.3 METABOLISM AND DISPOSITION; 5.4 IMMUNOGENICITY; 5.5 TOXICITY AND PRECLINICAL ASSESSMENT; 5.6 COMPARABILITY; 5.7 CONCLUSIONS; REFERENCES; 6: CLINICAL DOSE ESTIMATION USING PHARMACOKINETIC/PHARMACODYNAMIC MODELING AND SIMULATION; 6.1 INTRODUCTION; 6.2 BIOMARKERS IN PK AND PD; 6.2.1 PK; 6.2.2 PD; 6.2.3 Biomarkers; 6.3 MODEL-BASED CLINICAL DRUG DEVELOPMENT; 6.3.1 Modeling; 6.3.2 Simulation; 6.3.3 Population Modeling 6.3.4 Quantitative Pharmacology (QP) and Pharmacometrics |
| Record Nr. | UNINA-9910816078003321 |
| Hoboken, N.J., : Wiley, c2012 | ||
| Materiale a stampa | ||
| 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
| 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 | ||
| Materiale a stampa | ||
| 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
| 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 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Drug metabolism in drug design and development : basic concepts and practice / / edited by Donglu Zhang, Mingshe Zhu, W. Griffith Humphreys
| Drug metabolism in drug design and development : 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 |
| 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-9910877198703321 |
| Hoboken, N.J., : Wiley-Interscience, c2008 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||