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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
Opac: Controlla la disponibilità qui
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
Opac: Controlla la disponibilità qui
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-9910840505403321
Hoboken, N.J., : Wiley-Interscience, c2008
Materiale a stampa
Lo trovi qui: Univ. Federico II
Opac: Controlla la disponibilità qui