Evaluation of enzyme inhibitors in drug discovery: a guide for medicinal chemists and pharmacologists
Gespeichert in:
| 1. Verfasser: | |
|---|---|
| Format: | Elektronisch E-Book |
| Sprache: | English |
| Veröffentlicht: |
Hoboken, N.J.
Wiley
c2013
|
| Ausgabe: | 2nd ed |
| Schlagworte: | |
| Online-Zugang: | FRO01 UBG01 Volltext |
| Beschreibung: | Irreversible Enzyme Inactivators.8.1 Kinetic Evaluation of Irreversible Enzyme Inactivators.8.2 Affinity Labels.8.2.1 Quiescent Affinity Labels.8.2.2 Potential Liabilities of Affinity Labels as Drugs.8.3 Mechanism-Based Inactivators.8.3.1 Distinguishing Features of Mechanism-Based Inactivation.8.3.2 Determination of the Partition Ratio.8.3.3 Potential Clinical Advantages of Mechanism-Based Inactivators.8.3.4 Examples of Mechanism-Based Inactivators as Drugs.8.4 Use of Affinity Labels as Mechanistic Tools.8.5 Summary.References.Appendix 1. Kinetic of Biochemical Reactions.A1.1 The Law of Mass Action and Reaction Order.A1.2 First-Order Reaction Kinetics.A1.3 Second-Order Reaction Kinetics.A1.4 Pseudo-First-Order Reaction Conditions.A1.5 Approach to Equilibrium: An Example of the Kinetics of Reversible Reactions.References.Appendix 2. Derivation of the Enzyme-Ligand Binding Isotherm Equation.References.Appendix 3. Serial Dilution Schemes.Index Includes bibliographical references and index "There has been explosive growth in the hunt for new pharmaceutically agents globally. Traditionally, this has been the purview of the pharmaceutical industry, but today, this effort crosses academic, government, and industry laboratories across the world. Enzymes remain the most valued and common of drug targets; hence, a detailed understanding of their interactions with inhibitors is critical to successful drug discovery. This book provides a practical, readable, and comprehensive treatment of these topics that allows scientists to master the art of applied enzymology for drug discovery. The book addresses the opportunities for inhibitor interactions with enzyme targets arising from consideration of the catalytic reaction mechanism; discusses how inhibitors are properly evaluated for potency, selectivity, and mode of action, covers the potential advantages and liabilities of specific inhibition modalities with respect to efficacy in vivo, and provides valuable biochemical insights to help medicinal chemists and pharmacologists most effectively pursue lead optimization. It includes two new chapters, one on the pioneering idea of drug-target residence time fostered by Dr. Copeland, and the second on quantitative biochemistry. Five new appendices are added"--Provided by publisher |
| Beschreibung: | 1 Online-Ressource |
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| 500 | |a Irreversible Enzyme Inactivators.8.1 Kinetic Evaluation of Irreversible Enzyme Inactivators.8.2 Affinity Labels.8.2.1 Quiescent Affinity Labels.8.2.2 Potential Liabilities of Affinity Labels as Drugs.8.3 Mechanism-Based Inactivators.8.3.1 Distinguishing Features of Mechanism-Based Inactivation.8.3.2 Determination of the Partition Ratio.8.3.3 Potential Clinical Advantages of Mechanism-Based Inactivators.8.3.4 Examples of Mechanism-Based Inactivators as Drugs.8.4 Use of Affinity Labels as Mechanistic Tools.8.5 Summary.References.Appendix 1. Kinetic of Biochemical Reactions.A1.1 The Law of Mass Action and Reaction Order.A1.2 First-Order Reaction Kinetics.A1.3 Second-Order Reaction Kinetics.A1.4 Pseudo-First-Order Reaction Conditions.A1.5 Approach to Equilibrium: An Example of the Kinetics of Reversible Reactions.References.Appendix 2. Derivation of the Enzyme-Ligand Binding Isotherm Equation.References.Appendix 3. Serial Dilution Schemes.Index | ||
| 500 | |a Includes bibliographical references and index | ||
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Datensatz im Suchindex
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| author | Copeland, Robert Allen |
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| dewey-hundreds | 600 - Technology (Applied sciences) |
| dewey-ones | 615 - Pharmacology and therapeutics |
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| dewey-search | 615/.19 |
| dewey-sort | 3615 219 |
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| spelling | Copeland, Robert Allen Verfasser aut Evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists by Robert A. Copeland 2nd ed Hoboken, N.J. Wiley c2013 1 Online-Ressource txt rdacontent c rdamedia cr rdacarrier Irreversible Enzyme Inactivators.8.1 Kinetic Evaluation of Irreversible Enzyme Inactivators.8.2 Affinity Labels.8.2.1 Quiescent Affinity Labels.8.2.2 Potential Liabilities of Affinity Labels as Drugs.8.3 Mechanism-Based Inactivators.8.3.1 Distinguishing Features of Mechanism-Based Inactivation.8.3.2 Determination of the Partition Ratio.8.3.3 Potential Clinical Advantages of Mechanism-Based Inactivators.8.3.4 Examples of Mechanism-Based Inactivators as Drugs.8.4 Use of Affinity Labels as Mechanistic Tools.8.5 Summary.References.Appendix 1. Kinetic of Biochemical Reactions.A1.1 The Law of Mass Action and Reaction Order.A1.2 First-Order Reaction Kinetics.A1.3 Second-Order Reaction Kinetics.A1.4 Pseudo-First-Order Reaction Conditions.A1.5 Approach to Equilibrium: An Example of the Kinetics of Reversible Reactions.References.Appendix 2. Derivation of the Enzyme-Ligand Binding Isotherm Equation.References.Appendix 3. Serial Dilution Schemes.Index Includes bibliographical references and index "There has been explosive growth in the hunt for new pharmaceutically agents globally. Traditionally, this has been the purview of the pharmaceutical industry, but today, this effort crosses academic, government, and industry laboratories across the world. Enzymes remain the most valued and common of drug targets; hence, a detailed understanding of their interactions with inhibitors is critical to successful drug discovery. This book provides a practical, readable, and comprehensive treatment of these topics that allows scientists to master the art of applied enzymology for drug discovery. The book addresses the opportunities for inhibitor interactions with enzyme targets arising from consideration of the catalytic reaction mechanism; discusses how inhibitors are properly evaluated for potency, selectivity, and mode of action, covers the potential advantages and liabilities of specific inhibition modalities with respect to efficacy in vivo, and provides valuable biochemical insights to help medicinal chemists and pharmacologists most effectively pursue lead optimization. It includes two new chapters, one on the pioneering idea of drug-target residence time fostered by Dr. Copeland, and the second on quantitative biochemistry. Five new appendices are added"--Provided by publisher Enzyme Inhibitors / therapeutic use Drug Design Enzyme Inhibitors / chemistry MEDICAL / Drug Guides bisacsh MEDICAL / Nursing / Pharmacology bisacsh MEDICAL / Pharmacology bisacsh MEDICAL / Pharmacy bisacsh Medizin Enzyme inhibitors / Therapeutic use / Testing Drugs / Design Enzyme inhibitors / Structure-activity relationships Arzneimittelentwicklung (DE-588)4143176-5 gnd rswk-swf Enzyminhibitor (DE-588)4152479-2 gnd rswk-swf Electronic books Enzyminhibitor (DE-588)4152479-2 s Arzneimittelentwicklung (DE-588)4143176-5 s 1\p DE-604 Erscheint auch als Druck-Ausgabe, Hardcover 978-1-118-48813-3 https://onlinelibrary.wiley.com/doi/book/10.1002/9781118540398 Verlag URL des Erstveröffentlichers Volltext 1\p cgwrk 20201028 DE-101 https://d-nb.info/provenance/plan#cgwrk |
| spellingShingle | Copeland, Robert Allen Evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists Enzyme Inhibitors / therapeutic use Drug Design Enzyme Inhibitors / chemistry MEDICAL / Drug Guides bisacsh MEDICAL / Nursing / Pharmacology bisacsh MEDICAL / Pharmacology bisacsh MEDICAL / Pharmacy bisacsh Medizin Enzyme inhibitors / Therapeutic use / Testing Drugs / Design Enzyme inhibitors / Structure-activity relationships Arzneimittelentwicklung (DE-588)4143176-5 gnd Enzyminhibitor (DE-588)4152479-2 gnd |
| subject_GND | (DE-588)4143176-5 (DE-588)4152479-2 |
| title | Evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists |
| title_auth | Evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists |
| title_exact_search | Evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists |
| title_full | Evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists by Robert A. Copeland |
| title_fullStr | Evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists by Robert A. Copeland |
| title_full_unstemmed | Evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists by Robert A. Copeland |
| title_short | Evaluation of enzyme inhibitors in drug discovery |
| title_sort | evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists |
| title_sub | a guide for medicinal chemists and pharmacologists |
| topic | Enzyme Inhibitors / therapeutic use Drug Design Enzyme Inhibitors / chemistry MEDICAL / Drug Guides bisacsh MEDICAL / Nursing / Pharmacology bisacsh MEDICAL / Pharmacology bisacsh MEDICAL / Pharmacy bisacsh Medizin Enzyme inhibitors / Therapeutic use / Testing Drugs / Design Enzyme inhibitors / Structure-activity relationships Arzneimittelentwicklung (DE-588)4143176-5 gnd Enzyminhibitor (DE-588)4152479-2 gnd |
| topic_facet | Enzyme Inhibitors / therapeutic use Drug Design Enzyme Inhibitors / chemistry MEDICAL / Drug Guides MEDICAL / Nursing / Pharmacology MEDICAL / Pharmacology MEDICAL / Pharmacy Medizin Enzyme inhibitors / Therapeutic use / Testing Drugs / Design Enzyme inhibitors / Structure-activity relationships Arzneimittelentwicklung Enzyminhibitor |
| url | https://onlinelibrary.wiley.com/doi/book/10.1002/9781118540398 |
| work_keys_str_mv | AT copelandrobertallen evaluationofenzymeinhibitorsindrugdiscoveryaguideformedicinalchemistsandpharmacologists |