| Description |
1 online resource |
| Contents |
880-01 Frontmatter -- Introduction -- Kinetics of Single-Substrate Enzymatic Reactions -- Kinetics of Single-Substrate Enzymatic Reactions: Special Topics -- Enzyme Inhibition: The Phenomenon and Mechanism-Independent Analysis -- Kinetic Mechanism of Inhibition of One-Substrate Enzymatic Reactions -- Tight-Binding, Slow-Binding, and Irreversible Inhibition -- Kinetics of Two-Substrate Enzymatic Reactions -- Kinetic Mechanism of Inhibition of Two-Substrate Enzymatic Reactions -- Allosteric Modulation of Enzyme Activity -- Kinetics-Based Probes of Mechanism -- Appendix A: Basic Principles of Chemical Kinetics -- Appendix B: Transition State Theory and Enzymology: Enzyme Catalytic Power and Inhibitor Design -- Appendix C: Selecting Substrate Concentrations for High-Throughput Screens -- Index |
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880-01/(S Machine generated contents note: 1. Introduction -- 1.1. Brief History of Enzymology -- 1.2. Goal of Enzymology: The Elucidation of Mechanism -- 1.3. Emergence of Mechanism from Data -- 2. Kinetics Of Single-Substrate Enzymatic Reactions -- 2.1. Dependence of Initial Velocity on Substrate Concentration and the Requirement for an E: S Complex -- 2.2. Derivation of the Rate Equation for a Single-Substrate Reaction with the Assumption of Rapid Equilibrium -- 2.3. Derivation of Rate Equations Using the Steady-State Assumption -- 2.4. Methods of Enzyme Assay -- 2.5. Enzyme Kinetics Practicum: Assay Development, Experimental Design, Data Collection, and Data Analysis -- 3. Kinetics Of Single-Substrate Enzymatic Reactions: Special Topics -- 3.1. Transition State Theory and Free Energy Diagrams -- 3.2. Kinetic Consequences of an Enzyme: Substrate Complex -- 3.3. Reactions with More Than One Intermediary Complex -- 3.4. Deviations from Michaelis-Menten Kinetics -- 3.5. Kinetics of Enzymatic Action on Substrates with Multiple Reactive Centers -- 4. Enzyme Inhibition: The Phenomenon And Mechanism-Independent Analysis -- 4.1. Enzyme Inhibition: The Phenomenon -- 4.2. Enzyme Inhibition: The First Quantitative Steps -- 4.3. Enzyme-Inhibitor Systems Misbehaving -- 4.4. Case Studies -- 5. Kinetic Mechanism Of Inhibition Of One-Substrate Enzymatic Reactions -- 5.1. Importance in Drug Discovery -- 5.2. Theoretical Considerations -- 5.3. Analysis of Initial Velocity Data for Enzyme Inhibition -- 5.4. Inhibition of One-Substrate, Two-Intermediate Reactions -- 5.5. Inhibition by Depletion of Substrate -- 6. Tight-Binding, Slow-Binding, And Irreversible Inhibition -- 6.1. Importance in Drug Discovery -- 6.2. Tight-Binding Inhibition -- 6.3. Slow-Binding Inhibition -- 6.4. Irreversible Inhibition -- 7. Kinetics Of Two-Substrate Enzymatic Reactions -- 7.1. Importance in Drug Discovery -- 7.2. Basic Mechanisms -- 7.3. Conceptual Understanding of Sequential Mechanisms -- 7.4. Derivation of Rate Equations for Sequential Mechanisms -- 7.5. Ping-Pong Mechanisms -- 7.6. Determining the Kinetic Mechanism for Two-Substrate Reactions -- 7.7. Conceptual Understanding of the Shapes of Secondary Plots -- 7.8. Mistaken Identity: Rapid Equilibrium Random Versus Steady-State Ordered -- 8. Kinetic Mechanism Of Inhibition Of Two-Substrate Enzymatic Reactions -- 8.1. Importance in Drug Discovery -- 8.2. Mechanisms of Inhibition of Two-Substrate Reactions -- 8.3. Inhibition by Substrate Analogs -- 8.4. Analysis of Sequential Reactions in which Inhibitor Binds to Enzyme: Product Complexes -- 8.5. Driving SAR Programs for Two-Substrate Enzymatic Reactions -- 9. Allosteric Modulation Of Enzyme Activity -- 9.1. Mechanisms of Enzyme Modulation -- 9.2. Kinetics of Allosteric Modulation -- 9.3. Meaning of β and υ -- 9.4. Case Studies: Dependence of Allosteric Modulation on Structural Features of the Substrate -- 10. Kinetics-Based Probes Of Mechanism -- 10.1. pH Dependence of Enzymatic Reactions -- 10.2. Temperature Dependence of Enzymatic Reactions -- 10.3. Viscosity Dependence of Enzymatic Reactions -- 10.4. Kinetic Isotope Effects on Enzyme-Catalyzed Reactions -- APPENDIX A BASIC PRINCIPLES OF CHEMICAL KINETICS -- A.1. One-Step, Irreversible, Unimolecular Reactions -- A.2. One-Step, Irreversible, Bimolecular Reactions -- A.3. One-Step, Reversible Reactions -- A.4. Two-Step, Irreversible Reactions -- A.5. Two-Step Reaction, with Reversible First Step -- APPENDIX B TRANSITION STATE THEORY AND ENZYMOLOGY: ENZYME CATALYTIC POWER AND INHIBITOR DESIGN -- B.1. Catalytic Power of Enzymes -- B.2. Transition State Analog Inhibition -- APPENDIX C SELECTING SUBSTRATE CONCENTRATIONS FOR HIGH-THROUGHPUT SCREENS -- C.1. Balancing the Steady State for One-Substrate Reactions -- C.2. Balancing the Steady State for Two-Substrate, Rapid Equilibrium-Ordered Enzymatic Reactions -- C.3. Balancing the Steady State for Two-Substrate, Rapid Equilibrium Random Enzymatic Reactions -- C.4. Balancing the Steady State for Nonequilibrium Enzymatic Reactions Involving a Second Steady-State Intermediate -- C.5. Balancing the Steady State for Two-Substrate, Ping-Pong Enzymatic Reactions |
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Kinetics of single-substrate enzymatic reactions -- Kinetics of single-substrate enzymatic reactions : special topics -- Enzyme inhibition : the phenomenon and mechanistic analysis -- Kinetic mechanism of inhibition of one-substrate enzymatic reactions -- Tight-binding, slow-binding, and irreversible inhibitors -- Kinetics of two-substrate enzymatic reactions -- Kinetic mechanism of inhibition of two-substrate enzymatic reactions -- Allosteric modulation of enzyme-catalyzed reactions -- Kinetics-based probes of enzyme mechanisms |
| Summary |
"Few scientists have the knowledge to perform the studies that are necessary to discover and characterize enzyme inhibitors, despite the vested interest the pharmaceutical industry has in this field. Beginning with the most basic principles pertaining to simple, one-substrate enzyme reactions and their inhibitors, and progressing to a thorough treatment of two-substrate enzymes, Kinetics of Enzyme Action: Essential Principles for Drug Hunters provides biochemists, medicinal chemists, and pharmaceutical scientists with numerous case study examples to outline the tools and techniques necessary to perform, understand, and interpret detailed kinetic studies for drug discovery"--Provided by publisher |
| Bibliography |
Includes bibliographical references and index |
| Notes |
Print version record |
| Subject |
Enzymes -- Pharmacokinetics
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Enzyme inhibitors -- Pharmacokinetics
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Enzyme activation.
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Enzymes -- pharmacokinetics
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Drug Discovery
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Enzyme Activation
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Enzyme Inhibitors -- pharmacokinetics
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SCIENCE -- Life Sciences -- Biochemistry.
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Enzyme activation
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| Form |
Electronic book
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| ISBN |
9781118084410 |
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1118084411 |
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9781118084397 |
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111808439X |
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9780470414118 |
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0470414111 |
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1283176211 |
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9781283176217 |
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1118084403 |
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9781118084403 |
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