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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…mehr
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- Produktdetails
- Verlag: John Wiley & Sons
- Seitenzahl: 320
- Erscheinungstermin: 18. Mai 2011
- Englisch
- ISBN-13: 9781118084397
- Artikelnr.: 37353788
- Verlag: John Wiley & Sons
- Seitenzahl: 320
- Erscheinungstermin: 18. Mai 2011
- Englisch
- ISBN-13: 9781118084397
- Artikelnr.: 37353788
Enzymology: The Elucidation of Mechanism 11 1.3 The Emergence of Mechanism
from Data 13 2 KINETICS OF SINGLE-SUBSTRATE ENZYMATIC REACTIONS 19 2.1 The
Dependence of Initial Velocity on Substrate Concentration and the
Requirement for an E: S Complex 19 2.2 Derivation of the Rate Equation for
a Single-Substrate Reaction with the Assumption of Rapid Equilibrium 21 2.3
Derivation of Rate Equations Using the Steady-State Assumption 24 2.4
Methods of Enzyme Assay 26 2.5 Enzyme Kinetics Practicum: Assay
Development, Experimental Design, Data Collection, and Data Analysis 32 3
KINETICS OF SINGLE-SUBSTRATE ENZYMATIC REACTIONS: SPECIAL TOPICS 41 3.1
Transition State Theory and Free Energy Diagrams 41 3.2 Kinetic
Consequences of an Enzyme: Substrate Complex 46 3.3 Reactions with More
Than One Intermediary Complex 51 3.4 Deviations from Michaelis-Menten
Kinetics 53 3.5 Kinetics of Enzymatic Action on Substrates with Multiple
Reactive Centers 65 4 ENZYME INHIBITION: THE PHENOMENON AND
MECHANISM-INDEPENDENT ANALYSIS 73 4.1 Enzyme Inhibition: The Phenomenon 74
4.2 Enzyme Inhibition: The First Quantitative Steps 76 4.3 Enzyme-Inhibitor
Systems Misbehaving 77 4.4 Case Studies 83 5 KINETIC MECHANISM OF
INHIBITION OF ONE-SUBSTRATE ENZYMATIC REACTIONS 89 5.1 Importance in Drug
Discovery 89 5.2 Theoretical Considerations 90 5.3 Analysis of Initial
Velocity Data for Enzyme Inhibition 96 5.4 Inhibition of One-Substrate,
Two-Intermediate Reactions 108 5.5 Inhibition by Depletion of Substrate 111
6 TIGHT-BINDING, SLOW-BINDING, AND IRREVERSIBLE INHIBITION 115 6.1
Importance in Drug Discovery 115 6.2 Tight-Binding Inhibition 116 6.3
Slow-Binding Inhibition 122 6.4 Irreversible Inhibition 137 7 KINETICS OF
TWO-SUBSTRATE ENZYMATIC REACTIONS 141 7.1 Importance in Drug Discovery 141
7.2 Basic Mechanisms 142 7.3 Conceptual Understanding of Sequential
Mechanisms 143 7.4 Derivation of Rate Equations for Sequential Mechanisms
147 7.5 Ping-Pong Mechanisms 153 7.6 Determining the Kinetic Mechanism for
Two-Substrate Reactions 156 7.7 A Conceptual Understanding of the Shapes of
Secondary Plots 163 7.8 Mistaken Identity: Rapid Equilibrium Random Versus
Steady-State Ordered 168 8 KINETIC MECHANISM OF INHIBITION OF TWO-SUBSTRATE
ENZYMATIC REACTIONS 169 8.1 Importance in Drug Discovery 170 8.2 Mechanisms
of Inhibition of Two-Substrate Reactions 170 8.3 Inhibition by Substrate
Analogs 185 8.4 Analysis of Sequential Reactions in which Inhibitor Binds
to Enzyme: Product Complexes 191 8.5 Driving SAR Programs for Two-Substrate
Enzymatic Reactions 196 9 ALLOSTERIC MODULATION OF ENZYME ACTIVITY 199 9.1
Mechanisms of Enzyme Modulation 201 9.2 Kinetics of Allosteric Modulation
202 9.3 Meaning of ² and ³ 208 9.4 Case Studies: Dependence of Allosteric
Modulation on Structural Features of the Substrate 212 10 KINETICS-BASED
PROBES OF MECHANISM 219 10.1 pH Dependence of Enzymatic Reactions 220 10.2
Temperature Dependence of Enzymatic Reactions 229 10.3 Viscosity Dependence
of Enzymatic Reactions 235 10.4 Kinetic Isotope Effects on Enzyme-Catalyzed
Reactions 239 APPENDIX A BASIC PRINCIPLES OF CHEMICAL KINETICS 251 A.1
One-Step, Irreversible, Unimolecular Reactions 252 A.2 One-Step,
Irreversible, Bimolecular Reactions 253 A.3 One-Step, Reversible Reactions
254 A.4 Two-Step, Irreversible Reactions 257 A.5 Two-Step Reaction, with
Reversible First Step 259 APPENDIX B TRANSITION STATE THEORY AND
ENZYMOLOGY: ENZYME CATALYTIC POWER AND INHIBITOR DESIGN 263 B.1 Catalytic
Power of Enzymes 263 B.2 Transition State Analog Inhibition 268 APPENDIX C
SELECTING SUBSTRATE CONCENTRATIONS FOR HIGH-THROUGHPUT SCREENS 275 C.1
Balancing the Steady State for One-Substrate Reactions 276 C.2 Balancing
the Steady State for Two-Substrate, Rapid Equilibrium-Ordered Enzymatic
Reactions 276 C.3 Balancing the Steady State for Two-Substrate, Rapid
Equilibrium Random Enzymatic Reactions 279 C.4 Balancing the Steady State
for Nonequilibrium Enzymatic Reactions Involving a Second Steady-State
Intermediate 282 C.5 Balancing the Steady State for Two-Substrate,
Ping-Pong Enzymatic Reactions 283 Index 287
Enzymology: The Elucidation of Mechanism 11 1.3 The Emergence of Mechanism
from Data 13 2 KINETICS OF SINGLE-SUBSTRATE ENZYMATIC REACTIONS 19 2.1 The
Dependence of Initial Velocity on Substrate Concentration and the
Requirement for an E: S Complex 19 2.2 Derivation of the Rate Equation for
a Single-Substrate Reaction with the Assumption of Rapid Equilibrium 21 2.3
Derivation of Rate Equations Using the Steady-State Assumption 24 2.4
Methods of Enzyme Assay 26 2.5 Enzyme Kinetics Practicum: Assay
Development, Experimental Design, Data Collection, and Data Analysis 32 3
KINETICS OF SINGLE-SUBSTRATE ENZYMATIC REACTIONS: SPECIAL TOPICS 41 3.1
Transition State Theory and Free Energy Diagrams 41 3.2 Kinetic
Consequences of an Enzyme: Substrate Complex 46 3.3 Reactions with More
Than One Intermediary Complex 51 3.4 Deviations from Michaelis-Menten
Kinetics 53 3.5 Kinetics of Enzymatic Action on Substrates with Multiple
Reactive Centers 65 4 ENZYME INHIBITION: THE PHENOMENON AND
MECHANISM-INDEPENDENT ANALYSIS 73 4.1 Enzyme Inhibition: The Phenomenon 74
4.2 Enzyme Inhibition: The First Quantitative Steps 76 4.3 Enzyme-Inhibitor
Systems Misbehaving 77 4.4 Case Studies 83 5 KINETIC MECHANISM OF
INHIBITION OF ONE-SUBSTRATE ENZYMATIC REACTIONS 89 5.1 Importance in Drug
Discovery 89 5.2 Theoretical Considerations 90 5.3 Analysis of Initial
Velocity Data for Enzyme Inhibition 96 5.4 Inhibition of One-Substrate,
Two-Intermediate Reactions 108 5.5 Inhibition by Depletion of Substrate 111
6 TIGHT-BINDING, SLOW-BINDING, AND IRREVERSIBLE INHIBITION 115 6.1
Importance in Drug Discovery 115 6.2 Tight-Binding Inhibition 116 6.3
Slow-Binding Inhibition 122 6.4 Irreversible Inhibition 137 7 KINETICS OF
TWO-SUBSTRATE ENZYMATIC REACTIONS 141 7.1 Importance in Drug Discovery 141
7.2 Basic Mechanisms 142 7.3 Conceptual Understanding of Sequential
Mechanisms 143 7.4 Derivation of Rate Equations for Sequential Mechanisms
147 7.5 Ping-Pong Mechanisms 153 7.6 Determining the Kinetic Mechanism for
Two-Substrate Reactions 156 7.7 A Conceptual Understanding of the Shapes of
Secondary Plots 163 7.8 Mistaken Identity: Rapid Equilibrium Random Versus
Steady-State Ordered 168 8 KINETIC MECHANISM OF INHIBITION OF TWO-SUBSTRATE
ENZYMATIC REACTIONS 169 8.1 Importance in Drug Discovery 170 8.2 Mechanisms
of Inhibition of Two-Substrate Reactions 170 8.3 Inhibition by Substrate
Analogs 185 8.4 Analysis of Sequential Reactions in which Inhibitor Binds
to Enzyme: Product Complexes 191 8.5 Driving SAR Programs for Two-Substrate
Enzymatic Reactions 196 9 ALLOSTERIC MODULATION OF ENZYME ACTIVITY 199 9.1
Mechanisms of Enzyme Modulation 201 9.2 Kinetics of Allosteric Modulation
202 9.3 Meaning of ² and ³ 208 9.4 Case Studies: Dependence of Allosteric
Modulation on Structural Features of the Substrate 212 10 KINETICS-BASED
PROBES OF MECHANISM 219 10.1 pH Dependence of Enzymatic Reactions 220 10.2
Temperature Dependence of Enzymatic Reactions 229 10.3 Viscosity Dependence
of Enzymatic Reactions 235 10.4 Kinetic Isotope Effects on Enzyme-Catalyzed
Reactions 239 APPENDIX A BASIC PRINCIPLES OF CHEMICAL KINETICS 251 A.1
One-Step, Irreversible, Unimolecular Reactions 252 A.2 One-Step,
Irreversible, Bimolecular Reactions 253 A.3 One-Step, Reversible Reactions
254 A.4 Two-Step, Irreversible Reactions 257 A.5 Two-Step Reaction, with
Reversible First Step 259 APPENDIX B TRANSITION STATE THEORY AND
ENZYMOLOGY: ENZYME CATALYTIC POWER AND INHIBITOR DESIGN 263 B.1 Catalytic
Power of Enzymes 263 B.2 Transition State Analog Inhibition 268 APPENDIX C
SELECTING SUBSTRATE CONCENTRATIONS FOR HIGH-THROUGHPUT SCREENS 275 C.1
Balancing the Steady State for One-Substrate Reactions 276 C.2 Balancing
the Steady State for Two-Substrate, Rapid Equilibrium-Ordered Enzymatic
Reactions 276 C.3 Balancing the Steady State for Two-Substrate, Rapid
Equilibrium Random Enzymatic Reactions 279 C.4 Balancing the Steady State
for Nonequilibrium Enzymatic Reactions Involving a Second Steady-State
Intermediate 282 C.5 Balancing the Steady State for Two-Substrate,
Ping-Pong Enzymatic Reactions 283 Index 287