Kinetics of enzyme action: essential principles for drug hunters
Gespeichert in:
| 1. Verfasser: | |
|---|---|
| Format: | Buch |
| Sprache: | English |
| Veröffentlicht: |
Hoboken, NJ
Wiley
2011
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| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis |
| Beschreibung: | XII, 302 S. graph. Darst. |
| ISBN: | 9780470414118 |
Internformat
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Datensatz im Suchindex
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|---|---|
| adam_text | Titel: Kinetics of enzyme action
Autor: Stein, Ross L.
Jahr: 2011
CONTENTS
Preface xi
1 INTRODUCTION 1
1.1 A Brief History of Enzymology 2
1.2 Goal of 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
vii
ViÜ CONTENTS
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
CONTENTS ¡X
y ALLOSTERIC MODULATION OF ENZYME ACTIVITY 199
9.1 Mechanisms of Enzyme Modulation 201
9.2 Kinetics of Allosteric Modulation 202
9.3 Meaning of ß and y 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.I 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.I 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
|
| any_adam_object | 1 |
| author | Stein, Ross L. |
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| author_sort | Stein, Ross L. |
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| dewey-ones | 572 - Biochemistry |
| dewey-raw | 572/.7 |
| dewey-search | 572/.7 |
| dewey-sort | 3572 17 |
| dewey-tens | 570 - Biology |
| discipline | Chemie / Pharmazie Biologie |
| format | Book |
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| illustrated | Illustrated |
| indexdate | 2024-07-10T00:05:38Z |
| institution | BVB |
| isbn | 9780470414118 |
| language | English |
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| physical | XII, 302 S. graph. Darst. |
| publishDate | 2011 |
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| publisher | Wiley |
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| spelling | Stein, Ross L. Verfasser aut Kinetics of enzyme action essential principles for drug hunters Ross L. Stein Hoboken, NJ Wiley 2011 XII, 302 S. graph. Darst. txt rdacontent n rdamedia nc rdacarrier Enzym (DE-588)4014988-2 gnd rswk-swf Reaktionskinetik (DE-588)4048655-2 gnd rswk-swf Enzym (DE-588)4014988-2 s Reaktionskinetik (DE-588)4048655-2 s DE-604 HBZ Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=024383701&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Stein, Ross L. Kinetics of enzyme action essential principles for drug hunters Enzym (DE-588)4014988-2 gnd Reaktionskinetik (DE-588)4048655-2 gnd |
| subject_GND | (DE-588)4014988-2 (DE-588)4048655-2 |
| title | Kinetics of enzyme action essential principles for drug hunters |
| title_auth | Kinetics of enzyme action essential principles for drug hunters |
| title_exact_search | Kinetics of enzyme action essential principles for drug hunters |
| title_full | Kinetics of enzyme action essential principles for drug hunters Ross L. Stein |
| title_fullStr | Kinetics of enzyme action essential principles for drug hunters Ross L. Stein |
| title_full_unstemmed | Kinetics of enzyme action essential principles for drug hunters Ross L. Stein |
| title_short | Kinetics of enzyme action |
| title_sort | kinetics of enzyme action essential principles for drug hunters |
| title_sub | essential principles for drug hunters |
| topic | Enzym (DE-588)4014988-2 gnd Reaktionskinetik (DE-588)4048655-2 gnd |
| topic_facet | Enzym Reaktionskinetik |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=024383701&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
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