Kinetics of enzyme action: essential principles for drug hunters

Kinetics of enzyme action: essential principles for drug hunters

Stein, Ross L.

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ÍNDICE: Chapter 1. Introduction. 1.1 A Brief History of Enzymology. 1.2 Goal of Enzymology The Elucidation of Mechanism. 1.3 The Emergence of Mechanism from Data. Chapter 2. Kinetics of Single-Substrate Enzymatic Reactions. 2.1 TheDependence of Initial Velocity on Substrate Concentration and the Requirementfor an Enzyme: Substrate 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 EnzymeAssay. 2.5 Enzyme Kinetics Practicum Assay Development, Experimental Design, Data Collection, and Data Analysis. Chapter 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 Enzyme Action on Substrates with Multiple Reactive Centers. Chapter 4. Enzyme Inhibition The Phenomenon and Mechanistic 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. Chapter 5. Kinetic Mechanism of Inhibition of One-Substrate Enzymatic Reactions. 5.1 Importance in Drug Discovery. 5.2 Theoretical Consideration. 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. Chapter 6. Tight-Binding, Slow-Binding, and Irreversible Inhibitors. 6.1 Importancein Drug Discovery. 6.2 Tight-Binding Inhibition. 6.3 Slow-Binding Inhibition.6.4 Irreversible Inhibition. Chapter 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 KineticMechanism for Two-Substrate Reactions. 7.7 A Conceptual Understanding of the Shapes of Secondary Plots. 7.8 Mistaken Identity Rapid Equilibrium Random vs. Steady-State Ordered. Chapter 8. Kinetic Mechanism of Inhibition of Two-Substrate Enzymatic Reactions. 8.1 Importance in Drug Discovery. 8.2 Mechanism of Inhibition of Two-Substrate Reactions. 8.3 Inhibition by Substrate Analogs. 8.4 Analysis of Sequential Mechanisms in which Inhibitor Binds to Enzyme-Product Complexes. 8.5 Driving SAR Programs for Two-Substrate Enzymatic Reactions. Chapter 9. Allosteric Modulation of Enzyme-Catalyzed Reactions. 9.1 Mechanisms of Enzyme Modulation. 9.2 Kinetics of Allosteric Modulation. 9.3 Meaning of ² and³. 9.4 Case Studies Dependence of Allosteric Modulation on Structural Features of the Substrate. Chapter 10. Kinetics-Based Probes of Enzyme Mechanisms. 10.1 pH-Dependence of Enzymatic Reactions. 10.2 Temperature-Dependence of Enzymatic Reactions. 10.3 Viscosity-Dependence of Enz

  • ISBN: 978-0-470-41411-8
  • Editorial: John Wiley & Sons
  • Encuadernacion: Cartoné
  • Páginas: 320
  • Fecha Publicación: 22/07/2011
  • Nº Volúmenes: 1
  • Idioma: Inglés