Kinetics of Enzyme Action (ePub)

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 The Dependence of Initial Velocity on Substrate Concentration and the Requirement for 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 Enzyme Assay. 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 Importance in 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

ROSS L. STEIN received his PhD in physical organic chemistry from Indiana University in 1978, after which he conducted post-doctoral research in mechanistic enzymology at the University of Kansas. His career has included positions at Merck, where he headed the Enzymology Department, and ProScript (acquired by Millennium in 1999) as vice president of biochemistry. At ProScript, Dr. Stein was instrumental in the pre-clinical development and co-inventor of the drug VELCADETM, a proteasome inhibitor used to treat multiple myeloma. In 2001, he accepted a position at Harvard Medical School to establish and head the Laboratory for Drug Discovery in Neurodegeneration. Most recently, from 2009-2011, Dr. Stein was vice president of drug discovery at Sirtris Pharmaceuticals.

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