Screen LibraryEvaluation of enzyme inhibitors in drug discovery：a guide for medicinal chemists and pharmacologists
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| Main Authors: | |
|---|---|
| Published: |
Wiley,
|
| Publisher Address: | Hoboken, N.J. |
| Publication Dates: | c2013. |
| Literature type: | Book |
| Language: | English |
| Edition: | 2nd ed. |
| Subjects: | |
| Carrier Form: | xxxi, 538 p.: ill. ; 25 cm. |
| ISBN: |
9781118488133 (hardback) 111848813X (hardback) |
| Index Number: | R917 |
| CLC: | R917 |
| Call Number: | R917/C790/2nd ed. |
| Contents: |
Machine generated contents note: Foreword.Preface.Acknowledgments.1. Why Enzymes as Drug Targets?1.1 Enzymes Are Essentials for Life.1.2 Enzyme Structure and Catalysis.1.3 Permutations of Enzyme Structure During Catalysis.1.4 Other Reasons for Studying Enzymes.1.5 Summary.References.2. Enzyme Reaction Mechanisms.2.1 Initial Binding of Substrate.2.2 Noncovalent Forces in Reversible Ligand Binding to Enzymes.2.2.1 Electrostatic Forces.2.2.2 Hydrogen Bonds.2.2.3 Hydrophobic Forces.2.2.4 van der Waals Forces.2.3 Transformations of the Bond Substrate.2.3.1 Strategies for Transition State Stabilization.2.3.2 Enzyme Active Sites Are Most Complementary to the Transition State Structure.2.4 Steady State Analysis of Enzyme Kinetics.2.4.1 Factors Affecting the Steady State Kinetic Constants.2.5 Graphical Determination of kcat and KM2.6 Reactions Involving Multiple Substates.2.6.1 Bisubstrate Reaction Mechanisms.2.7 Summary.References.3. Reversible Modes of Inhibitor Interactions with Enzymes.3.1 Enzyme-Inhibitor Binding Equilibria.3.2 Competitive Inhibition.3.3 Noncompetitive Inhibition.3.3.1 Mutual Exclusively Studies.3.4 Uncompetitive Inhibition.3.5 Inhibition Modality in Bisubstrate Reactions... Includes bibliographical references and index. "There has been explosive growth in the hunt for new pharmaceutically agents globally. Traditionally, this has been the purview of the pharmaceutical industry, but today, this effort crosses academic, government, and industry laboratories across the world. Enzymes remain the most valued and common of drug targets; hence, a detailed understanding of their interactions with inhibitors is critical to successful drug discovery. This book provides a practical, readable, and comprehensive treatment of these topics that allows scientists to master the art of applied enzymology for drug discovery. The book addresses the opportunities for inhibitor interactions with enzyme targets arising from consideration of the catalytic reaction mechanism... |