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Evaluation of enzyme inhibitors in drug discovery : a guide for medicinal chemists and pharmacologists / Robert A. Copeland.

By: Series: Methods of biochemical analysis ; v. 46Publication details: Hoboken, N.J. : Wiley-Interscience, 2005.Description: xvii, 271 p. : ill. ; 25 cmISBN:
  • 0471686964 (hbk.)
Subject(s): DDC classification:
  • 615.19 COP
Contents:
Foreword. - Preface. - Acknowledgments. - 1. Why enzymes as drug targets? - 2. Enzyme reaction mechanisms. - 3. Reversible modes of inhibitor interactions with enzymes. - 4. Assay considerations for compound library screening. - 5. Lead optimization and structrue-activity relationships for reversible inhibitors. - 6. Slow binding inhibitors. - 7. Tight binding inhibitors. - 8. Irreversible enzyme inactivators. - Appendix 1. Kinetics of biochemical reactions. - Appendix 2. Derivation of the enzyme-ligand binding isotherm equation. - Appendix 3. Serial dilution schemes. - Index.
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Includes bibliographical references and index.

Foreword. - Preface. - Acknowledgments. - 1. Why enzymes as drug targets? - 2. Enzyme reaction mechanisms. - 3. Reversible modes of inhibitor interactions with enzymes. - 4. Assay considerations for compound library screening. - 5. Lead optimization and structrue-activity relationships for reversible inhibitors. - 6. Slow binding inhibitors. - 7. Tight binding inhibitors. - 8. Irreversible enzyme inactivators. - Appendix 1. Kinetics of biochemical reactions. - Appendix 2. Derivation of the enzyme-ligand binding isotherm equation. - Appendix 3. Serial dilution schemes. - Index.