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

Bibliographic Details
Main Author: Copeland, Robert Allen
Format: Book
Language:English
Published: Hoboken, N.J. : J. Wiley, 2005.
Series:Methods of biochemical analysis ; v. 46.
Subjects:
Table of Contents:
  • Why enzymes as drug targets?
  • Enzyme reaction mechanisms
  • Reversible modes of inhibitor interactions with enzymes
  • Assay considerations for compound library screening
  • Lead optimization and structure-activity relationships for reversible inhibitors
  • Slow binding inhibitors
  • Tight binding inhibitors
  • Irreversible enzyme inactivators
  • Appendix 1. Kinetics of biochemical reactions
  • Appendix 2. Derivation of the enzyme-ligand binding isotherm equation
  • Appendix 3. Serial dilution schemes