Research Catalog

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

Title
Evaluation of enzyme inhibitors in drug discovery : a guide for medicinal chemists and pharmacologists / Robert A. Copeland.
Author
Copeland, Robert Allen.
Publication
Hoboken, N.J. : J. Wiley, 2005.

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Details

Description
xvii, 271 pages : illustrations; 25 cm
Summary
"This publication provides readers with a thorough understanding of enzyme-inhibitor evaluation to assist them in their efforts to discover and optimize novel drug therapies. Key topics such as competitive, noncompetitive, and uncompetitive inhibition, slow binding, tight binding, and the use of Hill coefficients to study reaction stoichiometry are all presented. Examples of key concepts are presented with an emphasis on clinical relevance and practical applications."--BOOK JACKET.
Subjects
Bibliography (note)
  • Includes bibliographical references and index.
Contents
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 structure-activity relationships for reversible inhibitors -- 6. Slow binding inhibitors -- 7. Tight binding inhibitors -- 8. Irreversible enzyme inactivators -- App. 1. Kinetics of biochemical reactions -- App. 2. Derivation of the enzyme-ligand binding isotherm equation -- App. 3. Serial dilution schemes.
ISBN
0471686964 (cloth : alk. paper)
LCCN
2004023470
OCLC
  • 56793559
  • ocm56793559
  • SCSB-5166298
Owning Institutions
Columbia University Libraries