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

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

Label
Evaluation of enzyme inhibitors in drug discovery : a guide for medicinal chemists and pharmacologists
Title
Evaluation of enzyme inhibitors in drug discovery
Title remainder
a guide for medicinal chemists and pharmacologists
Statement of responsibility
Robert A. Copeland
Creator
Subject
Language
eng
Summary
"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; discusses how inhibitors are properly evaluated for potency, selectivity, and mode of action, covers the potential advantages and liabilities of specific inhibition modalities with respect to efficacy in vivo, and provides valuable biochemical insights to help medicinal chemists and pharmacologists most effectively pursue lead optimization. It includes two new chapters, one on the pioneering idea of drug-target residence time fostered by Dr. Copeland, and the second on quantitative biochemistry. Five new appendices are added"--Provided by publisher
Cataloging source
DNLM/DLC
http://library.link/vocab/creatorName
Copeland, Robert Allen
Illustrations
  • illustrations
  • plates
Index
index present
LC call number
QP601.5
LC item number
.C675 2013
Literary form
non fiction
Nature of contents
bibliography
http://library.link/vocab/subjectName
  • Enzyme inhibitors
  • Drugs
  • Enzyme inhibitors
Label
Evaluation of enzyme inhibitors in drug discovery : a guide for medicinal chemists and pharmacologists, Robert A. Copeland
Instantiates
Publication
Bibliography note
Includes bibliographical references and index
Contents
  • Appendix 1.
  • Kinetic of biochemical reactions
  • Appendix 2.
  • Derivation of the enzyme-ligand binding isotherm equation
  • Appendix 3.
  • Serial dilution schemes
  • 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
Dimensions
25 cm.
Edition
2nd ed.
Extent
xxxi, 538 p., [12] p. of plates
Isbn
9781118488133
Isbn Type
(hardback)
Lccn
2012045179
Other physical details
ill. (some col.)
System control number
  • 4193162-01okla_normanlaw
  • (SIRSI)4193162
  • (Sirsi) o818316875
  • (OCoLC)818316875
Label
Evaluation of enzyme inhibitors in drug discovery : a guide for medicinal chemists and pharmacologists, Robert A. Copeland
Publication
Bibliography note
Includes bibliographical references and index
Contents
  • Appendix 1.
  • Kinetic of biochemical reactions
  • Appendix 2.
  • Derivation of the enzyme-ligand binding isotherm equation
  • Appendix 3.
  • Serial dilution schemes
  • 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
Dimensions
25 cm.
Edition
2nd ed.
Extent
xxxi, 538 p., [12] p. of plates
Isbn
9781118488133
Isbn Type
(hardback)
Lccn
2012045179
Other physical details
ill. (some col.)
System control number
  • 4193162-01okla_normanlaw
  • (SIRSI)4193162
  • (Sirsi) o818316875
  • (OCoLC)818316875

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