Offers essential guidance for discovering and optimizing
novel drug therapies
Using detailed examples, Evaluation of Enzyme Inhibitors in
Drug Discovery equips researchers with the tools needed to
apply the science of enzymology and biochemistry to the discovery,
optimization, and preclinical development of drugs that work by
inhibiting specific enzyme targets. Readers will applaud this book
for its clear and practical presentations, including its expert
advice on best practices to follow and pitfalls to avoid.
This Second Edition brings the book thoroughly up to date
with the latest research findings and practices. Updates explore
additional forms of enzyme inhibition and special treatments for
enzymes that act on macromolecular substrates. Readers will also
find new discussions detailing the development and application of
the concept of drug-target residence time.
Evaluation of Enzyme Inhibitors in Drug Discovery begins
by explaining why enzymes are such important drug targets and then
examines enzyme reaction mechanisms. The book covers:
* Reversible modes of inhibitor interactions with enzymes
* Assay considerations for compound library screening
* Lead optimization and structure-activity relationships for
reversible inhibitors
* Slow binding and tight binding inhibitors
* Drug-target residence time
* Irreversible enzyme inactivators
The book ends with a new chapter exploring the application of
quantitative biochemical principles to the pharmacologic evaluation
of drug candidates during lead optimization and preclinical
development.
The Second Edition of Evaluation of Enzyme Inhibitors
in Drug Discovery continues to offer a treatment of enzymology
applied to drug discovery that is quantitative and mathematically
rigorous. At the same time, the clear and simple presentations
demystify the complex science of enzymology, making the book
accessible to many fields– from pharmacology to medicinal
chemistry to biophysics to clinical medicine.
About the author
ROBERT A. COPELAND, Ph D, is Executive Vice President and
Chief Scientific Officer at Epizyme, Inc., a biopharmaceutical
company in Cambridge, Massachusetts. He is on the Editorial Board
of The Journal of Biological Chemistry and a member
of the Faculty of 1000. Dr. Copeland has contributed more than 175
publications to the scientific literature and holds eight
U.S.-issued patents. He has authored several books in protein
science and enzymology, including Enzymes: A Practical
Introduction to Structure, Mechanism, and Data Analysis, Second
Edition (Wiley).
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