Overview

The goal of this book is to provide chemists and pharmacologists with the key information they need to answer questions such as: What opportunities for inhibitor interactions with enzyme targets arise from consideration of the catalytic reaction mechanism? How are inhibitors properly evaluated for potency, selectivity, and mode of action? What are the potential advantages and liabilities of specific inhibition modalities with respect to efficacy in vivo? And finally, what information should medicinal chemists and pharmacologist expect from their biochemistry/enzymology colleagues in order to most effectively pursue lead optimization?

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9780471686965

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Reviews

...a valuable addition to the library of individual investigators, as well as a must for any reference collection. (Drug Development and Industrial Pharmacy, No. 3, 2006) This book serves as an extremely valuable starting point for anyone who needs to acquire/or interpret good kinetic data for enzyme inhibition. (Clinical Chemistry, November 2005)

Author Information

ROBERT A. COPELAND, PhD, is Department Head of Enzymology and Mechanistic Pharmacology at GlaxoSmithKline, and Adjunct Professor of Biochemistry and Biophysics at the University of Pennsylvania School of Medicine. Dr. Copeland has published more than 100 papers and reviews and has authored three books, including Enzymes: A Practical Introduction to Structure, Mechanism, and Data Analysis, Second Edition (Wiley).

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