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Kinetics of Enzyme Action: Essential Principles for Drug Hunters Hardcover – August 23, 2011

ISBN-13: 978-0470414118 ISBN-10: 0470414111 Edition: 1st

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Kinetics of Enzyme Action: Essential Principles for Drug Hunters + Enzyme Kinetics for Systems Biology + Fundamentals of Enzyme Kinetics
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Editorial Reviews

Review

"Kinetics of Enzyme Action: Essential Principles for Drug Hunters provides a needed resource for pharmaceutical scientists whose job it is to discover and kinetically characterize enzyme inhibitors. This book starts with the most basic principles pertaining to simple, one-substrate enzyme reactions and their inhibitors, and progresses to a thorough treatment of two-substrate enzymes and their inhibitors." (News Blaze, 18 October 2011)

From the Back Cover

"Dr. Stein . . . make[s] a difficult topic easy to understand and comprehend."
Richard Harrison, Wyeth Research

Details on the approaches and applications essential to kinetically characterizing enzyme inhibitors for drug discovery

The ability of enzymes to bring about the transformation of one chemical substance into another makes them the favorite—and most productive—drug target in the pharmaceutical industry. Kinetics of Enzyme Action explores, in depth, the characteristics and applications of these proteins and their vital role in the development of new medicines by placing the subject of enzymology in a historical context that enriches and heightens understanding of this complex science. It introduces readers to a wide range of topics invaluable for helping them discover and kinetically characterize enzyme inhibitors—from simple, one-substrate enzyme reactions to the more complex two-substrate enzymes reactions. Some of the highlights in this book include:

  • A detailed description of enzyme kinetics as applied to drug discovery
  • A comprehensive collection of theory and pragmatic approaches to guide readers in the science of performing detailed enzyme mechanistic studies
  • An outline of the tools and techniques necessary to perform, understand, and interpret detailed kinetic studies for drug discovery
  • Numerous case studies from scientific literature that bring the topics to life

From discussion of the early developments in the kinetics of enzymatic reactions to fresh insights on contemporary enzymology, Kinetics of Enzyme Action offers comprehensive coverage of a discipline that holds vital significance for all pharmaceutical practitioners.

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Product Details

  • Hardcover: 320 pages
  • Publisher: Wiley; 1 edition (August 23, 2011)
  • Language: English
  • ISBN-10: 0470414111
  • ISBN-13: 978-0470414118
  • Product Dimensions: 6.3 x 0.9 x 9.6 inches
  • Shipping Weight: 1.4 pounds (View shipping rates and policies)
  • Average Customer Review: 5.0 out of 5 stars  See all reviews (1 customer review)
  • Amazon Best Sellers Rank: #1,923,764 in Books (See Top 100 in Books)

More About the Author

Ross Stein received his PhD in physical organic chemistry from Indiana University in 1978, after which he conducted post-doctoral research in mechanistic enzymology at the University of Kansas. His career has included positions at Merck, where he headed the Enzymology Department, and ProScript (acquired by Millennium in 1999) as vice president of biochemistry. At ProScript, Dr. Stein was instrumental in the pre-clinical development and co-inventor of the drug Velcade, a proteasome inhibitor used to treat multiple myeloma. In 2001, he accepted a position at Harvard Medical School to establish and head the Laboratory for Drug Discovery in Neurodegeneration. Leaving Harvard in 2009, Dr. Stein became Vice President of Discovery Research at Sirtris Pharmaceuticals where he and his team elucidated the mechanism of activation of the sirtuin family of protein deacetylases. In 2011, Dr. Stein accepted the position of Deputy Director of the Institute for Advancing Medical Innovation of the University of Kansas Medical Center. Dr. Stein's drug discovery responsibilities at the University of Kansas also included directing the High-Throughput Screening Laboratory, and the Laboratory for Early Stage Translational Research, which he founded. In 2013, Dr. Stein joined Targanox (Cambridge, MA) as Chief Scientific Officer.

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By JFFisher on March 21, 2012
Format: Hardcover Verified Purchase
The past decade has seen the publication of several outstanding texts on enzyme kinetics -- remarkably, each with different context and focus -- and to this list of outstanding texts we may now add Stein's "Kinetics of Enzyme Action". This text has particular strengths as both an introductory text as well as a desk reference for the maturing kineticist. I'll comment with respect to the former: including its concise appendix on basic kinetics, its historical introduction, and its exceptionally clear presentation of the mathematics. The figures complement particularly well the text. For example, the breadth of the initial velocity in a representative Michaelis-Menton progress curve (Fig. 2.1), the temporal correlation in this same progress curve of pre-steady state, steady-state, and post-steady state (Fig. 2.7), integrating the concepts of different k values in successive kforward/kreverse pairings with free energy diagrams (Fig. 3.6), criteria for the phenomenon of enzyme inhibition (Fig. 4.2, Fig. 5.7), and the emphatic emphasis (an emphasis that should never be forgotten!) that "all inhibition is time-dependent" (Figs. 6.6 & 6.7). There is no perfect text on enzyme kinetics--don't wait for it to appear--but in terms of its uncompromising rigor and clarity, Stein's "Kinetics" provides a resounding cornerstone covering this topic on your bookshelf.
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