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Kinetics of Enzyme Action:

Essential Principles for Drug Hunters (Google eBook)
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John Wiley & Sons, Aug 8, 2011 - Science - 320 pages
Few scientists have the knowledge to perform the studies that are necessary to discover and characterize enzyme inhibitors, despite the vested interest the pharmaceutical industry has in this field. Beginning with the most basic principles pertaining to simple, one-substrate enzyme reactions and their inhibitors, and progressing to a thorough treatment of two-substrate enzymes, Kinetics of Enzyme Action: Essential Principles for Drug Hunters provides biochemists, medicinal chemists, and pharmaceutical scientists with numerous case study examples to outline the tools and techniques necessary to perform, understand, and interpret detailed kinetic studies for drug discovery.
  

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Contents

KINETICS OF SINGLESUBSTRATE ENZYMATIC REACTIONS
19
THE PHENOMENON
73
5
89
6
115
KINETICS OF TWOSUBSTRATE ENZYMATIC REACTIONS 141 7 1 Importance in Drug Discovery
141
8
169
vii
213
KINETICSBASED PROBES OF MECHANISM
219
APPENDIX A BASIC PRINCIPLES OF CHEMICAL KINETICS
251
SELECTING SUBSTRATE CONCENTRATIONS
275
Index
287
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About the author (2011)

ROSS L. 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 VELCADETM, 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. Most recently, from 2009-2011, Dr. Stein was vice president of drug discovery at Sirtris Pharmaceuticals.

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