Kinetics of Enzyme Action: Essential Principles for Drug Hunters

Cover
John Wiley & Sons, 08.08.2011 - 320 Seiten
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.
 

Ausgewählte Seiten

Inhalt

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
Urheberrecht

Andere Ausgaben - Alle anzeigen

Kinetics of Enzyme Action: Essential Principles for Drug Hunters
Ross L. Stein
Eingeschränkte Leseprobe - 2011

Häufige Begriffe und Wortgruppen

activity allosteric modulation analysis assay best-fit Biochemistry catalysis catalytic Chapter chemical competitive inhibition conformational isomerization data set derivation determined dissociation constants drug discovery enzymatic reactions enzyme form enzyme inhibition enzyme kinetics enzyme’s equal estimates expression free energy diagrams free enzyme half reaction hydrolysis inhibitor binds inhibitor concentration initial velocity intermediate isotope effects kc/Km Ki,app Ki,e kinase kinetic mechanism kobs koff mechanism of Figure mechanism of inhibition mechanistic Michaelis complex Michaelis–Menten equation mixed inhibition molecule one-substrate ordered mechanism peptide pH dependence ping-pong mechanism progress curve protein random mechanism rapid equilibrium rate constant rate equation rate law rate parameters rate-limiting reactant reaction progress rearranged secondary plots sequential mechanisms shown in Figure simulations SIRT1 sirtuins slow-binding inhibition Stein studies substrate analog substrate concentration substrate inhibition tion titration transition two-substrate reactions uncompetitive VA,obs values Vmax

Autoren-Profil (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.

Bibliografische Informationen

TitelKinetics of Enzyme Action: Essential Principles for Drug Hunters
Autor/inRoss L. Stein
VerlagJohn Wiley & Sons, 2011
ISBN1118084403, 9781118084403
Länge320 Seiten
  
Zitat exportierenBiBTeX EndNote RefMan