Saturday, May 10, 2008
|Evaluation Of Enzyme Inhibitors In Drug Discovery|
Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists
(Methods of Biochemical Analysis)
By Robert A. Copeland
* Publisher: Wiley-Interscience
* Number Of Pages: 296
* Publication Date: 2005-03-28
* Sales Rank: 402011
* ISBN / ASIN: 0471686964
* EAN: 9780471686965
This publication provides readers with a thorough understanding of enzyme-inhibitor evaluation to assist them in their efforts to discover and optimize novel drug therapies. Key topics such as competitive, noncompetitive, and uncompetitive inhibition, slow binding, tight binding, and the use of Hill coefficients to study reaction stoichiometry are all presented. Examples of key concepts are presented with an emphasis on clinical relevance and practical applications.
Targeted to medicinal chemists and pharmacologists, Evaluation of Enzyme Inhibitors in Drug Discovery focuses on the questions that they need to address:
* What opportunities for inhibitor interactions with enzyme targets arise from consideration of the catalytic reaction mechanism?
* How are inhibitors evaluated for potency, selectivity, and mode of action?
* What are the advantages and disadvantages of specific inhibition modalities with respect to efficacy in vivo?
* What information do medicinal chemists and pharmacologists need from their biochemistry and enzymology colleagues to effectively pursue lead optimization?
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