By Robert A. Copeland
Offers crucial counsel for locating and optimizing novel drug therapies
Using specific examples, Evaluation of Enzyme Inhibitors in Drug Discovery equips researchers with the instruments had to practice the technological know-how of enzymology and biochemistry to the invention, optimization, and preclinical improvement of gear that paintings by way of inhibiting particular enzyme ambitions. Readers will applaud this e-book for its transparent and useful shows, together with its professional recommendation on most sensible practices to keep on with and pitfalls to avoid.
This Second Edition brings the publication completely brand new with the newest study findings and practices. Updates discover extra different types of enzyme inhibition and particular remedies for enzymes that act on macromolecular substrates. Readers also will locate new discussions detailing the advance and alertness of the concept that of drug-target place of dwelling time.
Evaluation of Enzyme Inhibitors in Drug Discovery starts via explaining why enzymes are such vital drug goals after which examines enzyme response mechanisms. The ebook covers:
- Reversible modes of inhibitor interactions with enzymes
- Assay issues for compound library screening
- Lead optimization and structure-activity relationships for reversible inhibitors
- Slow binding and tight binding inhibitors
- Drug-target place of dwelling time
- Irreversible enzyme inactivators
The e-book ends with a brand new bankruptcy exploring the applying of quantitative biochemical rules to the pharmacologic overview of drug applicants in the course of lead optimization and preclinical development.
The Second Edition of Evaluation of Enzyme Inhibitors in Drug Discovery keeps to supply a remedy of enzymology utilized to drug discovery that's quantitative and mathematically rigorous. even as, the transparent and straightforward shows demystify the advanced technology of enzymology, making the e-book available to many fields— from pharmacology to medicinal chemistry to biophysics to scientific medicine.
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Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists by Robert A. Copeland