Evaluation Of Enzyme Inhibitors In Drug Discovery: A Guide For Medicinal Chemists And Pharmacologists

Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists

Offers essential guidance for discovering and optimizingnovel drug therapies

Using detailed examples, Evaluation of Enzyme Inhibitors inDrug Discovery equips researchers with the tools needed toapply the science of enzymology and biochemistry to the discovery,optimization, and preclinical development of drugs that work byinhibiting specific enzyme targets. Readers will applaud this bookfor its clear and practical presentations, including its expertadvice on best practices to follow and pitfalls to avoid.

This Second Edition brings the book thoroughly up to datewith the latest research findings and practices. Updates exploreadditional forms of enzyme inhibition and special treatments forenzymes that act on macromolecular substrates. Readers will alsofind new discussions detailing the development and application ofthe concept of drug-target residence time.

Evaluation of Enzyme Inhibitors in Drug Discovery beginsby explaining why enzymes are such important drug targets and thenexamines enzyme reaction mechanisms. The book covers:

• Reversible modes of inhibitor interactions with enzymes
• Assay considerations for compound library screening
• Lead optimization and structure-activity relationships forreversible inhibitors
• Slow binding and tight binding inhibitors
• Drug-target residence time
• Irreversible enzyme inactivators

The book ends with a new chapter exploring the application ofquantitative biochemical principles to the pharmacologic evaluationof drug candidates during lead optimization and preclinicaldevelopment.

The Second Edition of Evaluation of Enzyme Inhibitorsin Drug Discovery continues to offer a treatment of enzymologyapplied to drug discovery that is quantitative and mathematicallyrigorous. At the same time, the clear and simple presentationsdemystify the complex science of enzymology, making the bookaccessible to many fields— from pharmacology to medicinalchemistry to biophysics to clinical medicine.