Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide by Robert A. Copeland PDF

By Robert A. Copeland

ISBN-10: 111848813X

ISBN-13: 9781118488133

Offers crucial tips for locating and optimizing novel drug therapies

Using certain examples, Evaluation of Enzyme Inhibitors in Drug Discovery equips researchers with the instruments had to practice the technology of enzymology and biochemistry to the invention, optimization, and preclinical improvement of substances that paintings by way of inhibiting particular enzyme pursuits. Readers will applaud this e-book for its transparent and useful displays, together with its specialist suggestion on most sensible practices to keep on with and pitfalls to avoid.

This Second Edition brings the booklet completely brand new with the newest examine 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 idea that of drug-target place of abode time.

Evaluation of Enzyme Inhibitors in Drug Discovery starts by means of explaining why enzymes are such vital drug goals after which examines enzyme response mechanisms. The e-book 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 booklet ends with a brand new bankruptcy exploring the applying of quantitative biochemical rules to the pharmacologic review of drug applicants in the course of lead optimization and preclinical development.

The Second Edition of Evaluation of Enzyme Inhibitors in Drug Discovery maintains to provide a therapy of enzymology utilized to drug discovery that's quantitative and mathematically rigorous. even as, the transparent and straightforward displays demystify the advanced technological know-how of enzymology, making the publication obtainable 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

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