Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad

Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad

Editor(s): Chuang Lu, Albert P. Li

Published Online: 23 FEB 2010

Print ISBN: 9780470281741

Online ISBN: 9780470538951

DOI: 10.1002/9780470538951

About this Book

The science and applied approaches of enzyme inhibition in drug discovery and development

Offering a unique approach that includes both the pharmacologic and pharmaco-kinetic aspects of enzyme inhibition, Enzyme Inhibition in Drug Discovery and Development examines the scientific concepts and experimental approaches related to enzyme inhibition as applied in drug discovery and drug development.

With chapters written by over fifty leading experts in their fields, Enzyme Inhibition in Drug Discovery and Development fosters a cross-fertilization of pharmacology, drug metabolism, pharmacokinetics, and toxicology by understanding the "good" inhibitions-desirable pharmacological effects-and "bad" inhibitions-drug-drug interactions and toxicity. The book discusses:

  • The drug discovery process, including drug discovery strategy, medicinal chemistry, analytical chemistry, drug metabolism, pharmacokinetics, and safety biomarker assessment

  • The manipulations of drug metabolizing enzymes and transporters as well as the negative consequences, such as drug-drug interactions

  • The inhibition of several major drug target pathways, such as the GPCR pathway, the NFkB pathway, and the ion channel pathway

Through this focused, single-source reference on the fundamentals of drug discovery and development, researchers in drug metabolism and pharmacokinetics (DMPK) will learn and appreciate target biology in drug discovery; discovery biologists and medicinal chemists will also broaden their understanding of DMPK.

Table of contents

    1. You have free access to this content
    1. You have free access to this content
  1. Part I: Drug Discovery Approaches and Technologies

    1. Chapter 6

      Applied Pharmacokinetics in Drug Discovery and Development (pages 177–239)

      Hua Yang, Xingrong Liu, Anjaneya Chimalakonda, Zheng Lu, Cuiping Chen, Frank Lee and Wen Chyi Shyu

  2. Part II: Inhibition of the Drug Metabolizing Enzymes—The Undesirable Inhibition

    1. Chapter 8

      Cytochrome P450 Induction (pages 265–314)

      Edward L. Lecluyse, Michael W. Sinz, Nicola Hewitt, Stephen S. Ferguson and Jasminder Sahi

    2. Chapter 11

      Cytochrome P450 Degradation and Its Clinical Relevance (pages 363–406)

      Mingxiang Liao, Ping Kang, Bernard P. Murray and Maria Almira Correia

  3. Part III: Inhibition of the Drug Target Enzymes—The Desirable Inhibition

    1. You have free access to this content

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