Enzymes as Targets for Drug Design

Enzymes as Targets for Drug Design

1st Edition - December 25, 1989

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  • Author: Michael Palfreyman
  • eBook ISBN: 9780323140485

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Enzymes as Targets for Drug Design is a collection of scientific discussions related to enzyme inhibitors that show the many facets of the drug discovery process from the basic sciences through clinical applications. Topics include the biogenesis of phosphatidylinositol glycosyl membrane proteins, structure and catalytic function of ADP-ribose polymerase (ADPRT), and modulation of the dopaminergic system in cardiovascular therapeutics. The therapeutic utility of selected enzyme-activated irreversible inhibitors, the role of proteinases in the fibrosis of systemic sclerosis, and therapeutic opportunities in eicosanoid biosynthesis are also discussed. This book consists of 18 chapters and begins with examples of enzymes whose activities have recently been elucidated, or for which newer insights have been gleaned, but which do not yet have selective or potent inhibitors. The second part provides examples of enzymes where inhibitors have been identified but it is still not clear whether or not such an enzymatic blockade will be therapeutically beneficial. The final section describes clinical studies of newer, and not so new, enzyme inhibitors that are clearly of therapeutic importance. The therapeutic activity of monoamine oxidase inhibitors and the associated clinical issues are considered. This book is intended for clinicians as well as basic scientists in biochemistry, chemistry, pharmacology, and cell biology.

Table of Contents

  • Contributors


    1. Enzyme Inhibitors as Drugs

    2. Biogenesis of Phosphatidylinositol Glycosyl Membrane Proteins and Their Significance

    3. Structure and Catalytic Function of ADP-Ribose Polymerase (ADPRT), a Target Site for Drugs Inhibiting Malignant Growth

    4. Modulation of the Dopaminergic System in Cardiovascular Therapeutics

    5. Alpha-Methyldopa

    6. Considering Receptor Non-Specificity as a Factor for Developing Effect, Tissue and Receptor Specific Agents

    7. Mechanism-Based Enzyme Inhibitors as an Approach to Drug Design

    8. Cofactor Dependency in the Inhibition of Steroid 5 Alpha-Reductase

    9. Hydroxylases as Targets for Drug Design

    10. Alpha-Fluoromethyltyrosine, Alpha-Fluoromethyltryptophan and Biogenic Amine Synthesis

    11. Tyrosine and Tryptophan Analogues as Dual Enzyme-Activated Inhibitors of Monoamine Oxidase

    12. Inhibition of Polyamine Biosynthesis and Function as an Approach to Drug Design

    13. Concepts for Deriving Specific Inhibitors of Polyamine Biosynthesis—Human Lung Cancer Cells as a Model System

    14. Therapeutic Utility of Selected Enzyme-Activated Irreversible Inhibitors

    15. Intra-Blood-Brain-Barrier IgG Synthesis in HIV

    16. Proteinases in the Fibrosis of Systemic Sclerosis

    17. Therapeutic Opportunities in Eicosanoid Biosynthesis

    18. MAO as a Target for Drug Design: Clinical Issues


Product details

  • No. of pages: 267
  • Language: English
  • Copyright: © Academic Press 1989
  • Published: December 25, 1989
  • Imprint: Academic Press
  • eBook ISBN: 9780323140485

About the Author

Michael Palfreyman

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