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Enzymes as Targets for Drug Design - 1st Edition - ISBN: 9780125440301, 9780323140485

Enzymes as Targets for Drug Design

1st Edition

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Author: Michael Palfreyman
eBook ISBN: 9780323140485
Imprint: Academic Press
Published Date: 28th December 1989
Page Count: 267
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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



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



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© Academic Press 1989
28th December 1989
Academic Press
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About the Author

Michael Palfreyman

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