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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.
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
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
- No. of pages:
- © Academic Press 1989
- 28th December 1989
- Academic Press
- eBook ISBN: