This volume is focused on the application of enzymology to drug discovery, with the overarching objective of introducing the general audience to the important role that enzymology plays in modern, molecular targeted drug discovery. The volume opens with a chapter on the role of enzymes in normal human physiology and the causal role played by aberrant enzyme activity in various disease state. A second chapter provides a comprehensive review of inhibition modalities for therapeutic enzyme inhibitors. From there the volume is composed of chapters that cover two general categories of information: (1) methodologies for studying enzyme-ligand interactions and (2) case studies of molecular targeted drug discovery against specific enzyme targets. Chapters within the first category cover methods such as assay design, the role of structural biology in drug optimization, analysis of slow and tight binding inhibitors, enzyme-inhibitor complex dynamics, and covalent enzyme inactivators. The second category includes case studies of therapeutic inhibitors of various enzyme target classes: proteases, methyltransferases, histone demethylases, helicases, nucleic acid processing enzymes, kinesin motor proteins, and cytochrome P450s. Finally, a chapter is also devoted to therapeutic replacement or repair of defective enzymes.
- Highlights key methodologies for the study of enzymes as therapeutic targets
- Provides in-depth case studies of enzyme-targeted therapeutic agents
- Introduces the reader to the dynamic and multidisciplinary approaches necessary in the search for new medicines
