Targeting Enzymes for Pharmaceutical Development

This volume explores detailed methods and experimental protocols evaluating the effect of a compound or a mixture of compounds on the action of enzymes that are significant targets in pharmaceuticals. Consisting of three sections, the book delves into recent biocomputing and bioinformatics protocols, state-of-the art modern biophysical, electrophoretic, and chromatographic methods and high-throughput screening approaches, as well as detailed protocols and examples of the inhibition analysis and evaluation of selected enzymes. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls.
Authoritative and cutting-edge, Targeting Enzymes for Pharmaceutical Development: Methods and Protocols serves as a vital reference for academics and industry professionals working on expanding our understanding of the wide range of important enzyme targets.

Includes cutting-edge techniques Provides step-by-step detail essential for reproducible results Contains key implementation advice from the experts

Inhalt
In Silico Laboratory: Tools for Similarity-Based Drug Discovery.- The In Silico Fischer Lock-and-Key Model: The Combined Use of Molecular Descriptors and Docking Poses for the Repurposing of Old Drugs.- Determination of Half-Maximal Inhibitory Concentration of an Enzyme Inhibitor.- Applications of Differential Scanning Fluorometry and Related Technologies in Characterization of Protein-Ligand Interactions.- High-Throughput Differential Scanning Fluorimetry of GFP-Tagged Proteins.- Enzyme-Ligand Interaction Monitored by Synchrotron Radiation Circular Dichroism.- Measuring Small Molecule Binding to Escherichia coli AcrB by Surface Plasmon Resonance.- Systematic Screening of Viral Entry Inhibitors Using Surface Plasmon Resonance.- Screening of Beta-Secretase Inhibitors by Capillary Electrophoresis-Mass Spectrometry.- Electrophoretic Mobility Shift Assays with GFP-Tagged Proteins (GFP-EMSA).- On-Line Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4Inhibitors.- Enzymatic Bioautographic Methods.- High-Throughput Assessment of Metabolism-Induced Toxicity of Compounds on a 384-Pillar Plate.- Droplet-Based Microfluidics Methods for Detecting Enzyme Inhibitors.- Ligand Fishing: An Approach for the Discovery Inhibitors from Complex Biological Mixtures.- HMG-CoA Reductase as Target for Drug Development.- Lipoxygenases as Targets for Drug Development.- Cholinesterase as a Target for Drug Development in Alzheimer's Disease.