Full Description
This second edition volume expands on the previous edition with a discussion of the latest experimental and computational strategies used in the study, characterization, and targeting of enzymes with therapeutic potential. The chapters in the book are organized into two parts: Part One presents detailed, reproducible protocols for enzyme characterization, inhibitor screening, and biochemical analysis. Part Two is dedicated to computational and in silico methodologies, reflecting the growing impact of computational biology in drug discovery. Written in the highly successful Methods in Molecular Biology series format, 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.
Cutting-edge and authoritative, Targeting Enzymes for Pharmaceutical Development: Methods and Protocols, Second Edition is a valuable resource for academic and industrial scientists in medicinal chemistry, chemical biology, pharmaceutical biotechnology, structural biology, and computational drug discovery. This book is both a technical manual and conceptual guide for scientists engaged in enzyme-related drug discovery and development.
Contents
Measuring Protein-Ligand Binding by Thermal Shift Assay.- Applications of Differential Scanning Fluorimetry and Related Technologies in Characterization of Protein-Ligand Interactions.- Enzyme-Ligand Interaction Monitored by Synchrotron Radiation Circular Dichroism.- Binding Interaction Analysis of Lysozyme and Brilliant Blue using Surface Plasmon Resonance.- Evaluation of Endolysin Activity Using Nephelometric Assays with Whole Bacterial Cells and Isolated Peptidoglycan.- In Vitro Assays for Endolysin Efficacy and Safety Profiling.- Droplet-Based Microfluidics Methods for Detecting Enzyme Inhibitors.- HMG-CoA Reductase Inhibition Assays: Updated Protocols for Drug Discovery and Enzyme Kinetics.- The Enzyme-Bag Platform for Cytochrome P450 Biotransformation and High-Throughput Drug Metabolism Screening.- Enzymatic Bioautographic Methods.- On-Line Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 Inhibitors.- Isolation and Endopeptidase Inhibition of Human α2-Macroglobulin.- Harnessing Affinity Tags for Recombinant Protein Purification: Concepts, Methods, and Troubleshooting.- Computational Strategies for Discovering Inhibitors Targeting Therapeutic Enzymes.- Computational Study of Enzyme Inhibition.- In Silico Laboratory: New and Updated Tools for Protein-Centered Drug Discovery.- Combined In Silico Approaches for Virtual Screening of Non-Covalent Immunoproteasome Inhibitors for Multiple Myeloma Treatment.- Deep Learning Pipeline for Accelerating Virtual Screening in Drug Discovery.- In Silico Methodology for Human Carboxylesterases 1 and 2 Isoforms Substrate Selectivity Study.
