Main description:

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.

Contents:

1. In Silico Laboratory: Tools for Similarity-Based Drug Discovery

Samo Lesnik and Janez Konc

2. The In Silico Fischer Lock-and-Key Model: The Combined Use of Molecular Descriptors and Docking Poses for the Repurposing of Old Drugs

Marco Tutone and Anna Maria Almerico

3. Determination of Half-Maximal Inhibitory Concentration of an Enzyme Inhibitor

Nikolaos Georgakis, Elisavet Ioannou, Christina Varotsou, Geogios Permetis, Evangelia G. Chronopoulou, and Nikolaos E. Labrou

4. Applications of Differential Scanning Fluorometry and Related Technologies in Characterization of Protein-Ligand Interactions

Bolormaa Baljinnyam, Michael Ronzetti, Adam Yasgar, and Anton Simeonov

5. High-Throughput Differential Scanning Fluorimetry of GFP-Tagged Proteins

Alanna E. Sorenson and Patrick M. Schaeffer

6. Enzyme-Ligand Interaction Monitored by Synchrotron Radiation Circular Dichroism

Rohanah Hussain, Charlotte S Hughes, and Giuliano Siligardi

7. Measuring Small Molecule Binding to Escherichia coli AcrB by Surface Plasmon Resonance

Steven W. Polyak, Rumana Mowla, and Henrietta Venter

8. Systematic Screening of Viral Entry Inhibitors Using Surface Plasmon Resonance

Penmetcha K.R. Kumar

9. Screening of Beta-Secretase Inhibitors by Capillary Electrophoresis-Mass Spectrometry

Jan Schejbal, Roman Reminek, and Zdenek Glatz

10. Electrophoretic Mobility Shift Assays with GFP-Tagged Proteins (GFP-EMSA)

Alanna E. Sorenson and Patrick M. Schaeffer

11. On-Line Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 Inhibitors

Roman Reminek, Zdenek Glatz, and Wolfgang Thormann

12. Enzymatic Bioautographic Methods

I. Ayelen Ramallo, Mario O. Salazar, and Ricardo L.E. Furlan

13. High-Throughput Assessment of Metabolism-Induced Toxicity of Compounds on a 384-Pillar Plate

Soo-Yeon Kang, Kyeong-Nam Yu, Pranav Joshi, and Moo-Yeal Lee

14. Droplet-Based Microfluidics Methods for Detecting Enzyme Inhibitors

Abraham Ochoa, Frida Trejo, and Luis F. Olguin

15. Ligand Fishing: An Approach for the Discovery Inhibitors from Complex Biological Mixtures

Evangelia G. Chronopoulou, Christina Varotsou, Nikolaos Georgakis, Georgios Permetis, Elisavet Ioannou, and Nikolaos E. Labrou

16. HMG-CoA Reductase as Target for Drug Development

Baskaran Gunasekaran and Mohd Yunus Shukor

17. Lipoxygenases as Targets for Drug Development

Xiao-Yuan Mao

18. Cholinesterase as a Target for Drug Development in Alzheimer's Disease

Piyoosh Sharma, Manish Kumar Tripathi, and Sushant Kumar Shrivastava