Targeting Enzymes for Pharmaceutical Development: Methods and Protocols

ISBN-13: 9781071601655 / Angielski / Miękka / 2020 / 290 str.

Nikolaos E. Labrou

Spis treści

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

            Samo Lešnik 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 Řemínek, and Zdeněk 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 Řemínek, Zdeněk 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. Olguín

 

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

Blurb

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.

The chapter “Enzyme–Ligand Interaction Monitored by Synchrotron Radiation Circular Dichroism” is available open access under a Creative Commons Attribution 4.0 International License via link.springer.com.