Main description:

This third edition volume
expands on the previous editions both by presenting more detailed protocols for
the techniques described in the first and second editions of High Throughput
Screening: Methods and Protocols
and by covering important new procedures. The first chapter of
this book provides an overview of important assay development techniques, while
the rest of the chapters detail how to develop and execute screens at whatever
throughput the user needs. Some chapter examples are: structure-based virtual
screening, high throughput screening using mass spectrometry, identification of state-dependent
blockers for voltage gated calcium channels, bioluminescence resonance
energy transfer platform to monitor protein-protein interactions in live cells,
high throughput flow cytometry, and application of imaging-based assays in microplate formats for high
content screening. 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 thorough, High Throughput Screening: Methods and Protocols,
Third Edition, is a valuable resource for anyone who is interested in HTS
research.

Contents:

1. Design and Implementation of High Throughput Screening Assays

David J. Powell, Robert P. Hertsberg,
and Ricardo Macarr n

2. Characterization of Inhibitor
Binding Through Multiple Inhibitor Analysis: A Novel Local Fitting Method

Thomas V. Riera, Tim J. Wigle, and
Robert A. Copeland

3. High Throughput Screening Using
Mass Spectrometry within Drug Discovery

Mattias Rohman and Jonathan Wingfield

4. Structure-Based Virtual Screening
of Commercially Available Compound Libraries

Dmitri Kireev

5. AlphaScreen-Based Assays:
Ultra-High Throughput Screening for Small Molecule Inhibitors of Challenging
Enzymes and Protein-Protein Interactions

Adam Yasgar, Ajit Jadhav, Anton
Simeonov, and Nathan P. Coussens

6. Instrument Quality Control

Chatura Jayakody and Emily A.
Hull-Ryde

7. Application of Fluorescence
Polarization in HTS Assays<
Xinyi Huang and Ann Aulabaugh

8. Time Resolved Fluorescence Assays

Chen-Ting Ma and Eduard A. Sergienko

9. Protein Kinase Selectivity
Profiling Using Microfluid Mobility Shift Assays

Peter Drueckes

10. Screening for Inhibitors of
Kinase Autophosphorylation

Bianca Heedmann and Martin Klumpp

11. A Fluorescence-Based High
Throughput Screening Assay to Identify Growth Inhibitors of the Pathogenic
Fungus Aspergillus fumigatus

Thomas M. Smith, Daryl L. Richie,
Jianshi Tao

12. Mycobacterium tuberculosis
High Throughput Screening

E. Lucile White, Nichole A. Tower,
and Lynn Rasmussen

13. Identification of
State-Dependent Blockers for Voltage Gated Calcium Channels Using a FLIPR Based
Assay

Alberto di Silvio

14. A Luciferase Reporter Gene
System for High Throughput Screening of -Globin Gene
Activators

Wensheng Xie, Robert Silvers, Michael
Ouellette, Zining Wu, Quinn Lu, Hu Li, Kathleen Gallagher, Kathy Johnson, and
Monica Montoute

15. A High Throughput Flow Cytometry
Assay for Identification of Inhibitors of 3', 5'-Cyclic Adenosine Monophosphate
Efflux

Dominique Perez, Peter C. Simons,
Yelena Smagley, Larry A. Sklar, and Alexandre Chigaev

16. High Throughput Cell Toxicity
Assays

David Murray, Lisa McWilliams, and
Mark Wigglesworth

17. BRETn: NanoLuc-Based
Bioluminescence Resonance Energy Transfer Platform to Monitor Protein-Protein
Interactions in Live Cells

Xiu-Lei Mo and Haian Fu

18. Application of Imaging-Based
Assays in Microplate Formats for High Content Screening

Adam I. Fogel, Scott E. Martin, and
Samuel A. Hasson