Handbook of Assay Development in Drug Discovery is a reference that describes the complete armament of tools currently available for performing various assay techniques.

Features:

• Contains detailed protocols of assay methodologies that facilitate setting up specific assays
• Utilizes examples that illustrate the use of a particular assay methodology in context and demonstrate how the data should appear
• Features troubleshooting advice for common problems from experienced assay developers and scientists in the pharmaceutical industry
• Dedicates several chapters to the development of reporter assays, mRNA detection assays, and assays for cell viability, cytotoxicity, and apoptosis
• Includes GPCR assays for signal transduction molecules and image analysis assays for receptor internalization and arrestin translocation

Contents

1. Protein Kinases in Drug Discovery: Rationale, Success, and Challenge
2. An Introduction to the Protein Tyrosine Phosphatase Gene Family and Screening Assay Development
3. Time-Resolved Fluorescence Based Assays for Kinases
4. Development of High-throughput Screening Assays in Scintillating Microplates (FlashPlates) to Identify Inhibitors of Kinase Activity
5. Development of High-Throughput Screening Assays for Kinase Drug Targets using AlphaScreen™ Technology
6. Homogeneous High-Throughput Screening (HTS) Assays for Serine/Threonine Kinases Using ß-Galactosidase Enzyme Fragment Complementation
7. IMAP Assays for Assaying Protein Kinases
8. A Homogenous, Luminescent, High-Throughput, Versatile Assay for a Wide Range of Kinases
9. Proteases as Drug Targets
10. A Comparison of Homogeneous Bioluminescent and Fluorescent Methods for Protease Assays
11. Scintillation Proximity Assay (SPA) Receptor Binding Assays
12. Radioligand Binding Filtration Assay: Full Automation
13. Nuclear Receptors As Drug Targets
14. Nuclear Receptor Scintillation Proximity Assays
15. Homogenous Assay Development for Nuclear Receptor Using the AlphaScreen Technology
16. Development of Nuclear Receptor Homogenous Assay Using the Lance Technology
17. The Emerging Role of Cell-based Assays in Discovery
18. The Preparation of Cells for High-Content Screening
19. The Evolution of cAMP Assays
20. A Homogenous Fluorescent Polariaiton assay for Inositol 1,4,5-Trisphoshpate (Ins P3)
21. Scintillation Proximity Assay of Inositol Phosphates
22. Measuring Calcium Mobilization with Gq-Coupled GPCRs Using the Fluorometric Imaging Plate Reader (FLIPR)
23. Development of FLIPR-Based HTS Assay for Gi-Coupled GPCRs
24. Aurora Assays
25. Membrane Potential Based Assays for Ion Channels and Electrogenic Transporters
26. Reporter Gene Assays for Drug Discovery
27. mRNA Detection from Cells Using Quantigene® Branched DNA Technology
28. Homogeneous Miltiwell Assays for Measuring Cell Viability, Cytotoxicity and Apoptosis
29. Development of Image-Bases Assays for Drug Discovery
30. GPCR Internalization Measured by Image Analysis
31. TRANSFLUOR®, a Universal Cell-Based Assay for Screening G-Protein Coupled Receptors

Index

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