Handbook of Assay Development in Drug Discovery

The Handbook of Assay Development in Drug Discovery describes all the tools currently available for performing various assay techniques. Featuring troubleshooting advice for common problems from experienced assay developers, the vendor community, and scientists in the pharmaceutical industry, the book presents descriptions of methods, laboratory guidelines and protocols used to perform such methods, specific examples of each assay system, and troubleshooting tools. Designed as a guide to running an assay from start to finish, this is an ideal bench top companion for scientists involved in drug discovery screening, lead profiling, therapeutic target evaluation, and assay development and implementation.

The need to screen targets faster and more efficiently, coupled with advances in parallel and multiplex chemical synthesis, has contributed to the increasing use of multiwell assays for drug discovery. The Handbook of Assay Development in Drug Discovery is a reference that describes the complete armament of tools currently available for performing various assay techniques. Featuring contributions from assay developers in the pharmaceutical and vendor communities, the book presents descriptions of methods, laboratory guidelines and protocols used to perform such methods, specific examples of each assay system, and troubleshooting tools. The handbook describes biochemical assay classes as well as non-class specific assay development for cell-based assays. It covers a wide range of target classes—including kinases, proteases, nuclear receptors, and GPCRs—and describes currently employed methods and assay types, such as radioligand binding assays, image analysis assays, enzyme fragment complementation, and bioluminescent and fluorescent-based assays. Designed as a guide to running an assay from start to finish, the Handbook of Assay Development in Drug Discovery is an ideal bench top companion for discovery researchers, laboratory managers, academics, and other scientists involved in drug discovery screening, lead profiling, therapeutic target evaluation, and assay development and implementation in the pharmaceutical and biotechnology industries. Daniel E. Levy, editor of the Drug Discovery Series, is the founder of DEL BioPharma, a consulting service for drug discovery programs. He also maintains a blog that explores organic chemistry.

Protein Kinases in Drug Discovery: Rationale, Success, and Challenge; Dana L. Johnson and Jan L. Sechler An Introduction to the Protein Tyrosine Phosphatase Gene Family and Screening Assay Development; Dominique Perrin and Rob Hooft van Huijsduijnen Time-Resolved Fluorescence Based Assays for Kinases; Zhuyin Li and Tina Garyantes Development of High-throughput Screening Assays in Scintillating Microplates (FlashPlates) to Identify Inhibitors of Kinase Activity; Stewart Emanual Development of High-Throughput Screening Assays for Kinase Drug Targets using AlphaScreen™ Technology; D. Wenham, C. Illy, J.A. St. Pierre, and N. Bouchard Homogeneous High-Throughput Screening (HTS) Assays for Serine/Threonine Kinases Using ß-Galactosidase Enzyme Fragment Complementation; I. Vainshtein, T. Naqvi, A. Lim, R. Rouhani, L. Kauffman, R. Singh, and R.M. Eglen IMAP Assays for Assaying Protein Kinases; R. Sportsman A Homogenous, Luminescent, High-Throughput, Versatile Assay for a Wide Range of Kinases; S.A. Goueli, K. Hsiao, and B. Bulleit Proteases as Drug Targets; R.L. Thurmond and J.P. Edwards A Comparison of Homogeneous Bioluminescent and Fluorescent Methods for Protease Assays; M. O’Brien Scintillation Proximity Assay (SPA) Receptor Binding Assays; J.R. Cook, R. Graves, K. Lowitz, M.J. Price-Jones, J.A. Berry and K.T. Hughes Radioligand Binding Filtration Assay: Full Automation; S.K.F. Wong Nuclear Receptors As Drug Targets; P.D. Pelton Nuclear Receptor Scintillation Proximity Assays; D. Powell and M.J. Price-Jones Homogenous Assay Development for Nuclear Receptor Using the AlphaScreen Technology; N. Rouleau and R. Bossé Development of Nuclear Receptor Homogenous Assay Using the Lance Technology; N. Rouleau, P. Hurskainen, I. Hemmilä and R. Bossé The Emerging Role of Cell-based Assays in Discovery; R. Garippa The Preparation of Cells for High-Content Screening; A. Hoffman The Evolution of cAMP Assays; P. Kasila and H. Harney A Homogenous Fluorescent Polariaiton assay for Inositol 1,4,5-Trisphoshpate (Ins P3); P. Fung, R. Singh, L. Kauffman, R.M. Eglen and T. Naqvi Scintillation Proximity Assay of Inositol Phosphates; W. Zheng and P. Brandish Measuring Calcium Mobilization with Gq-Coupled GPCRs Using the Fluorometric Imaging Plate Reader (FLIPR); J. Dunlop, Y. Zhang, R. Ring and D. Kowal Development of FLIPR-Based HTS Assay for Gi-Coupled GPCRs; C. Chen, C. Smith, L. Minor, and B. Damiano Aurora Assays; P, Kunapuli Membrane Potential Based Assays for Ion Channels and Electrogenic Transporters; Q, Lü, S, Lin, and J, Dunlop Reporter Gene Assays for Drug Discovery; K.A. Houck, W.P. Bocchinfuso, M.S. Dowless, and K.M. Borchert mRNA Detection from Cells Using Quantigene® Branched DNA Technology; L. Minor Homogeneous Miltiwell Assays for Measuring Cell Viability, Cytotoxicity and Apoptosis; Terry Riss, R.A. Moravec, M.A. O’Brien, E.M. Hawkins, and A. Niles Development of Image-Bases Assays for Drug Discovery; S.M. Catalano GPCR Internalization Measured by Image Analysis; R. Graves, M.J. Francis, L. Smith, J.R. Cook, and E.J. Adie TRANSFLUOR®, a Universal Cell-Based Assay for Screening G-Protein Coupled Receptors; R. Oakley C.L. Cowan, C.C. Hudson, and C.R. Loomis

Lisa K. Minor