1st Edition

Handbook of Assay Development in Drug Discovery

Edited By Lisa K. Minor Copyright 2006
    482 Pages 226 B/W Illustrations
    by CRC Press

    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

    “To be as advanced as possible, Dr. Minor has had individual chapters written by experts from equipment vendors (GE, PerkinElmer); pharmaceutical companies (J&J, Merck, Lilly), government (NIH) and more. These individual chapters describe in practical terms what these organizations have developed.”