G protein-coupled receptors in drug discovery / edited by Wayne R. Leifert. — Dordrecht : Humana, c2009. – (58.17/M592/v.552)

Contents

    Contents
    Preface Contributors
    1 New Insights into GPCR Function: Implications for HTS
    2 Screening Technologies for G Protein-Coupled Receptors: From HTS to uHTS
    3 GPCR Signaling: Understanding the Pathway to Successful Drug Discovery
    4 An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs
    5 Understanding the Ligand-Receptor-G Protein Ternary Complex for GPCR Drug Discovery
    6 Assay Data Quality Assessment
    7 Homology Modeling of GPCRs
    8 GPCR Expression Using Baculovirus-Infected $3a9 Cells
    9 Radioligand Binding Assays: Application of [125I] Angiotensin II Receptor Binding
    10 [35S]GTPγS Binding in G Protein-Coupled Receptor Assays
    11 A Time-Resolved Fluorescent Lanthanide (Eu)-GTP Binding Assay for Chemokine Receptors as Targets in Drug Discovery
    12 Use of the DiscoveRx Hithunter cAMPII Assay for Direct Measurement of cAMP in Gs and Gi GPCRs
    13 Use of Aequorin for G protein-Coupled Receptor Hit Identification and Compound Profiling
    14 BacMam: Versatile Gene Delivery Technology for GPCR Assays
    15 Yeast Assays for G Protein-Coupled Receptors
    16 GPCR Microspot Assays on Solid Substrates
    17 Resonant Waveguide Grating Biosensor for Whole-Cell GPCR Assays 239
    18 FRET-Based Measurement of GPCR Conformational Changes
    19 FLIPR Assays of lntracellular Calcium in GPCR Drug Discovery
    20 Use of Fluorescence Indicators in Receptor Ligands
    21 Application of Fluorescence Resonance Energy Transfer Techniques to Establish Ligand-Receptor Orientation
    22 Detection of GPCR/β-Arresdn Interactions in Live Cells Using Bioluminescence Resonance Energy Transfer Technology
    23 Using Reporter Gene Technologies to Detect Changes in cAMP as a Result of GPCR Activation
    24 A Quantum Dot-Labeled Ligand-Receptor Binding Assay for G Protein-Coupled Receptors Contained in Minimally Purified Membrane Nanopatches
    25 Xenopus Oocyte Electrophysiology in GPCR Drug Discovery
    26 Immunoprecipitation and Phosphorylation of G Protein-Coupled Receptors
    Index