Book contents
- Frontmatter
- Contents
- List of Figures
- List of Tables
- List of Contributors
- Introduction
- PART I ADVANCES IN GPCR PROTEIN RESEARCH
- PART II OLIGOMERIZATION OF GPCRS
- PART III GPCR SIGNALING FEATURES
- 7 G protein functions identified using genetic mouse models
- 8 Kinetics of GPCR, G protein, and effector activation
- 9 RGS-RhoGEFs and other RGS multidomain proteins as effector molecules in GPCR-dependent and GPCR-independent cell signaling
- 10 Adenylyl cyclase isoform-specific signaling of GPCRs
- 11 G protein-independent and β arrestin-dependent GPCR signaling
- 12 Assays to read GPCR modulation and signaling
- PART IV LIGAND PHARMACOLOGY OF GPCRS
- PART V PHYSIOLOGICAL FUNCTIONS AND DRUG TARGETING OF GPCRS
- Index
- References
12 - Assays to read GPCR modulation and signaling
from PART III - GPCR SIGNALING FEATURES
Published online by Cambridge University Press: 05 June 2012
Book contents
- Frontmatter
- Contents
- List of Figures
- List of Tables
- List of Contributors
- Introduction
- PART I ADVANCES IN GPCR PROTEIN RESEARCH
- PART II OLIGOMERIZATION OF GPCRS
- PART III GPCR SIGNALING FEATURES
- 7 G protein functions identified using genetic mouse models
- 8 Kinetics of GPCR, G protein, and effector activation
- 9 RGS-RhoGEFs and other RGS multidomain proteins as effector molecules in GPCR-dependent and GPCR-independent cell signaling
- 10 Adenylyl cyclase isoform-specific signaling of GPCRs
- 11 G protein-independent and β arrestin-dependent GPCR signaling
- 12 Assays to read GPCR modulation and signaling
- PART IV LIGAND PHARMACOLOGY OF GPCRS
- PART V PHYSIOLOGICAL FUNCTIONS AND DRUG TARGETING OF GPCRS
- Index
- References
Summary
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- Chapter
- Information
- G Protein-Coupled ReceptorsStructure, Signaling, and Physiology, pp. 231 - 246Publisher: Cambridge University PressPrint publication year: 2010
References
, , , and (2006). The 7 TM G-protein-coupled receptor target family. ChemMedChem. 1, 761–782.CrossRefGoogle ScholarPubMed
, , , and (1989). Na+ regulation of formyl peptide receptor-mediated signal transduction in HL 60 cells. Evidence that the cation prevents activation of the G-protein by unoccupied receptors. Eur. J. Pharmacol. 172, 481–492.CrossRefGoogle ScholarPubMed
and (1989). Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. U. S. A 86, 7321–7325.CrossRefGoogle ScholarPubMed
and (2006). Inverse agonism or neutral antagonism at G-protein coupled receptors: a medicinal chemistry challenge worth pursuing?Eur. J. Pharmacol. 553, 1–9.CrossRefGoogle ScholarPubMed
, , , , , , , , , , , and (2002). Differential in vivo effects of H3 receptor ligands in a new mouse dipsogenia model. Pharmacol. Biochem. Behav. 72, 741–750.CrossRefGoogle Scholar
, , , and (1999). Effect of 5-HT2 receptor antagonists on a cranial nerve reflex in the rabbit: evidence for inverse agonism. Psychopharmacology (Berl) 141, 162–168.CrossRefGoogle ScholarPubMed
, , , and (2001). Constitutive activity of the human beta(1)-adrenergic receptor in beta(1)-receptor transgenic mice. Mol. Pharmacol. 60, 712–717.Google ScholarPubMed
, , , , , and (2008). {beta}-Arrestin-biased Agonism at the {beta}2-Adrenergic Receptor. J. Biol. Chem. 283, 5669–5676.CrossRefGoogle Scholar
, , , , and (2002b). Comparison of photomultiplier tube- and charge coupled device-based scintillation counting. Life Science News 11, 1–3.Google Scholar
(1999). Imaging systems in assay screening. Drug Discov. Today 4, 401–410.CrossRefGoogle ScholarPubMed
(2003). Principles: extending the utility of [35S]GTP gamma S binding assays. Trends Pharmacol. Sci. 24, 87–90.CrossRefGoogle Scholar
, , , , , , , , , , , , , and (2008). Identification of a serotonin/glutamate receptor complex implicated in psychosis. Nature 452, 93–97.CrossRefGoogle ScholarPubMed
, , , , , , , , and (2005). GPCR screening via ERK 1/2: a novel platform for screening G protein-coupled receptors. J. Biomol. Screen. 10, 730–737.CrossRefGoogle ScholarPubMed
, , and (1999). Measurement of [Ca2+] using the Fluorometric Imaging Plate Reader (FLIPR). Methods Mol. Biol. 114, 125–133.Google Scholar
and (2002). Considerations for using fluorescence polarization in the screening of g protein-coupled receptors. J. Biomol. Screen. 7, 111–117.CrossRefGoogle ScholarPubMed
, , , and (2008). Activation and Translocation of Glucokinase in Rat Primary Hepatocytes Monitored by High Content Image Analysis. J. Biomol. Screen. 13, 837–46.CrossRefGoogle ScholarPubMed
and (2006). Deorphanization of G-protein-coupled receptors. Ernst Schering Found. Symp. Proc. 2, 163–186.Google Scholar
, , , and (2002a). Automated high throughput screening for serine kinase inhibitors using a LEADseeker scintillation proximity assay in the 1536-well format. J. Biomol. Screen. 7, 11–19.CrossRefGoogle ScholarPubMed
and (2002). Automated high-throughput screening. European Pharmaceutical Review 3, 25–35.Google Scholar
, , , and (2003). Miniaturization of fluorescence polarization receptor-binding assays using CyDye-labeled ligands. J. Biomol. Screen. 8, 410–420.CrossRefGoogle Scholar
, , and (2000). Macroscopic versus microscopic fluorescence techniques in (ultra)-high-throughput screening. Drug Discov. Today HTS Suppl 1, 3–9.CrossRefGoogle Scholar
, , , , , and (1998). Fluorescence correlation spectroscopy: lead discovery by miniaturized HTS. Drug Discov. Today 3, 457–465.Google Scholar
, , , , and (2003). Confocal optics microscopy for biochemical and cellular high-throughput screening. Drug Discov. Today 8, 1085–1093.Google ScholarPubMed
(2008). Cell-based assays in GPCR drug discovery. Biotechnol. J. 3, 471–483.CrossRefGoogle ScholarPubMed
, , , and (2005). Confocal fluorescence microscopy for high-throughput screening of G-protein coupled receptors. Current Medicinal Chemistry 12, 2551–2559.CrossRefGoogle ScholarPubMed
, , , , , , , , , and (2006). beta-arrestin-dependent, G protein-independent ERK1/2 activation by the beta2 adrenergic receptor. J. Biol. Chem. 281, 1261–1273.CrossRefGoogle Scholar
, , , , , , and (2003). Insights into G protein structure, function, and regulation. Endocr. Rev. 24, 765–781.CrossRefGoogle ScholarPubMed
, , , , and (2001). Molecular determinants underlying the formation of stable intracellular G protein-coupled receptor-beta-arrestin complexes after receptor endocytosis*. J. Biol. Chem. 276, 19452–19460.CrossRefGoogle Scholar
, , , and (2008). Reversible translocation of p115-RhoGEF by G(12/13)-coupled receptors. J. Cell Biochem. 104, 1660–1670.CrossRefGoogle Scholar
(2004). The antibody-capture [(35)S]GTPgammaS scintillation proximity assay: a powerful emerging technique for analysis of GPCR pharmacology. Trends Pharmacol. Sci. 25, 400–401.CrossRefGoogle ScholarPubMed
, , and (2005). Techniques: Promiscuous Galpha proteins in basic research and drug discovery. Trends Pharmacol. Sci. 26, 595–602.CrossRefGoogle ScholarPubMed
(2008). Signaling mechanisms of GPCR ligands. Curr. Opin. Drug Discov. Devel. 11, 196–202.Google ScholarPubMed
, , , , and (2002). Aequorin-based functional assays for G-protein-coupled receptors, ion channels, and tyrosine kinase receptors. Receptors. Channels 8, 319–330.CrossRefGoogle ScholarPubMed
, , , , , and (2003). High throughput screening technologies for direct cyclic AMP measurement. Assay Drug Dev. Technol. 1, 291–303.CrossRefGoogle ScholarPubMed
, , and (2001). Reporter-gene systems for the study of G-protein-coupled receptors. Curr. Opin. Pharmacol. 1, 526–532.CrossRefGoogle Scholar
(1993). Inositol trisphosphate and calcium signalling. Nature 361, 315–325.CrossRefGoogle ScholarPubMed
(2003). G-proteins as transducers in transmembrane signalling. Prog. Biophys. Mol. Biol. 83, 101–130.CrossRefGoogle ScholarPubMed
, , , , , , , and (2010). High content screening of CXCR2-dependent signalling pathways. Comb. Chem. High Throughput Screen. 13, 3–15.CrossRefGoogle ScholarPubMed
(1998). G protein-coupled receptors. III. New roles for receptor kinases and beta-arrestins in receptor signaling and desensitization. J. Biol. Chem. 273, 18677–18680.CrossRefGoogle ScholarPubMed
, , , , , , , , , , , , , , , , , and (2007). Nicotinic acid receptor agonists differentially activate downstream effectors. J. Biol. Chem. 282, 18028–18036.CrossRefGoogle ScholarPubMed
(2005). Functional G protein-coupled receptor assays for primary and secondary screening. Comb. Chem. High Throughput Screen. 8, 311–318.CrossRefGoogle ScholarPubMed
(2008). Microscopic imaging techniques for drug discovery. Nat. Rev. Drug Discov. 7, 54–67.CrossRefGoogle ScholarPubMed
and (2007). A pharmaceutical company user's perspective on the potential of high content screening in drug discovery. Methods Mol. Biol. 356, 19–31.Google ScholarPubMed
, , , and (2006). Systems cell biology based on high-content screening. Methods Enzymol. 414, 601–619.CrossRefGoogle ScholarPubMed
, , , , , , , , , and (2006). Automated High Content Screening for phosphoinositide 3 kinase inhibition using an AKT1 redistribution assay. Comb. Chem. High Throughput Screen. 9, 339–350.CrossRefGoogle ScholarPubMed
, , and (2006). Orphan seven transmembrane receptor screening. Ernst Schering Found. Symp. Proc. 105–143.Google Scholar
, , , and (2009). G-protein-coupled receptor-focused drug discovery using a target class platform approach. Drug Discov. Today 14, 231–40.CrossRefGoogle ScholarPubMed
(2006). High Content Screening to monitor G-protein coupled receptor internalisation. Ernst Schering Foundation Symposium Proceedings 2, 229–248.Google Scholar
, , , and (2006). G protein-coupled receptor internalization assays in the high-content screening format. Methods Enzymol. 414, 121–139.CrossRefGoogle ScholarPubMed
, , , , , and (2008). Pharmacological profiling of chemokine receptor-directed compounds using high-content screening. J. Biomol. Screen. 13, 40–53.CrossRefGoogle ScholarPubMed
(2001). Evolving concepts in G protein-coupled receptor endocytosis: the role in receptor desensitization and signaling. Pharmacol. Rev. 53, 1–24.Google Scholar
(2004). G protein-coupled receptor dimerization: function and ligand pharmacology. Mol. Pharmacol. 2004. Jul.;66. (1):1–7. 66, 1–7.CrossRefGoogle ScholarPubMed
, , , , , , and (2002). The cellular distribution of fluorescently labeled arrestins provides a robust, sensitive, and universal assay for screening of G protein-coupled receptors. Assay Drug Dev. Technol. 1, 21–30.CrossRefGoogle ScholarPubMed
, , , , , , , and (2009). CXCR2 inverse agonism detected by arrestin redistribution. J. Biomol. Screen. 14, 1076–91.CrossRefGoogle ScholarPubMed
, , and (2001). The biological functions of A-kinase anchor proteins. J. Mol. Biol. 308, 99–114.CrossRefGoogle ScholarPubMed
and (2005). Transduction of receptor signals by beta-arrestins. Science 308, 512–517.CrossRefGoogle ScholarPubMed
, , and (2008). Label-free cell-based assays for GPCR screening. Comb. Chem. High Throughput Screen. 11, 357–369.CrossRefGoogle Scholar
, , , , and (2005). High-throughput screening of interactions between G protein-coupled receptors and ligands using confocal optics microscopy. Methods Mol. Biol. 305, 365–384.Google ScholarPubMed