Troubleshooting and deconvoluting label-free cell phenotypic assays in drug discovery. (Q46013288)

18 December 2017

title

Troubleshooting and deconvoluting label-free cell phenotypic assays in drug discovery. (English)

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18 December 2017

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1

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18 December 2017

publication date

20 January 2013

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18 December 2017

Journal of Pharmacological and Toxicological Methods

published in

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18 December 2017

volume

67

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18 December 2017

issue

2

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18 December 2017

page(s)

69-81

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18 December 2017

Lipid raft microdomains and neurotransmitter signalling

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Cell death assays for drug discovery

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Biased signaling pathways in β2-adrenergic receptor characterized by 19F-NMR.

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Kinetics of G-protein-coupled receptor signals in intact cells

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GPR35 as a Novel Therapeutic Target.

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Zebrafish-Based Small Molecule Discovery

7 January 2021

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A novel, conformation-specific allosteric inhibitor of the tachykinin NK2 receptor (NK2R) with functionally selective properties

7 January 2021

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GPCR functional selectivity has therapeutic impact

7 January 2021

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Functional selectivity of G protein signaling by agonist peptides and thrombin for the protease-activated receptor-1.

7 January 2021

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Mechanisms of cell death in rhodopsin retinitis pigmentosa: implications for therapy

7 January 2021

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Rational approaches to targeted polypharmacology: creating and navigating protein-ligand interaction networks

7 January 2021

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Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target

7 January 2021

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The relative activity of "function sparing" HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property?

7 January 2021

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Lessons from 60 years of pharmaceutical innovation

7 January 2021

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Review article: cellular and molecular mechanisms of NSAID-induced peptic ulcers

7 January 2021

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The alpha1L-adrenoceptor is an alternative phenotype of the alpha1A-adrenoceptor

7 January 2021

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"Phenotypic" pharmacology: the influence of cellular environment on G protein-coupled receptor antagonist and inverse agonist pharmacology.

7 January 2021

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International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative pharmacology

7 January 2021

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Molecular basis of partial agonism at the neurotransmitter alpha2A-adrenergic receptor and Gi-protein heterotrimer

7 January 2021

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Target-drug interactions: first principles and their application to drug discovery

7 January 2021

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A comprehensive pathway map of epidermal growth factor receptor signaling

7 January 2021

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Advanced dynamic monitoring of cellular status using label-free and non-invasive cell-based sensing technology for the prediction of anticancer drug efficacy

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Where have all the active receptor states gone?

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How many drug targets are there?

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Dynamic mass redistribution assay decodes differentiation of a neural progenitor stem cell

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The productivity crisis in pharmaceutical R&D.

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A series of case studies: practical methodology for identifying antinociceptive multi-target drugs

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A cell-based impedance assay for monitoring transient receptor potential (TRP) ion channel activity.

7 January 2021

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Global mapping of pharmacological space

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Ensemble of G protein-coupled receptor active states

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How to improve R&D productivity: the pharmaceutical industry's grand challenge

7 January 2021

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Evaluating cellular impedance assays for detection of GPCR pleiotropic signaling and functional selectivity

7 January 2021

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Comparing label-free biosensors for pharmacological screening with cell-based functional assays.

7 January 2021

1 reference

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Computational polypharmacology with text mining and ontologies

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Advancing schizophrenia drug discovery: optimizing rodent models to bridge the translational gap.

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Unveiling the role of network and systems biology in drug discovery

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Morphine side effects in beta-arrestin 2 knockout mice

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Teaching old receptors new tricks: biasing seven-transmembrane receptors

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Kinetics of adhesion and spreading of animal cells

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Trends in the exploitation of novel drug targets

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

7TM pharmacology measured by label-free: a holistic approach to cell signalling

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

The structure and function of G-protein-coupled receptors

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Targeting and tinkering with interaction networks

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Single-molecule imaging of EGFR signalling on the surface of living cells

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Cardiac GPCRs: GPCR signaling in healthy and failing hearts

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Deciphering biased-agonism complexity reveals a new active AT1 receptor entity.

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Diagnosing the decline in pharmaceutical R&D efficiency

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

A network view of disease and compound screening

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements.

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells.

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Label-free whole-cell assays: expanding the scope of GPCR screening

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Functional selectivity of GPCR ligand stereoisomers: new pharmacological opportunities

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity.

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Impedance responses reveal β₂-adrenergic receptor signaling pluridimensionality and allow classification of ligands with distinct signaling profiles

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Retinal dynamics underlie its switch from inverse agonist to agonist during rhodopsin activation

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Applying surface plasmon resonance to monitor the IgE-mediated activation of human basophils

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Probing the beta2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Sequential binding of agonists to the beta2 adrenoceptor. Kinetic evidence for intermediate conformational states

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Biochemical mechanisms of drug action: what does it take for success?

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

How were new medicines discovered?

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Surface plasmon resonance biosensor detects the downstream events of active PKCbeta in antigen-stimulated mast cells

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Duplexed label-free G protein--coupled receptor assays for high-throughput screening

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Label-free optical biosensor for probing integrative role of adenylyl cyclase in G protein-coupled receptor signaling

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Dynamic mass redistribution assays decode surface influence on signaling of endogenous purinergic P2Y receptors.

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Functional Selectivity and Classical Concepts of Quantitative Pharmacology

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Cellular dielectric spectroscopy: a label-free comprehensive platform for functional evaluation of endogenous receptors

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

GPCRs regulate the assembly of a multienzyme complex for purine biosynthesis.

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

beta-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

The use of stimulus-biased assay systems to detect agonist-specific receptor active states: implications for the trafficking of receptor stimulus by agonists.

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Multitargeted drugs: the end of the "one-target-one-disease" philosophy?

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Mammalian G proteins and their cell type specific functions

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Computational modeling of the EGF-receptor system: a paradigm for systems biology

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

DrugBank: a comprehensive resource for in silico drug discovery and exploration

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Development of a label-free assay for sodium-dependent phosphate transporter NaPi-IIb.

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Stereochemistry of an agonist determines coupling preference of beta2-adrenoceptor to different G proteins in cardiomyocytes

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

BioGPS: an extensible and customizable portal for querying and organizing gene annotation resources

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Aspirin: old drug, new uses and challenges

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Integrating high-content screening and ligand-target prediction to identify mechanism of action

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Real-time monitoring of morphological changes in living cells by electronic cell sensor arrays: an approach to study G protein-coupled receptors

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

High-quality binary protein interaction map of the yeast interactome network

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Knockouts model the 100 best-selling drugs--will they model the next 100?

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Systems pharmacology: network analysis to identify multiscale mechanisms of drug action

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

Network-Based Relating Pharmacological and Genomic Spaces for Drug Target Identification

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

The analysis of the drug-targets based on the topological properties in the human protein-protein interaction network

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

In vivo drug discovery in the zebrafish

7 January 2021

1 reference

https://api.crossref.org/works/10.1016%2FJ.VASCN.2013.01.004

10.1016/J.VASCN.2013.01.004

7 January 2021

Identifiers

DOI

1 reference

18 December 2017

1 reference

18 December 2017