An update of novel screening methods for GPCR in drug discovery (Q38020237)

27 August 2017

title

An update of novel screening methods for GPCR in drug discovery (English)

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G protein-coupled receptor

27 August 2017

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Linjie Chen

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27 August 2017

Lili Jin

series ordinal

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27 August 2017

Naiming Zhou

series ordinal

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27 August 2017

language of work or name

English

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publication date

21 June 2012

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Expert Opinion on Drug Discovery

27 August 2017

published in

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27 August 2017

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27 August 2017

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27 August 2017

page(s)

791-806

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The G protein-coupled receptor repertoires of human and mouse

27 August 2017

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Decoding the signaling of a GPCR heteromeric complex reveals a unifying mechanism of action of antipsychotic drugs.

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Prime time for G-protein-coupled receptor heteromers as therapeutic targets for CNS disorders: the dopamine D₁-D₃ receptor heteromer

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Effects of calcium on ACTH stimulation of the adrenal: separation of hormone binding from adenyl cyclase activation

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Use of red-shifted dyes in a fluorescence polarization AKT kinase assay for detection of biological activity in natural product extracts

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6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.

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Kinetics of G-protein-coupled receptor endosomal trafficking pathways revealed by single quantum dots

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Fluorescence polarization assays in small molecule screening

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Fluorescence polarization/anisotropy in diagnostics and imaging

21 January 2018

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Fluorescence polarization screening for allosteric small molecule ligands of the cholecystokinin receptor

21 January 2018

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Novel Alexa Fluor-488 labeled antagonist of the A(2A) adenosine receptor: Application to a fluorescence polarization-based receptor binding assay

21 January 2018

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A general method for the covalent labeling of fusion proteins with small molecules in vivo

21 January 2018

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An engineered protein tag for multiprotein labeling in living cells

21 January 2018

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HaloTag: a novel protein labeling technology for cell imaging and protein analysis

21 January 2018

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A Fluorescent Ligand-Binding Alternative Using Tag-lite® Technology

21 January 2018

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Drugability of extracellular targets: discovery of small molecule drugs targeting allosteric, functional, and subunit-selective sites on GPCRs and ion channels

21 January 2018

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Allosteric modulators of g protein-coupled receptors: future therapeutics for complex physiological disorders.

21 January 2018

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Emerging role of surface plasmon resonance in fragment-based drug discovery.

21 January 2018

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Screening for GPCR Ligands Using Surface Plasmon Resonance

21 January 2018

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Fragment screening of stabilized G-protein-coupled receptors using biophysical methods

21 January 2018

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A fully automated [35S]GTPgammaS scintillation proximity assay for the high-throughput screening of Gi-linked G protein-coupled receptors

21 January 2018

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21 January 2018

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21 January 2018

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A time-resolved fluorescent lanthanide (Eu)-GTP binding assay for chemokine receptors as targets in drug discovery.

21 January 2018

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Photoproteins: important new tools in drug discovery

21 January 2018

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Development of a Ca(2+)-activated photoprotein, Photina, and its application to high-throughput screening

21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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Comparison on functional assays for Gq-coupled GPCRs by measuring inositol monophospate-1 and intracellular calcium in 1536-well plate format

21 January 2018

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21 January 2018

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21 January 2018

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Application of the BD ACTOne technology for the high-throughput screening of Gs-coupled receptor antagonists.

21 January 2018

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Development of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay

21 January 2018

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Innovative functional cAMP assay for studying G protein-coupled receptors: application to the pharmacological characterization of GPR17.

21 January 2018

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Novel single chain cAMP sensors for receptor-induced signal propagation.

21 January 2018

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Novel genetically encoded biosensors using firefly luciferase

21 January 2018

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The oxytocin receptor antagonist atosiban inhibits cell growth via a "biased agonist" mechanism

21 January 2018

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Pertussis toxin-sensitive signaling of melanocortin-4 receptors in hypothalamic GT1-7 cells defines agouti-related protein as a biased agonist

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Teaching old receptors new tricks: biasing seven-transmembrane receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

A beta-arrestin-biased agonist of the parathyroid hormone receptor (PTH1R) promotes bone formation independent of G protein activation.

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

The evasive nature of drug efficacy: implications for drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

The role of conformational ensembles of seven transmembrane receptors in functional selectivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Heterodimerization of the GABAB receptor-implications for GPCR signaling and drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Heteromerization of G protein-coupled receptors: relevance to neurological disorders and neurotherapeutics

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

G protein-coupled receptor sorting to endosomes and lysosomes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Transduction of receptor signals by beta-arrestins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Nicotinic acid receptor agonists differentially activate downstream effectors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

The BRET2/arrestin assay in stable recombinant cells: a platform to screen for compounds that interact with G protein-coupled receptors (GPCRS).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

High-throughput screening of G protein-coupled receptor antagonists using a bioluminescence resonance energy transfer 1-based beta-arrestin2 recruitment assay

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Improved donor/acceptor BRET couples for monitoring beta-arrestin recruitment to G protein-coupled receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Development of a BRET2 screening assay using beta-arrestin 2 mutants

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Phosphorylation of the delta-opioid receptor regulates its beta-arrestins selectivity and subsequent receptor internalization and adenylyl cyclase desensitization

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Recruitment of beta-arrestin2 to the dopamine D2 receptor: insights into anti-psychotic and anti-parkinsonian drug receptor signaling.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Antagonism of dopamine D2 receptor/beta-arrestin 2 interaction is a common property of clinically effective antipsychotics.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Beta galactosidase complementation: a cell-based luminescent assay platform for drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

beta-Arrestin recruitment assay for the identification of agonists of the sphingosine 1-phosphate receptor EDG1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

The genetic design of signaling cascades to record receptor activation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Utilization of the Tango beta-arrestin recruitment technology for cell-based EDG receptor assay development and interrogation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Kappa opioid receptor screen with the Tango beta-arrestin recruitment technology and characterization of hits with second-messenger assays

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Studying G protein-coupled receptor activation using split-tobacco etch virus assays.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Monitoring regulated protein-protein interactions using split TEV

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Development of a novel DnaE intein-based assay for quantitative analysis of G-protein-coupled receptor internalization.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

High-throughput sensing and noninvasive imaging of protein nuclear transport by using reconstitution of split Renilla luciferase

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

A high-content subtractive screen for selecting small molecules affecting internalization of GPCRs

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

High-Content Analysis of CCR2 Antagonists on Human Primary Monocytes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Multiplexed assays by high-content imaging for assessment of GPCR activity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

High-throughput analysis of ligand-induced internalization of β2-adrenoceptors using the coiled-coil tag-probe method

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Cell-based assays in GPCR drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Lessons from 60 years of pharmaceutical innovation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

How were new medicines discovered?

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Primary cells and stem cells in drug discovery: emerging tools for high-throughput screening

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

The use of immortalized cell lines in GPCR screening: the good, bad and ugly.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Using label-free screening technology to improve efficiency in drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

The development of label-free cellular assays for drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Insider access: pepducin symposium explores a new approach to GPCR modulation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Direct interaction between an allosteric agonist pepducin and the chemokine receptor CXCR4.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

G protein-coupled receptor modulation with pepducins: moving closer to the clinic

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

Highly efficient proteintrans-splicing by a naturally split DnaE intein fromNostoc punctiforme

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.699036

10.1517/17460441.2012.699036

21 January 2018

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DOI

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27 August 2017

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