Cellular assays as portals to seven-transmembrane receptor-based drug discovery (Q37553926)

21 August 2017

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title

Cellular assays as portals to seven-transmembrane receptor-based drug discovery (English)

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21 August 2017

main subject

transmembrane protein

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Terry P Kenakin

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21 August 2017

publication date

17 July 2009

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Nature Reviews Drug Discovery

21 August 2017

published in

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21 August 2017

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21 August 2017

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21 August 2017

page(s)

617-626

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Comparison of some properties of pronethalol and propranolol

21 August 2017

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A statistical thermodynamic model of the protein ensemble

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Agonist efficacy and allosteric models of receptor action.

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The ligand paradox between affinity and efficacy: can you be there and not make a difference?

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Efficacy at G-protein-coupled receptors

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Fluorescent labeling of purified beta 2 adrenergic receptor. Evidence for ligand-specific conformational changes

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Functionally different agonists induce distinct conformations in the G protein coupling domain of the beta 2 adrenergic receptor

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Plasmon-waveguide resonance (PWR) spectroscopy for directly viewing rates of GPCR/G-protein interactions and quantifying affinities

31 March 2020

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The neurokinin A receptor activates calcium and cAMP responses through distinct conformational states

31 March 2020

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

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Transduction of receptor signals by beta-arrestins

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Regulation of alpha2AR trafficking and signaling by interacting proteins

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GPCR functional selectivity has therapeutic impact

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Collateral efficacy in drug discovery: taking advantage of the good (allosteric) nature of 7TM receptors

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31 March 2020

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

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Measuring intracellular calcium fluxes in high throughput mode

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31 March 2020

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The cellular distribution of fluorescently labeled arrestins provides a robust, sensitive, and universal assay for screening G protein-coupled receptors

31 March 2020

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Quantitative cell-based high-content screening for vasopressin receptor agonists using transfluor technology

31 March 2020

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

31 March 2020

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Applications of bioluminescence- and fluorescence resonance energy transfer to drug discovery at G protein-coupled receptors

31 March 2020

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

31 March 2020

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

31 March 2020

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A homogeneous enzyme fragment complementation-based beta-arrestin translocation assay for high-throughput screening of G-protein-coupled receptors

31 March 2020

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The genetic design of signaling cascades to record receptor activation

31 March 2020

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G protein-independent cell-based assays for drug discovery on seven-transmembrane receptors

31 March 2020

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Micropatterned immobilization of a G protein-coupled receptor and direct detection of G protein activation.

31 March 2020

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Looking towards label-free biomolecular interaction analysis in a high-throughput format: a review of new surface plasmon resonance technologies

31 March 2020

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31 March 2020

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G-protein-coupled receptors in drug discovery: nanosizing using cell-free technologies and molecular biology approaches.

31 March 2020

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Techniques: plasmon-waveguide resonance (PWR) spectroscopy as a tool to study ligand-GPCR interactions

31 March 2020

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Plasmon-waveguide resonance studies of ligand binding to the human beta 2-adrenergic receptor

31 March 2020

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Plasmon resonance studies of agonist/antagonist binding to the human delta-opioid receptor: new structural insights into receptor-ligand interactions

31 March 2020

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Binding of agonists, antagonists and inverse agonists to the human delta-opioid receptor produces distinctly different conformational states distinguishable by plasmon-waveguide resonance spectroscopy

31 March 2020

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Resonant waveguide grating biosensor for living cell sensing.

31 March 2020

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Epidermal growth factor-induced tumor cell invasion and metastasis initiated by dephosphorylation and downregulation of focal adhesion kinase

31 March 2020

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Characteristics of dynamic mass redistribution of epidermal growth factor receptor signaling in living cells measured with label-free optical biosensors

31 March 2020

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Optical biosensor provides insights for bradykinin B(2) receptor signaling in A431 cells

31 March 2020

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Label-free cell-based assays with optical biosensors in drug discovery.

31 March 2020

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Label-free assays on the BIND system

31 March 2020

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

31 March 2020

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

31 March 2020

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Impedance-based cellular assay technologies: recent advances, future promise

31 March 2020

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Evaluation of cellular dielectric spectroscopy, a whole-cell, label-free technology for drug discovery on Gi-coupled GPCRs

31 March 2020

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Back to basics: label-free technologies for small molecule screening

31 March 2020

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High-content analysis in preclinical drug discovery

31 March 2020

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An opioid agonist that does not induce mu-opioid receptor--arrestin interactions or receptor internalization

31 March 2020

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Molecular mechanism of desensitization of the chemokine receptor CCR-5: receptor signaling and internalization are dissociable from its role as an HIV-1 co-receptor

31 March 2020

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Implementation of BacMam virus gene delivery technology in a drug discovery setting

31 March 2020

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Evolution of cell-based reagent provision

31 March 2020

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The industrialisation of cellular screening

31 March 2020

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GRKs and beta-arrestins: roles in receptor silencing, trafficking and signaling

31 March 2020

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Functional antagonism of different G protein-coupled receptor kinases for beta-arrestin-mediated angiotensin II receptor signaling

31 March 2020

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Different G protein-coupled receptor kinases govern G protein and beta-arrestin-mediated signaling of V2 vasopressin receptor

31 March 2020

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Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor

31 March 2020

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12 December 2020

CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding

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12 December 2020

Conformational changes and drug action

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12 December 2020

Self-cancellation of drug properties as a mode of organ selectivity: the antimuscarinic effects of ambenonium

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12 December 2020

A modification of receptor theory

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12 December 2020

Identifiers

DOI

10.1038/NRD2838

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Dimensions Publication ID

21 August 2017

1042808302

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