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

21 August 2017

1 reference

title

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

1 reference

21 August 2017

transmembrane protein

0 references

1 reference

Terry P Kenakin

1

1 reference

21 August 2017

17 July 2009

1 reference

Nature Reviews Drug Discovery

21 August 2017

1 reference

21 August 2017

8

1 reference

21 August 2017

8

1 reference

21 August 2017

617-626

1 reference

https://scigraph.springernature.com/pub.10.1038/nrd2838

21 August 2017

0 references

cites work

Comparison of some properties of pronethalol and propranolol

1 reference

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

31 March 2020

1 reference

Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins

31 March 2020

1 reference

Efficacy as a vector: the relative prevalence and paucity of inverse agonism

31 March 2020

1 reference

Beta-blockers in heart failure: are pharmacological differences clinically important?

31 March 2020

1 reference

A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling

31 March 2020

1 reference

Distinct signaling profiles of beta1 and beta2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy

31 March 2020

1 reference

On becoming and being a pharmacologist.

31 March 2020

1 reference

The release and fate of vaso-active hormones in the circulation

31 March 2020

1 reference

Histamine and its receptors

31 March 2020

1 reference

The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor

31 March 2020

1 reference

Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro

31 March 2020

1 reference

G-protein coupled receptors as allosteric machines

31 March 2020

1 reference

Modeling the functional effects of allosteric modulators at pharmacological receptors: an extension of the two-state model of receptor activation.

31 March 2020

1 reference

Amylin receptors: molecular composition and pharmacology

31 March 2020

1 reference

Distinct receptor activity-modifying protein domains differentially modulate interaction with calcitonin receptors

31 March 2020

1 reference

31 March 2020

GPCR modulation by RAMPs

1 reference

Characterisation using microphysiometry of CRF receptor pharmacology

31 March 2020

1 reference

The Energy Landscapes and Motions of Proteins

31 March 2020

1 reference

A statistical thermodynamic model of the protein ensemble

31 March 2020

1 reference

Intrinsic disorder as a mechanism to optimize allosteric coupling in proteins

31 March 2020

1 reference

Intrinsic disorder in transcription factors

31 March 2020

1 reference

Agonist efficacy and allosteric models of receptor action.

31 March 2020

1 reference

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

31 March 2020

1 reference

Efficacy at G-protein-coupled receptors

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Transduction of receptor signals by beta-arrestins

31 March 2020

1 reference

Composition and function of g protein-coupled receptor signalsomes controlling mitogen-activated protein kinase activity.

31 March 2020

1 reference

Regulation of alpha2AR trafficking and signaling by interacting proteins

31 March 2020

1 reference

G protein-coupled receptor interacting proteins: emerging roles in localization and signal transduction

31 March 2020

1 reference

Ligand-selective receptor conformations revisited: the promise and the problem

31 March 2020

1 reference

Paradoxical trafficking and regulation of 5-HT(2A) receptors by agonists and antagonists

31 March 2020

1 reference

New concepts in drug discovery: collateral efficacy and permissive antagonism

31 March 2020

1 reference

Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMAP analysis in complex human primary cell-based models

31 March 2020

1 reference

Agonist-receptor efficacy. II. Agonist trafficking of receptor signals

31 March 2020

1 reference

Drug efficacy at G protein-coupled receptors

31 March 2020

1 reference

Beta-arrestin-biased ligands at seven-transmembrane receptors

31 March 2020

1 reference

GPCR functional selectivity has therapeutic impact

31 March 2020

1 reference

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

31 March 2020

1 reference

Biochemical and pharmacological control of the multiplicity of coupling at G-protein-coupled receptors

31 March 2020

1 reference

Multiple signaling states of G-protein-coupled receptors

31 March 2020

1 reference

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

31 March 2020

1 reference

Measuring intracellular calcium fluxes in high throughput mode

31 March 2020

1 reference

cAMP detection methods in HTS: selecting the best from the rest

31 March 2020

1 reference

High-content assays for ligand regulation of G-protein-coupled receptors

31 March 2020

1 reference

beta-arrestins: traffic cops of cell signaling

31 March 2020

1 reference

The repertoire of G-protein-coupled receptors in fully sequenced genomes

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

The genetic design of signaling cascades to record receptor activation

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Surface plasmon resonance: towards an understanding of the mechanisms of biological molecular recognition

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

1 reference

Resonant waveguide grating biosensor for living cell sensing.

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Label-free assays on the BIND system.

31 March 2020

1 reference

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

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

High-content analysis in preclinical drug discovery

31 March 2020

1 reference

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

31 March 2020

1 reference

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

1 reference

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

31 March 2020

1 reference

Evolution of cell-based reagent provision

31 March 2020

1 reference

The industrialisation of cellular screening

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

12 December 2020

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

1 reference

12 December 2020

Conformational changes and drug action

1 reference

12 December 2020

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

1 reference

12 December 2020

A modification of receptor theory

1 reference

12 December 2020

Identifiers

DOI

10.1038/NRD2838

1 reference

PubMed ID

19609267

Dimensions Publication ID

21 August 2017

0 references

1 reference

PubMed ID

19609267