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

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Intrinsic Disorder in Transcription Factors

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β-Arrestin-biased ligands at seven-transmembrane receptors

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A unique mechanism of β-blocker action: Carvedilol stimulates β-arrestin signaling

2007 • 571 citations

The Repertoire of G-Protein–Coupled Receptors in Fully Sequenced Genomes

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Histamine and its receptors

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

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

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Intrinsic disorder as a mechanism to optimize allosteric coupling in proteins

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Resonant Waveguide Grating Biosensor for Living Cell Sensing

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Functionally Different Agonists Induce Distinct Conformations in the G Protein Coupling Domain of the β2Adrenergic Receptor

2001 • 361 citations

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

2005 • 339 citations

Sequential Binding of Agonists to the β2 Adrenoceptor

2003 • 333 citations

Epidermal Growth Factor-Induced Tumor Cell Invasion and Metastasis Initiated by Dephosphorylation and Downregulation of Focal Adhesion Kinase

2001 • 325 citations

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

1999 • 324 citations

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

2006 • 323 citations

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

2005 • 323 citations

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

2003 • 319 citations

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

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Drug Efficacy at G Protein–Coupled Receptors

2002 • 315 citations

New Concepts in Drug Discovery: Collateral Efficacy and Permissive Antagonism

2005 • 313 citations

The CCR5 Receptor-Based Mechanism of Action of 873140, a Potent Allosteric Noncompetitive HIV Entry Inhibitor

2005 • 297 citations

Distinct Signaling Profiles of β₁ and β₂ Adrenergic Receptor Ligands toward Adenylyl Cyclase and Mitogen-Activated Protein Kinase Reveals the Pluridimensionality of Efficacy

2006 • 284 citations

Paradoxical trafficking and regulation of 5-HT2A receptors by agonists and antagonists

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β-arrestins: traffic cops of cell signaling

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

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Fluorescent Labeling of Purified β2 Adrenergic Receptor

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COMPARISON OF SOME PROPERTIES OF PRONETHALOL AND PROPRANOLOL

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

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Efficacy at g-protein-coupled receptors

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Label-Free Assays on the BIND System

2004 • 251 citations

Multiple Signaling States of G-Protein-Coupled Receptors

2005 • 237 citations

Real-Time Monitoring of Morphological Changes in Living Cells by Electronic Cell Sensor Arrays: An Approach To Study G Protein-Coupled Receptors

2005 • 234 citations

GPCR modulation by RAMPs

2005 • 227 citations

Spirodiketopiperazine-Based CCR5 Inhibitor Which Preserves CC-Chemokine/CCR5 Interactions and Exerts Potent Activity against R5 Human Immunodeficiency Virus Type 1 In Vitro

2004 • 221 citations

An Opioid Agonist that Does Not Induce μ-Opioid Receptor—Arrestin Interactions or Receptor Internalization

2006 • 221 citations

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

2007 • 208 citations

Efficacy as a Vector: the Relative Prevalence and Paucity of Inverse Agonism

2004 • 207 citations

GPCR functional selectivity has therapeutic impact

2007 • 204 citations

Label-Free Cell-Based Assays with Optical Biosensors in Drug Discovery

2006 • 200 citations

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

1997 • 198 citations

Modeling the Functional Effects of Allosteric Modulators at Pharmacological Receptors: An Extension of the Two-State Model of Receptor Activation

2000 • 188 citations

A Statistical Thermodynamic Model of the Protein Ensemble

2006 • 179 citations

High-Throughput Screening of G Protein-Coupled Receptor Antagonists Using a Bioluminescence Resonance Energy Transfer 1-Based β-Arrestin2 Recruitment Assay

2005 • 173 citations

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

2004 • 167 citations

Characteristics of Dynamic Mass Redistribution of Epidermal Growth Factor Receptor Signaling in Living Cells Measured with Label-Free Optical Biosensors

2005 • 138 citations

The Neurokinin A Receptor Activates Calcium and cAMP Responses through Distinct Conformational States

2001 • 129 citations

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

2002 • 124 citations

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

2004 • 119 citations

The Cellular Distribution of Fluorescently Labeled Arrestins Provides a Robust, Sensitive, and Universal Assay for Screening G Protein-Coupled Receptors

2002 • 117 citations

Composition and Function of G Protein-Coupled Receptor Signalsomes Controlling Mitogen-Activated Protein Kinase Activity

2005 • 111 citations

Plasmon Resonance Studies of Agonist/Antagonist Binding to theHuman δ-Opioid Receptor: New Structural Insights into Receptor-Ligand Interactions

2000 • 109 citations

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

2007 • 106 citations

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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Agonist Efficacy and Aliosteric Models of Receptor Action^a

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Conformational changes and drug action.

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Cellular Dielectric Spectroscopy: A Label-Free Comprehensive Platform for Functional Evaluation of Endogenous Receptors

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

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Rapid Structure-Activity and Selectivity Analysis of Kinase Inhibitors by BioMAP Analysis in Complex Human Primary Cell-Based Models

2004 • 81 citations

Amylin receptors: molecular composition and pharmacology

2004 • 80 citations

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

2007 • 79 citations

βGalactosidase Complementation: A Cell-Based Luminescent Assay Platform for Drug Discovery

2007 • 79 citations

Evaluation of Cellular Dielectric Spectroscopy, a Whole-Cell, Label-Free Technology for Drug Discovery on Gi-Coupled GPCRs

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Readings in Pharmacology

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Optical biosensor provides insights for bradykinin B₂ receptor signaling in A431 cells

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A Homogeneous Enzyme Fragment Complementation-Based β-Arrestin Translocation Assay for High-Throughput Screening of G-Protein-Coupled Receptors

2008 • 71 citations

Quantitative Cell-Based High-Content Screening for Vasopressin Receptor Agonists Using Transfluor®Technology

2005 • 70 citations

Back to Basics: Label-Free Technologies for Small Molecule Screening

2008 • 68 citations

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

2003 • 67 citations

Plasmon-Waveguide Resonance Studies of Ligand Binding to the Human β₂-Adrenergic Receptor

2004 • 62 citations

Distinct Receptor Activity-Modifying Protein Domains Differentially Modulate Interaction with Calcitonin Receptors

2006 • 59 citations

Measuring Intracellular Calcium Fluxes in High Throughput Mode

2003 • 57 citations

A unique mechanism of -blocker action: Carvedilol stimulates -arrestin signaling

2007 • 51 citations

Beta-Blockers in Heart Failure: Are Pharmacological Differences Clinically Important?

2004 • 50 citations

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

2003 • 46 citations

G-Protein Coupled Receptors as Allosteric Machines

2004 • 45 citations

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

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G-Protein-Coupled Receptors in Drug Discovery: Nanosizing Using Cell-Free Technologies and Molecular Biology Approaches

2005 • 39 citations

Characterisation using microphysiometry of CRF receptor pharmacology

1999 • 39 citations

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

2008 • 36 citations

Regulation of α2AR trafficking and signaling by interacting proteins

2006 • 35 citations

High-Content Analysis in Preclinical Drug Discovery

2008 • 33 citations

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

2007 • 30 citations

Evolution of cell-based reagent provision

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Multiplexed Assays by High-Content Imaging for Assessment of GPCR Activity

2008 • 22 citations

On Becoming and Being a Pharmacologist

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

1985 • 20 citations

The industrialisation of cellular screening

2008 • 7 citations