New concepts in pharmacological efficacy at 7TM receptors: IUPHAR Review 2

Functional efficacy of adenosine A2A receptor agonists is positively correlated to their receptor residence time

(2012) Dong Guo et al.   BRITISH JOURNAL OF PHARMACOLOGY

Ligands and signaling proteins govern the conformational landscape explored by a G protein-coupled receptor

(2012) S. Mary et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Biased Signaling Pathways in  2-Adrenergic Receptor Characterized by 19F-NMR

(2012) J. J. Liu et al.   SCIENCE

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

(2011) Terry Kenakin et al.   ACS Chemical Neuroscience

Greatly enhanced detection of a volatile ligand at femtomolar levels using bioluminescence resonance energy transfer (BRET)

(2011) Helen Dacres et al.   BIOSENSORS & BIOELECTRONICS

The subtleties of µ-opioid receptor phosphorylation

(2011) Eamonn Kelly   BRITISH JOURNAL OF PHARMACOLOGY

Agonist-selective patterns of µ-opioid receptor phosphorylation revealed by phosphosite-specific antibodies

(2011) Christian Doll et al.   BRITISH JOURNAL OF PHARMACOLOGY

Guide to Receptors and Channels (GRAC), 5th edition

(2011) SPH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

G Protein–Dependent and G Protein–Independent Signaling Pathways and Their Impact on Cardiac Function

(2011) Douglas G. Tilley   CIRCULATION RESEARCH

Biased Ligands for Better Cardiovascular Drugs

(2011) Scott M. DeWire et al.   CIRCULATION RESEARCH

Cardiorenal Actions of TRV120027, a Novel ß-Arrestin–Biased Ligand at the Angiotensin II Type I Receptor, in Healthy and Heart Failure Canines

(2011) Guido Boerrigter et al.   Circulation-Heart Failure

The Antidepressant Desipramine Is an Arrestin-biased Ligand at the α2A-Adrenergic Receptor Driving Receptor Down-regulationin Vitroandin Vivo

(2011) Christopher Cottingham et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Quantifying Ligand Bias at Seven-Transmembrane Receptors

(2011) S. Rajagopal et al.   MOLECULAR PHARMACOLOGY

Developing Chemical Genetic Approaches to Explore G Protein-Coupled Receptor Function: Validation of the Use of a Receptor Activated Solely by Synthetic Ligand (RASSL)

(2011) E. Alvarez-Curto et al.   MOLECULAR PHARMACOLOGY

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

Discovery of  -Arrestin-Biased Dopamine D2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy

(2011) J. A. Allen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Quantitative Encoding of the Effect of a Partial Agonist on Individual Opioid Receptors by Multisite Phosphorylation and Threshold Detection

(2011) E. K. Lau et al.   Science Signaling

Apical and basolateral pools of proteinase-activated receptor-2 direct distinct signaling events in the intestinal epithelium

(2010) Chang Lau et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Ligand-directed signalling at β-adrenoceptors

(2010) Bronwyn A. Evans et al.   BRITISH JOURNAL OF PHARMACOLOGY

Impact of species variability and ‘probe-dependence’ on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor

(2010) S Suratman et al.   BRITISH JOURNAL OF PHARMACOLOGY

Differential G-protein-coupled Receptor Phosphorylation Provides Evidence for a Signaling Bar Code

(2010) Adrian J. Butcher et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Functional Selectivity and Biased Receptor Signaling

(2010) T. Kenakin   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Selectively Engaging  -Arrestins at the Angiotensin II Type 1 Receptor Reduces Blood Pressure and Increases Cardiac Performance

(2010) J. D. Violin et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Agonist-Biased Signaling at the Histamine H4 Receptor: JNJ7777120 Recruits  -Arrestin without Activating G Proteins

(2010) E. M. Rosethorne et al.   MOLECULAR PHARMACOLOGY

Histidine 6.55 Is a Major Determinant of Ligand-Biased Signaling in Dopamine D2L Receptor

(2010) N. Tschammer et al.   MOLECULAR PHARMACOLOGY

Allosteric Ligands of the Glucagon-Like Peptide 1 Receptor (GLP-1R) Differentially Modulate Endogenous and Exogenous Peptide Responses in a Pathway-Selective Manner: Implications for Drug Screening

(2010) C. Koole et al.   MOLECULAR PHARMACOLOGY

Quantification of Functional Selectivity at the Human  1A-Adrenoceptor

(2010) B. A. Evans et al.   MOLECULAR PHARMACOLOGY

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

(2010) Ralf Schröder et al.   NATURE BIOTECHNOLOGY

Directed molecular evolution of DREADDs: a generic approach to creating next-generation RASSLs

(2010) Shuyun Dong et al.   Nature Protocols

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

(2010) T. Kenakin et al.   PHARMACOLOGICAL REVIEWS

Global phosphorylation analysis of  -arrestin-mediated signaling downstream of a seven transmembrane receptor (7TMR)

(2010) K. Xiao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Differential Presentation of Protein Interaction Surfaces on the Androgen Receptor Defines the Pharmacological Actions of Bound Ligands

(2009) John David Norris et al.   CHEMISTRY & BIOLOGY

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

(2009) Robert W. Walters et al.   JOURNAL OF CLINICAL INVESTIGATION

Genetic Deletion of p90 Ribosomal S6 Kinase 2 Alters Patterns of 5-Hydroxytryptamine2A Serotonin Receptor Functional Selectivity

(2009) R. T. Strachan et al.   MOLECULAR PHARMACOLOGY

Conformational Toggle Switches Implicated in Basal Constitutive and Agonist-Induced Activated States of 5-Hydroxytryptamine-4 Receptors

(2009) L. P. Pellissier et al.   MOLECULAR PHARMACOLOGY

Exploring the Mechanism of Agonist Efficacy: A Relationship between Efficacy and Agonist Dissociation Rate at the Muscarinic M3 Receptor

(2009) D. A. Sykes et al.   MOLECULAR PHARMACOLOGY

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

(2009) Terry P. Kenakin   NATURE REVIEWS DRUG DISCOVERY

Selective engagement of G protein coupled receptor kinases (GRKs) encodes distinct functions of biased ligands

(2009) D. A. Zidar et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A  -Arrestin-Biased Agonist of the Parathyroid Hormone Receptor (PTH1R) Promotes Bone Formation Independent of G Protein Activation

(2009) D. Gesty-Palmer et al.   Science Translational Medicine

‘7TM Receptor Allostery: Putting Numbers to Shapeshifting Proteins

(2009) Terry P. Kenakin   TRENDS IN PHARMACOLOGICAL SCIENCES

Gα-Subunits Differentially Alter the Conformation and Agonist Affinity of κ-Opioid Receptors†

(2008) Feng Yan et al.   BIOCHEMISTRY

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

(2008) M J Lohse et al.   BRITISH JOURNAL OF PHARMACOLOGY

G-protein-coupled receptor phosphorylation: where, when and by whom

(2008) A B Tobin   BRITISH JOURNAL OF PHARMACOLOGY

Molecular mechanism of Zn2+agonism in the extracellular domain of GPR39

(2008) Laura Storjohann et al.   FEBS LETTERS

Ribosomal S6 Kinase 2 Directly Phosphorylates the 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptor, Thereby Modulating 5-HT2ASignaling

(2008) Ryan T. Strachan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Selectivity of Agonists for the Active State of M1 to M4 Muscarinic Receptor Subtypes

(2008) K. W. Figueroa et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Fluorescence Resonance Energy Transfer Analysis of  2a-Adrenergic Receptor Activation Reveals Distinct Agonist-Specific Conformational Changes

(2008) A. Zurn et al.   MOLECULAR PHARMACOLOGY

Conformational Rearrangements and Signaling Cascades Involved in Ligand-Biased Mitogen-Activated Protein Kinase Signaling through the  1-Adrenergic Receptor

(2008) S. Galandrin et al.   MOLECULAR PHARMACOLOGY

Estimation of Relative Microscopic Affinity Constants of Agonists for the Active State of the Receptor in Functional Studies on M2 and M3 Muscarinic Receptors

(2008) J. A. Tran et al.   MOLECULAR PHARMACOLOGY

Engineering GPCR signaling pathways with RASSLs

(2008) Bruce R Conklin et al.   NATURE METHODS

Engineered GPCRs as Tools to Modulate Signal Transduction

(2008) Ying Pei et al.   PHYSIOLOGY

Distinct conformational changes in  -arrestin report biased agonism at seven-transmembrane receptors

(2008) A. K. Shukla et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Location, location, location…site-specific GPCR phosphorylation offers a mechanism for cell-type-specific signalling

(2008) Andrew B. Tobin et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Ligand-Stabilized Conformational States of Human β2 Adrenergic Receptor: Insight into G-Protein-Coupled Receptor Activation

(2007) Supriyo Bhattacharya et al.   BIOPHYSICAL JOURNAL

Pharmacological Onomastics: What's in a name?

(2007) T P Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

Unique agonist-bound cannabinoid CB1 receptor conformations indicate agonist specificity in signaling

(2007) Teodora Georgieva et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Multiple diverse ligands binding at a single protein site: A matter of pre-existing populations

(2002) Buyong Ma et al.   PROTEIN SCIENCE