Biased signalling: from simple switches to allosteric microprocessors

Conformational Profiling of the AT1 Angiotensin II Receptor Reflects Biased Agonism, G Protein Coupling, and Cellular Context

(2017) Dominic Devost et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

G Protein-Coupled Receptor Kinase 3 and Protein Kinase C Phosphorylate the Distal C-Terminal Tail of the Chemokine Receptor CXCR4 and Mediate Recruitment of β -Arrestin

(2017) Jiansong Luo et al.   MOLECULAR PHARMACOLOGY

C-X-C Motif Chemokine Receptor 3 Splice Variants Differentially Activate Beta-Arrestins to Regulate Downstream Signaling Pathways

(2017) Jeffrey S. Smith et al.   MOLECULAR PHARMACOLOGY

Phase-plate cryo-EM structure of a class B GPCR–G-protein complex

(2017) Yi-Lynn Liang et al.   NATURE

Structural basis for selectivity and diversity in angiotensin II receptors

(2017) Haitao Zhang et al.   NATURE

Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein

(2017) Yan Zhang et al.   NATURE

Applications of chemogenomic library screening in drug discovery

(2017) Lyn H. Jones et al.   NATURE REVIEWS DRUG DISCOVERY

Opportunities and challenges in phenotypic drug discovery: an industry perspective

(2017) John G. Moffat et al.   NATURE REVIEWS DRUG DISCOVERY

Distinct conformations of GPCR–β-arrestin complexes mediate desensitization, signaling, and endocytosis

(2017) Thomas J. Cahill et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling

(2017) Chun-Hua Liu et al.   Nature Communications

Systematic errors in detecting biased agonism: Analysis of current methods and development of a new model-free approach

(2017) H. Ongun Onaran et al.   Scientific Reports

ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse

(2016) Larry S. Barak et al.   ACS Chemical Biology

Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor

(2016) Denise Wootten et al.   BIOCHEMICAL PHARMACOLOGY

The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling

(2016) Elizabeth A. Vecchio et al.   BIOCHEMICAL PHARMACOLOGY

GPCR-G Protein-β-Arrestin Super-Complex Mediates Sustained G Protein Signaling

(2016) Alex R.B. Thomsen et al.   CELL

Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy

(2016) Sebastian George Barton Furness et al.   CELL

The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism

(2016) Denise Wootten et al.   CELL

The adenosine metabolite inosine is a functional agonist of the adenosine A2A receptor with a unique signaling bias

(2016) Ajith A. Welihinda et al.   CELLULAR SIGNALLING

VCP746, a novel A1adenosine receptor biased agonist, reduces hypertrophy in a rat neonatal cardiac myocyte model

(2016) Chung H Chuo et al.   CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY

Partial Agonist and Biased Signaling Properties of the Synthetic Enantiomers J113863/UCB35625 at Chemokine Receptors CCR2 and CCR5

(2016) Jenny Corbisier et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A G Protein-biased Designer G Protein-coupled Receptor Useful for Studying the Physiological Relevance of Gq/11-dependent Signaling Pathways

(2016) Jianxin Hu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The β-Arrestins: Multifunctional Regulators of G Protein-coupled Receptors

(2016) Jeffrey S. Smith et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure of the adenosine A2A receptor bound to an engineered G protein

(2016) Byron Carpenter et al.   NATURE

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

(2016) Yi Zheng et al.   NATURE

Backbone NMR reveals allosteric signal transduction networks in the β1-adrenergic receptor

(2016) Shin Isogai et al.   NATURE

The conformational signature of β-arrestin2 predicts its trafficking and signalling functions

(2016) Mi-Hye Lee et al.   NATURE

β-Arrestin biosensors reveal a rapid, receptor-dependent activation/deactivation cycle

(2016) Susanne Nuber et al.   NATURE

Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation

(2016) Dean P. Staus et al.   NATURE

Extra-helical binding site of a glucagon receptor antagonist

(2016) Ali Jazayeri et al.   NATURE

Intracellular allosteric antagonism of the CCR9 receptor

(2016) Christine Oswald et al.   NATURE

Structure-based discovery of opioid analgesics with reduced side effects

(2016) Aashish Manglik et al.   NATURE

Diverse activation pathways in class A GPCRs converge near the G-protein-coupling region

(2016) A. J. Venkatakrishnan et al.   NATURE

β-Arrestin drives MAP kinase signalling from clathrin-coated structures after GPCR dissociation

(2016) K. Eichel et al.   NATURE CELL BIOLOGY

Conformationally selective RNA aptamers allosterically modulate the β2-adrenoceptor

(2016) Alem W Kahsai et al.   Nature Chemical Biology

Screening out irrelevant cell-based models of disease

(2016) Peter Horvath et al.   NATURE REVIEWS DRUG DISCOVERY

Biophysics in drug discovery: impact, challenges and opportunities

(2016) Jean-Paul Renaud et al.   NATURE REVIEWS DRUG DISCOVERY

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

A randomized, phase 2 study investigating TRV130, a biased ligand of the μ-opioid receptor, for the intravenous treatment of acute pain

(2016) Eugene R. Viscusi et al.   PAIN

β-Arrestin mediates the Frank–Starling mechanism of cardiac contractility

(2016) Dennis M. Abraham et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Distinct cortical and striatal actions of a β-arrestin–biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties

(2016) Nikhil M. Urs et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria

(2016) Tarsis F. Brust et al.   Science Signaling

Functional competence of a partially engaged GPCR–β-arrestin complex

(2016) Punita Kumari et al.   Nature Communications

Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET

(2016) Yoon Namkung et al.   Nature Communications

Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria

(2016) Tarsis F. Brust et al.   Science Signaling

Structure–Activity Relationship Studies of Functionally Selective Kappa Opioid Receptor Agonists that Modulate ERK 1/2 Phosphorylation While Preserving G Protein Over βArrestin2 Signaling Bias

(2015) Kimberly M. Lovell et al.   ACS Chemical Neuroscience

Gaddum Memorial Lecture 2014: receptors as an evolving concept: from switches to biased microprocessors

(2015) Terry Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

Structural Insights into the Dynamic Process of β 2 -Adrenergic Receptor Signaling

(2015) Aashish Manglik et al.   CELL

Structure of the Angiotensin Receptor Revealed by Serial Femtosecond Crystallography

(2015) Haitao Zhang et al.   CELL

Novel Allosteric Modulators of G Protein-coupled Receptors

(2015) Patrick R. Gentry et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Biased Signaling at Chemokine Receptors

(2015) Jenny Corbisier et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Basis for Ligand Recognition and Functional Selectivity at Angiotensin Receptor

(2015) Haitao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

β-Arrestin Recruitment and Biased Agonism at Free Fatty Acid Receptor 1

(2015) Arturo D. Mancini et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Kappa Opioid Receptor-Induced Aversion Requires p38 MAPK Activation in VTA Dopamine Neurons

(2015) J. M. Ehrich et al.   JOURNAL OF NEUROSCIENCE

Structural insights into µ-opioid receptor activation

(2015) Weijiao Huang et al.   NATURE

Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser

(2015) Yanyong Kang et al.   NATURE

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

(2015) Wesley K Kroeze et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Noribogaine is a G-protein biased κ-opioid receptor agonist

(2015) Emeline L. Maillet et al.   NEUROPHARMACOLOGY

Effects of β-Arrestin-Biased Dopamine D2 Receptor Ligands on Schizophrenia-Like Behavior in Hypoglutamatergic Mice

(2015) Su M Park et al.   NEUROPSYCHOPHARMACOLOGY

Dynorphin, Dysphoria and Dependence: the Stress of Addiction

(2015) Charles Chavkin et al.   NEUROPSYCHOPHARMACOLOGY

Structural dynamics and energetics underlying allosteric inactivation of the cannabinoid receptor CB1

(2015) Jonathan F. Fay et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural basis for chemokine recognition and activation of a viral G protein-coupled receptor

(2015) J. S. Burg et al.   SCIENCE

Optodynamic simulation of β-adrenergic receptor signalling

(2015) Edward R. Siuda et al.   Nature Communications

Phospho-selective mechanisms of arrestin conformations and functions revealed by unnatural amino acid incorporation and 19F-NMR

(2015) Fan Yang et al.   Nature Communications

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

(2015) Wesley K Kroeze et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Heart Failure Therapeutics on the Basis of a Biased Ligand of the Angiotensin-2 Type 1 Receptor

(2015) G. Michael Felker et al.   JACC-Heart Failure

Arrestin-dependent Angiotensin AT1Receptor Signaling Regulates Akt and mTor-mediated Protein Synthesis

(2014) Ryan T. Kendall et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Divergent Transducer-specific Molecular Efficacies Generate Biased Agonism at a G Protein-coupled Receptor (GPCR)

(2014) Ryan T. Strachan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of Serine 348 on the Apelin Receptor as a Novel Regulatory Phosphorylation Site in Apelin-13-induced G Protein-independent Biased Signaling

(2014) Xiaoyu Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

CXCL11-dependent induction of FOXP3-negative regulatory T cells suppresses autoimmune encephalomyelitis

(2014) Yaniv Zohar et al.   JOURNAL OF CLINICAL INVESTIGATION

A Functional Selectivity Mechanism at the Serotonin-2A GPCR Involves Ligand-Dependent Conformations of Intracellular Loop 2

(2014) Jose Manuel Perez-Aguilar et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Minireview: More Than Just a Hammer: Ligand “Bias” and Pharmaceutical Discovery

(2014) Louis M. Luttrell   MOLECULAR ENDOCRINOLOGY

Visualization of arrestin recruitment by a G-protein-coupled receptor

(2014) Arun K. Shukla et al.   NATURE

Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers

(2014) David G. Soergel et al.   PAIN

Prolonged Calcitonin Receptor Signaling by Salmon, but Not Human Calcitonin, Reveals Ligand Bias

(2014) Kim Vietz Andreassen et al.   PLoS One

Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist

(2014) C. Valant et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

CXCL10 Is Critical for the Progression and Maintenance of Depigmentation in a Mouse Model of Vitiligo

(2014) M. Rashighi et al.   Science Translational Medicine

What is biased efficacy? Defining the relationship between intrinsic efficacy and free energy coupling

(2014) H. Ongun Onaran et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Biased ligands at G-protein-coupled receptors: promise and progress

(2014) Jonathan D. Violin et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Crystal structure of a common GPCR-binding interface for G protein and arrestin

(2014) Michal Szczepek et al.   Nature Communications

Biased and G Protein-Independent Signaling of Chemokine Receptors

(2014) Anne Steen et al.   Frontiers in Immunology

The Dynamic Process of β2-Adrenergic Receptor Activation

(2013) Rie Nygaard et al.   CELL

β-Arrestin1–Biased β 1 -Adrenergic Receptor Signaling Regulates MicroRNA Processing

(2013) Il-man Kim et al.   CIRCULATION RESEARCH

Recent developments in biased agonism

(2013) James W Wisler et al.   CURRENT OPINION IN CELL BIOLOGY

Distinct Roles of β-Arrestin 1 and β-Arrestin 2 in ORG27569-induced Biased Signaling and Internalization of the Cannabinoid Receptor 1 (CB1)

(2013) Kwang H. Ahn et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Constitutive Internalization of the Leucine-rich G Protein-coupled Receptor-5 (LGR5) to the Trans-Golgi Network

(2013) Joshua C. Snyder et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Development of Functionally Selective, Small Molecule Agonists at Kappa Opioid Receptors

(2013) Lei Zhou et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Biased Agonism as a Mechanism for Differential Signaling by Chemokine Receptors

(2013) Sudarshan Rajagopal et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Structure–Activity Analysis of Biased Agonism at the Dopamine D2 Receptor

(2013) Jeremy Shonberg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of κ Opioid Receptor Antagonists

(2013) F. Ivy Carroll et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal structure of pre-activated arrestin p44

(2013) Yong Ju Kim et al.   NATURE

Structure of class B GPCR corticotropin-releasing factor receptor 1

(2013) Kaspar Hollenstein et al.   NATURE

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

Conformational biosensors reveal GPCR signalling from endosomes

(2013) Roshanak Irannejad et al.   NATURE

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

Measurements of ligand bias and functional affinity

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

Quantifying biased agonism: understanding the links between affinity and efficacy

(2013) Sudarshan Rajagopal   NATURE REVIEWS DRUG DISCOVERY

Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein

(2013) J. Quoyer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Role of kappa-opioid receptors in stress and anxiety-related behavior

(2013) Ashlee Van’t Veer et al.   PSYCHOPHARMACOLOGY

Structural Features for Functional Selectivity at Serotonin Receptors

(2013) D. Wacker et al.   SCIENCE

Discovery of ML314, a Brain Penetrant Nonpeptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor

(2013) Satyamaheshwar Peddibhotla et al.   ACS Medicinal Chemistry Letters

Psychotomimetic Effects of Kappa Opioid Receptor Agonists

(2012) Kate L. White et al.   BIOLOGICAL PSYCHIATRY

6′-Guanidinonaltrindole (6′-GNTI) Is a G Protein-biased κ-Opioid Receptor Agonist That Inhibits Arrestin Recruitment

(2012) Marie-Laure Rives et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure–Functional Selectivity Relationship Studies of β-Arrestin-Biased Dopamine D2 Receptor Agonists

(2012) Xin Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

(2012) Aashish Manglik et al.   NATURE

TGFα shedding assay: an accurate and versatile method for detecting GPCR activation

(2012) Asuka Inoue et al.   NATURE METHODS

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

Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity

(2012) Thomas A Munro et al.   BMC Pharmacology & Toxicology

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

(2011) Terry Kenakin et al.   ACS Chemical Neuroscience

The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy

(2011) Suzanne E. Wardell et al.   BIOCHEMICAL PHARMACOLOGY

A Single Mutation in Arrestin-2 Prevents ERK1/2 Activation by Reducing c-Raf1 Binding

(2011) Sergio Coffa et al.   BIOCHEMISTRY

Biased signalling and allosteric machines: new vistas and challenges for drug discovery

(2011) Terry P Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

CXCR3 ligands: redundant, collaborative and antagonistic functions

(2011) Joanna R Groom et al.   IMMUNOLOGY AND CELL BIOLOGY

CXCR7/CXCR4 Heterodimer Constitutively Recruits β-Arrestin to Enhance Cell Migration

(2011) Fabien M. Décaillot et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Quantifying Ligand Bias at Seven-Transmembrane Receptors

(2011) S. Rajagopal et al.   MOLECULAR PHARMACOLOGY

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

(2011) Guillaume Lebon et al.   NATURE

Crystal structure of metarhodopsin II

(2011) Hui-Woog Choe et al.   NATURE

The structural basis of agonist-induced activation in constitutively active rhodopsin

(2011) Jörg Standfuss et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

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

Multiple ligand-specific conformations of the β2-adrenergic receptor

(2011) Alem W Kahsai et al.   Nature Chemical Biology

How were new medicines discovered?

(2011) David C. Swinney et al.   NATURE REVIEWS DRUG DISCOVERY

CXCR4 and CXCR7 Have Distinct Functions in Regulating Interneuron Migration

(2011) Yanling Wang et al.   NEURON

Selective p38α MAPK Deletion in Serotonergic Neurons Produces Stress Resilience in Models of Depression and Addiction

(2011) Michael R. Bruchas et al.   NEURON

Monomeric and dimeric CXCL12 inhibit metastasis through distinct CXCR4 interactions and signaling pathways

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

Structural flexibility of the G s  -helical domain in the  2-adrenoceptor Gs complex

(2011) G. H. Westfield et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu et al.   SCIENCE

Distinct Phosphorylation Sites on the  2-Adrenergic Receptor Establish a Barcode That Encodes Differential Functions of  -Arrestin

(2011) K. N. Nobles et al.   Science Signaling

β-arrestin-mediated receptor trafficking and signal transduction

(2011) Sudha K. Shenoy et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Diversity and modularity of G protein-coupled receptor structures

(2011) Vsevolod Katritch et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Multiplexing of Multicolor Bioluminescence Resonance Energy Transfer

(2010) Billy Breton et al.   BIOPHYSICAL JOURNAL

Site-specific Phosphorylation of CXCR4 Is Dynamically Regulated by Multiple Kinases and Results in Differential Modulation of CXCR4 Signaling

(2010) John M. Busillo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Identification of Orthosteric and Allosteric Site Mutations in M2Muscarinic Acetylcholine Receptors That Contribute to Ligand-selective Signaling Bias

(2010) Karen J. Gregory et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Teaching old receptors new tricks: biasing seven-transmembrane receptors

(2010) Sudarshan Rajagopal et al.   NATURE REVIEWS DRUG DISCOVERY

Review: The chemokine receptor CXCR3 and its ligands CXCL9, CXCL10 and CXCL11 in neuroimmunity - a tale of conflict and conundrum

(2010) M. Müller et al.   NEUROPATHOLOGY AND APPLIED NEUROBIOLOGY

The M3-muscarinic receptor regulates learning and memory in a receptor phosphorylation/arrestin-dependent manner

(2010) B. Poulin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Ligand-directed c-Jun N-terminal kinase activation disrupts opioid receptor signaling

(2010) E. J. Melief et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Therapeutic potential of β-arrestin- and G protein-biased agonists

(2010) Erin J. Whalen et al.   TRENDS IN MOLECULAR MEDICINE

CXCR7 heterodimerizes with CXCR4 and regulates CXCL12-mediated G protein signaling

(2009) A. Levoye et al.   BLOOD

β-Arrestin-2 Mediates Anti-apoptotic Signaling through Regulation of BAD Phosphorylation

(2009) Seungkirl Ahn et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Allosteric Modulators of the Adenosine A1Receptor: Synthesis and Pharmacological Evaluation of 4-Substituted 2-Amino-3-benzoylthiophenes

(2009) Luigi Aurelio et al.   JOURNAL OF MEDICINAL CHEMISTRY

Sustained cyclic AMP production by parathyroid hormone receptor endocytosis

(2009) Sébastien Ferrandon et al.   Nature Chemical Biology

 -arrestin- but not G protein-mediated signaling by the "decoy" receptor CXCR7

(2009) S. Rajagopal et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Activation of the kappa opioid receptor in the dorsal raphe nucleus mediates the aversive effects of stress and reinstates drug seeking

(2009) Benjamin B. Land et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

The Dopamine Hypothesis of Schizophrenia: Version III--The Final Common Pathway

(2009) O. D. Howes et al.   SCHIZOPHRENIA BULLETIN

Persistent cAMP-Signals Triggered by Internalized G-Protein–Coupled Receptors

(2009) Davide Calebiro et al.   PLOS BIOLOGY

Differing pharmacological activities of thiazolidinone analogs at the FSH receptor

(2008) Brian J. Arey et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

The Dysphoric Component of Stress Is Encoded by Activation of the Dynorphin  -Opioid System

(2008) B. B. Land et al.   JOURNAL OF NEUROSCIENCE

Structural diversity of G protein-coupled receptors and significance for drug discovery

(2008) Malin C. Lagerström et al.   NATURE REVIEWS DRUG DISCOVERY

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

 -Blockers alprenolol and carvedilol stimulate  -arrestin-mediated EGFR transactivation

(2008) I.-M. Kim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE

Regulation of GPCRs by Endocytic Membrane Trafficking and Its Potential Implications

(2007) Aylin C. Hanyaloglu et al.   Annual Review of Pharmacology and Toxicology