The role of kinetic context in apparent biased agonism at GPCRs

Investigating the molecular mechanisms through which FTY720-P causes persistent S1P1receptor internalization

(2014) David A Sykes et al.   BRITISH JOURNAL OF PHARMACOLOGY

Functionally Selective Dopamine D2, D3 Receptor Partial Agonists

(2014) Dorothee Möller et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationships of Privileged Structures Lead to the Discovery of Novel Biased Ligands at the Dopamine D2 Receptor

(2014) Monika Szabo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biased Agonism at G Protein-Coupled Receptors: The Promise and the Challenges-A Medicinal Chemistry Perspective

(2014) Jeremy Shonberg et al.   MEDICINAL RESEARCH REVIEWS

Endosomal generation of cAMP in GPCR signaling

(2014) Jean-Pierre Vilardaga et al.   Nature Chemical Biology

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

(2014) Kim Vietz Andreassen et al.   PLoS One

An evaluation of the safety and efficacy of cariprazine in patients with acute exacerbation of schizophrenia: A phase II, randomized clinical trial

(2014) Suresh Durgam et al.   SCHIZOPHRENIA RESEARCH

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

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

Structure–Kinetic Relationships—An Overlooked Parameter in Hit-to-Lead Optimization: A Case of Cyclopentylamines as Chemokine Receptor 2 Antagonists

(2013) Maris Vilums et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain

(2013) Xiao-Tao Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Structural Features for Functional Selectivity at Serotonin Receptors

(2013) D. Wacker et al.   SCIENCE

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

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

Deciphering biased-agonism complexity reveals a new active AT1 receptor entity

(2012) Aude Saulière et al.   Nature Chemical Biology

Impedance Responses Reveal β2-Adrenergic Receptor Signaling Pluridimensionality and Allow Classification of Ligands with Distinct Signaling Profiles

(2012) Wayne Stallaert et al.   PLoS One

Structural insights into biased G protein-coupled receptor signaling revealed by fluorescence spectroscopy

(2012) R. Rahmeh 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

Crystal Structures of a Stabilized β1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol

(2012) Tony Warne et al.   STRUCTURE

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

(2011) Terry Kenakin et al.   ACS Chemical Neuroscience

Slow dissociation of partial agonists from the D2 receptor is linked to reduced prolactin release

(2011) Lucia Carboni et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Quantifying Ligand Bias at Seven-Transmembrane Receptors

(2011) S. Rajagopal et al.   MOLECULAR PHARMACOLOGY

Pardoprunox in early Parkinson's disease: Results from 2 large, randomized double-blind trials

(2011) Cristina Sampaio et al.   MOVEMENT DISORDERS

Multiple ligand-specific conformations of the β2-adrenergic receptor

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

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

Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays

(2010) Steven J Charlton et al.   BRITISH JOURNAL OF PHARMACOLOGY

Morphine-like Opiates Selectively Antagonize Receptor-Arrestin Interactions

(2010) Paola Molinari et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2010) N. Tschammer et al.   MOLECULAR PHARMACOLOGY

 -Opioid Receptors: Correlation of Agonist Efficacy for Signalling with Ability to Activate Internalization

(2010) J. McPherson et al.   MOLECULAR PHARMACOLOGY

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

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

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

Sustained cyclic AMP production by parathyroid hormone receptor endocytosis

(2009) Sébastien Ferrandon et al.   Nature Chemical Biology

Endosomes: A legitimate platform for the signaling train

(2009) J. E. Murphy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Residence Time of Receptor−Ligand Complexes and Its Effect on Biological Function

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

Emerging drugs for schizophrenia

(2008) Ofer Agid et al.   EXPERT OPINION ON EMERGING DRUGS

Antagonism of dopamine D2 receptor/ -arrestin 2 interaction is a common property of clinically effective antipsychotics

(2008) B. Masri et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA