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

Modeling of Bias for the Analysis of Receptor Signaling in Biochemical Systems

(2012) Larry S. Barak et al.   BIOCHEMISTRY

TRV120027, a Novel β-Arrestin Biased Ligand at the Angiotensin II Type I Receptor, Unloads the Heart and Maintains Renal Function When Added to Furosemide in Experimental Heart Failure

(2012) Guido Boerrigter et al.   Circulation-Heart Failure

Synthesis and Characterization of Novel 2-Amino-3-benzoylthiophene Derivatives as Biased Allosteric Agonists and Modulators of the Adenosine A1 Receptor

(2012) Celine Valant et al.   JOURNAL OF MEDICINAL CHEMISTRY

Where have all the active receptor states gone?

(2012) H Ongun Onaran et al.   Nature Chemical Biology

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

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

(2011) Terry P Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

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

Positive and Negative Allosteric Modulators Promote Biased Signaling at the Calcium-Sensing Receptor

(2011) Anna E. Davey et al.   ENDOCRINOLOGY

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

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

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

Crystal structure of the β2 adrenergic receptor–Gs protein complex

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

Meningococcus Hijacks a β2-Adrenoceptor/β-Arrestin Pathway to Cross Brain Microvasculature Endothelium

(2010) Mathieu Coureuil et al.   CELL

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

A Novel Biased Allosteric Compound Inhibitor of Parturition Selectively Impedes the Prostaglandin F2α-mediated Rho/ROCK Signaling Pathway

(2010) Eugénie Goupil 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

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

(2010) J. McPherson 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

Prediction of Functionally Selective Allosteric Interactions at an M3 Muscarinic Acetylcholine Receptor Mutant Using Saccharomyces cerevisiae

(2010) G. D. Stewart et al.   MOLECULAR PHARMACOLOGY

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

(2010) Peter Keov et al.   NEUROPHARMACOLOGY

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

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

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

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

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

Membrane Type 1 Matrix Metalloproteinase Induces Epithelial-to-Mesenchymal Transition in Prostate Cancer

(2008) Jian Cao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Molecular determinants of angiotensin II type 1 receptor functional selectivity

(2008) Mark Aplin et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

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

Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity

(2008) J. E. Marlo 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

On the analysis of ligand-directed signaling at G protein-coupled receptors

(2008) Frederick J. Ehlert   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Agonist-directed signaling of the serotonin 2A receptor depends on  -arrestin-2 interactions in vivo

(2008) C. L. Schmid et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

 -Arrestin-1 mediates glucagon-like peptide-1 signaling to insulin secretion in cultured pancreatic   cells

(2008) N. Sonoda et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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