Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor

Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors

(2017) Kathryn E. Livingston et al.   MOLECULAR PHARMACOLOGY

Unravelling intrinsic efficacy and ligand bias at G protein coupled receptors: A practical guide to assessing functional data

(2016) Lisa A. Stott et al.   BIOCHEMICAL PHARMACOLOGY

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

(2016) Dean P. Staus et al.   NATURE

Structure-based discovery of opioid analgesics with reduced side effects

(2016) Aashish Manglik et al.   NATURE

The role of kinetic context in apparent biased agonism at GPCRs

(2016) Carmen Klein Herenbrink et al.   Nature Communications

Methadone Reverses Analgesic Tolerance Induced by Morphine Pretreatment

(2015) Luca Posa et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Ligand-Based Discovery of a New Scaffold for Allosteric Modulation of the μ-Opioid Receptor

(2015) Paola Bisignano et al.   Journal of Chemical Information and Modeling

Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor

(2015) Neil T. Burford et al.   JOURNAL OF MEDICINAL CHEMISTRY

Use of radiolabeled antagonist assays for assessing agonism at D2 and D3 dopamine receptors: Comparison with functional GTPγS assays

(2015) Juan Zhen et al.   JOURNAL OF NEUROSCIENCE METHODS

Agonist stimulation at human μ opioid receptors in a [35S]GTPγS incorporation assay: observation of “bell-shaped” concentration–response relationships under conditions of strong receptor G protein coupling

(2015) Peter Heusler et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Structural insights into µ-opioid receptor activation

(2015) Weijiao Huang et al.   NATURE

Propagation of conformational changes during μ-opioid receptor activation

(2015) Rémy Sounier et al.   NATURE

Disruption of the Na+ion binding site as a mechanism for positive allosteric modulation of the mu-opioid receptor

(2014) Kathryn E. Livingston et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Discovery of positive allosteric modulators and silent allosteric modulators of the  -opioid receptor

(2013) N. T. Burford et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2012) Aashish Manglik et al.   NATURE

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

(2011) Terry Kenakin et al.   ACS Chemical Neuroscience

Analysis of opioid efficacy, tolerance, addiction and dependence from cell culture to human

(2011) Michael M Morgan et al.   BRITISH JOURNAL OF PHARMACOLOGY

The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

(2011) Tony Warne et al.   NATURE

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

Analytical pharmacology: the impact of numbers on pharmacology

(2011) Terry Kenakin et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

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

(2010) J. McPherson et al.   MOLECULAR PHARMACOLOGY

Teaching old receptors new tricks: biasing seven-transmembrane receptors

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

Neutral antagonist activity of naltrexone and 6β-naltrexol in naïve and opioid-dependent C6 cells expressing a µ-opioid receptor

(2009) MF Divin et al.   BRITISH JOURNAL OF PHARMACOLOGY

Purification and Functional Reconstitution of Monomeric μ-Opioid Receptors

(2009) Adam J. Kuszak et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Opioid Rotation: The Science and the Limitations of the Equianalgesic Dose Table

(2009) Helena Knotkova et al.   JOURNAL OF PAIN AND SYMPTOM MANAGEMENT

Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties

(2009) Katie Leach et al.   NEUROPSYCHOPHARMACOLOGY

Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors

(2008) P G Strange   BRITISH JOURNAL OF PHARMACOLOGY

Crystal structure of opsin in its G-protein-interacting conformation

(2008) Patrick Scheerer et al.   NATURE