Biased ligand quantification in drug discovery: from theory to high throughput screening to identify new biased μ opioid receptor agonists

The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors

(2015) Stephen PH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Concise Guide to PHARMACOLOGY 2015/16: Overview

(2015) Stephen PH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Concise Guide to PHARMACOLOGY 2015/16: Enzymes

(2015) Stephen PH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

Experimental design and analysis and their reporting: new guidance for publication in BJP

(2015) Michael J Curtis et al.   BRITISH JOURNAL OF PHARMACOLOGY

Identifying ligand-specific signalling within biased responses: focus on δ opioid receptor ligands

(2014) I Charfi et al.   BRITISH JOURNAL OF PHARMACOLOGY

Novel GPCR paradigms at the μ-opioid receptor

(2014) G L Thompson et al.   BRITISH JOURNAL OF PHARMACOLOGY

Biased ligands: pathway validation for novel GPCR therapeutics

(2014) David H Rominger et al.   CURRENT OPINION IN PHARMACOLOGY

Cathepsin S Causes Inflammatory PainviaBiased Agonism of PAR2and TRPV4

(2014) Peishen Zhao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Emerging structural insights into biased GPCR signaling

(2014) Arun K. Shukla et al.   TRENDS IN BIOCHEMICAL SCIENCES

Biased signalling and proteinase-activated receptors (PARs): targeting inflammatory disease

(2013) M D Hollenberg et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

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

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

The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands

(2013) Adam J. Pawson et al.   NUCLEIC ACIDS RESEARCH

Co-Expression of GRK2 Reveals a Novel Conformational State of the µ-Opioid Receptor

(2013) Sarah A. Nickolls et al.   PLoS One

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

(2012) Terry Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

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

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

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

(2011) Terry Kenakin et al.   ACS Chemical Neuroscience

Quantifying Ligand Bias at Seven-Transmembrane Receptors

(2011) S. Rajagopal et al.   MOLECULAR PHARMACOLOGY

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

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

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