Identification of psychedelic new psychoactive substances (NPS) showing biased agonism at the 5-HT2AR through simultaneous use of β-arrestin 2 and miniGαq bioassays

Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists

(2020) Alexander Gillis et al.   Science Signaling

In vitro functional characterization of a panel of non-fentanyl opioid new psychoactive substances

(2020) Marthe M. Vandeputte et al.   ARCHIVES OF TOXICOLOGY

Assessment of biased agonism at the A3 adenosine receptor using β-arrestin and miniGαi recruitment assays

(2020) Eline Pottie et al.   BIOCHEMICAL PHARMACOLOGY

Assessment of structure-activity relationships and biased agonism at the Mu opioid receptor of novel synthetic opioids using a novel, stable bio-assay platform

(2020) Lakshmi Vasudevan et al.   BIOCHEMICAL PHARMACOLOGY

Structure of a Hallucinogen-Activated Gq-Coupled 5-HT2A Serotonin Receptor

(2020) Kuglae Kim et al.   CELL

Biased Receptor Signaling in Drug Discovery

(2019) Terry Kenakin   PHARMACOLOGICAL REVIEWS

DARK Classics in Chemical Neuroscience: NBOMes

(2019) Christian B. M. Poulie et al.   ACS Chemical Neuroscience

Setup of a Serotonin 2A Receptor (5-HT2AR) Bioassay: Demonstration of Its Applicability To Functionally Characterize Hallucinogenic New Psychoactive Substances and an Explanation Why 5-HT2AR Bioassays Are Not Suited for Universal Activity-Based Screening of Biofluids for New Psychoactive Substances

(2019) Eline Pottie et al.   ANALYTICAL CHEMISTRY

Insights into biased signaling at cannabinoid receptors: synthetic cannabinoid receptor agonists

(2019) Elise Wouters et al.   BIOCHEMICAL PHARMACOLOGY

Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells

(2018) Qingwen Wan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure–Functional Selectivity Relationships (SFSRs) and Therapeutic Potential

(2018) Liang Tan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Comparison of the behavioral responses induced by phenylalkylamine hallucinogens and their tetrahydrobenzodifuran (“FLY”) and benzodifuran (“DragonFLY”) analogs

(2018) Adam L. Halberstadt et al.   NEUROPHARMACOLOGY

A kinetic view of GPCR allostery and biased agonism

(2017) J Robert Lane et al.   Nature Chemical Biology

Psychedelic Drugs in Biomedicine

(2017) Evan J. Kyzar et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Mini-G proteins: Novel tools for studying GPCRs in their active conformation

(2017) Rony Nehmé et al.   PLoS One

Detection and Activity Profiling of Synthetic Cannabinoids and Their Metabolites with a Newly Developed Bioassay

(2016) Annelies Cannaert et al.   ANALYTICAL CHEMISTRY

Psychedelics as Medicines: An Emerging New Paradigm

(2016) DE Nichols et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

NanoLuc Complementation Reporter Optimized for Accurate Measurement of Protein Interactions in Cells

(2015) Andrew S. Dixon et al.   ACS Chemical Biology

Structure and function of serotonin G protein-coupled receptors

(2015) John D. McCorvy et al.   PHARMACOLOGY & THERAPEUTICS

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

Quantitative Phosphoproteomics Unravels Biased Phosphorylation of Serotonin 2A Receptor at Ser280by HallucinogenicversusNonhallucinogenic Agonists

(2014) Samah Karaki et al.   MOLECULAR & CELLULAR PROTEOMICS

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

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

Heterocomplex formation of 5-HT2A-mGlu2 and its relevance for cellular signaling cascades

(2012) Hannah K. Delille et al.   NEUROPHARMACOLOGY

Quantifying Ligand Bias at Seven-Transmembrane Receptors

(2011) S. Rajagopal et al.   MOLECULAR PHARMACOLOGY

Serotonin receptor signaling and regulation via β-arrestins

(2010) Laura M. Bohn et al.   CRITICAL REVIEWS IN BIOCHEMISTRY AND MOLECULAR BIOLOGY

Serotonin, But Not N-Methyltryptamines, Activates the Serotonin 2A Receptor Via a  -Arrestin2/Src/Akt Signaling Complex In Vivo

(2010) C. L. Schmid et al.   JOURNAL OF NEUROSCIENCE

Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells

(2008) Didier Cussac et al.   EUROPEAN JOURNAL OF 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

Structure and Function of the Third Intracellular Loop of the 5-Hydroxytryptamine2A Receptor: The Third Intracellular Loop Is α-Helical and Binds Purified Arrestins

(2003) Edward I. Gelber et al.   JOURNAL OF NEUROCHEMISTRY