Conformational cross-talk between α2A-adrenergic and μ-opioid receptors controls cell signaling

JP Vilardaga, VO Nikolaev, K Lorenz… - Nature chemical …, 2008 - nature.com
Morphine, a powerful analgesic, and norepinephrine, the principal neurotransmitter of
sympathetic nerves, exert major inhibitory effects on both peripheral and brain neurons by …

Single-molecule analysis reveals agonist-specific dimer formation of µ-opioid receptors

J Möller, A Isbilir, T Sungkaworn, B Osberg… - Nature Chemical …, 2020 - nature.com
G-protein-coupled receptors (GPCRs) are key signaling proteins that mostly function as
monomers, but for several receptors constitutive dimer formation has been described and in …

Propagation of conformational changes during μ-opioid receptor activation

R Sounier, C Mas, J Steyaert, T Laeremans, A Manglik… - Nature, 2015 - nature.com
Abstract µ-Opioid receptors (µORs) are G-protein-coupled receptors that are activated by a
structurally diverse spectrum of natural and synthetic agonists including endogenous …

Structure of the µ-opioid receptor–Gi protein complex

A Koehl, H Hu, S Maeda, Y Zhang, Q Qu, JM Paggi… - Nature, 2018 - nature.com
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most
clinically and recreationally used opioids. The induced positive effects of analgesia and …

Molecular control of δ-opioid receptor signalling

G Fenalti, PM Giguere, V Katritch, XP Huang… - Nature, 2014 - nature.com
Opioids represent widely prescribed and abused medications, although their signal
transduction mechanisms are not well understood. Here we present the 1.8 Å high …

Identification of a μ-δ opioid receptor heteromer-biased agonist with antinociceptive activity

I Gomes, W Fujita, A Gupta… - Proceedings of the …, 2013 - National Acad Sciences
G protein-coupled receptors play a pivotal role in many physiological signaling pathways.
Mounting evidence suggests that G protein-coupled receptors, including opioid receptors …

Role for G protein-coupled receptor kinase in agonist-specific regulation of μ-opioid receptor responsiveness

J Zhang, SSG Ferguson, LS Barak… - Proceedings of the …, 1998 - National Acad Sciences
The G protein-coupled μ-opioid receptor (μOR) mediates the physiological effects of
endogenous opioid peptides as well as the structurally distinct opioid alkaloids morphine …

Functional interactions between μ opioid and α2A-adrenergic receptors

BA Jordan, I Gomes, C Rios, J Filipovska… - Molecular pharmacology, 2003 - ASPET
Adrenergic and opioid receptors belong to the rhodopsin family of G-protein coupled
receptors, couple to analogous signal transduction pathways, and affect the nociceptive …

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

A Manglik, AC Kruse, TS Kobilka, FS Thian… - Nature, 2012 - nature.com
Opium is one of the world's oldest drugs, and its derivatives morphine and codeine are
among the most used clinical drugs to relieve severe pain. These prototypical opioids …

Plasma membrane localization of the μ-opioid receptor controls spatiotemporal signaling

ML Halls, HR Yeatman, CJ Nowell, GL Thompson… - Science …, 2016 - science.org
Differential regulation of the μ-opioid receptor (MOR), a G protein (heterotrimeric guanine
nucleotide–binding protein)–coupled receptor, contributes to the clinically limiting effects of …