β− Arrestins: structure, function, physiology, and pharmacological perspectives

J Wess, AB Oteng, O Rivera-Gonzalez… - Pharmacological …, 2023 - ASPET
The two β-arrestins, β-arrestin-1 and-2 (systematic names: arrestin-2 and-3, respectively),
are multifunctional intracellular proteins that regulate the activity of a very large number of …

Biased receptor signaling in drug discovery

T Kenakin - Pharmacological reviews, 2019 - ASPET
A great deal of experimental evidence suggests that ligands can stabilize different receptor
active states that go on to interact with cellular signaling proteins to form a range of different …

Structure of the δ-opioid receptor bound to naltrindole

S Granier, A Manglik, AC Kruse, TS Kobilka, FS Thian… - Nature, 2012 - nature.com
The opioid receptor family comprises three members, the µ-, δ-and κ-opioid receptors, which
respond to classical opioid alkaloids such as morphine and heroin as well as to …

Opioid receptors: distinct roles in mood disorders

PE Lutz, BL Kieffer - Trends in neurosciences, 2013 - cell.com
The roles of opioid receptors in pain and addiction have been extensively studied, but their
function in mood disorders has received less attention. Accumulating evidence from animal …

Biased agonism: lessons from studies of opioid receptor agonists

E Kelly, A Conibear, G Henderson - Annual review of …, 2023 - annualreviews.org
In ligand bias different agonist drugs are thought to produce distinct signaling outputs when
activating the same receptor. If these signaling outputs mediate therapeutic versus adverse …

Historical review: opiate addiction and opioid receptors

S Wang - Cell transplantation, 2019 - journals.sagepub.com
Substance use disorders (SUDs), defined as a collection of symptoms including tolerance
and withdrawal, are chronic illnesses characterized by relapse and remission. In the United …

Opioid receptors: drivers to addiction?

E Darcq, BL Kieffer - Nature Reviews Neuroscience, 2018 - nature.com
Drug addiction is a worldwide societal problem and public health burden, and results from
recreational drug use that develops into a complex brain disorder. The opioid system, one of …

[HTML][HTML] A mu–delta opioid receptor brain atlas reveals neuronal co-occurrence in subcortical networks

E Erbs, L Faget, G Scherrer, A Matifas, D Filliol… - Brain Structure and …, 2015 - Springer
Opioid receptors are G protein-coupled receptors (GPCRs) that modulate brain function at
all levels of neural integration, including autonomic, sensory, emotional and cognitive …

[HTML][HTML] Biased opioid ligands

A Faouzi, BR Varga, S Majumdar - Molecules, 2020 - mdpi.com
Achieving effective pain management is one of the major challenges associated with
modern day medicine. Opioids, such as morphine, have been the reference treatment for …

[HTML][HTML] The kappa opioid receptor: from addiction to depression, and back

L Lalanne, G Ayranci, BL Kieffer, PE Lutz - Frontiers in psychiatry, 2014 - frontiersin.org
Comorbidity is a major issue in psychiatry that notably associates with more severe
symptoms, longer illness duration, and higher service utilization. Therefore, identifying key …