The promises and perils of psychedelic pharmacology for psychiatry

TD McClure-Begley, BL Roth - Nature Reviews Drug Discovery, 2022 - nature.com
Psychedelic drugs including psilocybin, N, N ʹ-dimethyltryptamine (DMT) and lysergic acid
diethylamide (LSD) are undergoing a renaissance as potentially useful drugs for various …

Mechanisms of signalling and biased agonism in G protein-coupled receptors

D Wootten, A Christopoulos, M Marti-Solano… - … reviews Molecular cell …, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …

Molecular recognition of morphine and fentanyl by the human μ-opioid receptor

Y Zhuang, Y Wang, B He, X He, XE Zhou, S Guo… - Cell, 2022 - cell.com
Morphine and fentanyl are among the most used opioid drugs that confer analgesia and
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …

[HTML][HTML] Structure of a hallucinogen-activated Gq-coupled 5-HT2A serotonin receptor

K Kim, T Che, O Panova, JF DiBerto, J Lyu, BE Krumm… - Cell, 2020 - cell.com
Hallucinogens like lysergic acid diethylamide (LSD), psilocybin, and substituted N-benzyl
phenylalkylamines are widely used recreationally with psilocybin being considered as a …

Structure, function and pharmacology of human itch GPCRs

C Cao, HJ Kang, I Singh, H Chen, C Zhang, W Ye… - Nature, 2021 - nature.com
The MRGPRX family of receptors (MRGPRX1–4) is a family of mas-related G-protein-
coupled receptors that have evolved relatively recently. Of these, MRGPRX2 and MRGPRX4 …

Structures of the entire human opioid receptor family

Y Wang, Y Zhuang, JF DiBerto, XE Zhou, GP Schmitz… - Cell, 2023 - cell.com
Opioids are effective analgesics, but their use is beset by serious side effects, including
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

Molecular mechanism of biased signaling at the kappa opioid receptor

A El Daibani, JM Paggi, K Kim, YD Laloudakis… - Nature …, 2023 - nature.com
The κ-opioid receptor (KOR) has emerged as an attractive drug target for pain management
without addiction, and biased signaling through particular pathways of KOR may be key to …

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 …

Untangling the complexity of opioid receptor function

RJ Valentino, ND Volkow - Neuropsychopharmacology, 2018 - nature.com
Mu opioid receptor agonists are among the most powerful analgesic medications but also
among the most addictive. The current opioid crisis has energized a quest to develop opioid …