The neural basis of psychedelic action

AC Kwan, DE Olson, KH Preller, BL Roth - Nature Neuroscience, 2022 - nature.com
Psychedelics are serotonin 2A receptor agonists that can lead to profound changes in
perception, cognition and mood. In this review, we focus on the basic neurobiology …

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 …

Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity

AL Kaplan, DN Confair, K Kim, X Barros-Álvarez… - Nature, 2022 - nature.com
There is considerable interest in screening ultralarge chemical libraries for ligand discovery,
both empirically and computationally,,–. Efforts have focused on readily synthesizable …

Structure-based discovery of nonhallucinogenic psychedelic analogs

D Cao, J Yu, H Wang, Z Luo, X Liu, L He, J Qi, L Fan… - Science, 2022 - science.org
Drugs that target the human serotonin 2A receptor (5-HT2AR) are used to treat
neuropsychiatric diseases; however, many have hallucinogenic effects, hampering their use …

[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 …

Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD

C Cao, X Barros-Álvarez, S Zhang, K Kim, MA Dämgen… - Neuron, 2022 - cell.com
Summary Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …

Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential

J Wallach, AB Cao, MM Calkins, AJ Heim… - Nature …, 2023 - nature.com
Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT2A
receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5 …

Molecular dynamics simulation for all

SA Hollingsworth, RO Dror - Neuron, 2018 - cell.com
The impact of molecular dynamics (MD) simulations in molecular biology and drug discovery
has expanded dramatically in recent years. These simulations capture the behavior of …

TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome

RHJ Olsen, JF DiBerto, JG English, AM Glaudin… - Nature chemical …, 2020 - nature.com
G-protein-coupled receptors (GPCRs) remain major drug targets, despite our incomplete
understanding of how they signal through 16 non-visual G-protein signal transducers …

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 …