Current concepts and treatments of schizophrenia

P Stępnicki, M Kondej, AA Kaczor - Molecules, 2018 - mdpi.com
Schizophrenia is a debilitating mental illness which involves three groups of symptoms, ie,
positive, negative and cognitive, and has major public health implications. According to …

Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …

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 …

[HTML][HTML] 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 …

Psychedelics

DE Nichols - Pharmacological reviews, 2016 - Elsevier
Psychedelics (serotonergic hallucinogens) are powerful psychoactive substances that alter
perception and mood and affect numerous cognitive processes. They are generally …

How ligands illuminate GPCR molecular pharmacology

D Wacker, RC Stevens, BL Roth - Cell, 2017 - cell.com
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and
synthetic ligands, represent the largest family of druggable targets in the human genome …

Bias factor and therapeutic window correlate to predict safer opioid analgesics

CL Schmid, NM Kennedy, NC Ross, KM Lovell, Z Yue… - Cell, 2017 - cell.com
Biased agonism has been proposed as a means to separate desirable and adverse drug
responses downstream of G protein-coupled receptor (GPCR) targets. Herein, we describe …

Psychedelics in psychiatry: neuroplastic, immunomodulatory, and neurotransmitter mechanisms

A Inserra, D De Gregorio, G Gobbi - Pharmacological Reviews, 2021 - Elsevier
Mounting evidence suggests safety and efficacy of psychedelic compounds as potential
novel therapeutics in psychiatry. Ketamine has been approved by the Food and Drug …

[HTML][HTML] Crystal structure of an LSD-bound human serotonin receptor

D Wacker, S Wang, JD McCorvy, RM Betz… - Cell, 2017 - cell.com
The prototypical hallucinogen LSD acts via serotonin receptors, and here we describe the
crystal structure of LSD in complex with the human serotonin receptor 5-HT 2B. The complex …

Structure of the nanobody-stabilized active state of the kappa opioid receptor

T Che, S Majumdar, SA Zaidi, P Ondachi, JD McCorvy… - Cell, 2018 - cell.com
The κ-opioid receptor (KOP) mediates the actions of opioids with hallucinogenic, dysphoric,
and analgesic activities. The design of KOP analgesics devoid of hallucinatory and …