Cited by 481Receptor Mechanisms and SignalingPsychedelics and Drug StudiesNeuroscience and Neuropharmacology Research

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Structure of a Hallucinogen-Activated Gq-Coupled 5-HT2A Serotonin Receptor

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Kim, Kuglae, Che, Tao, Panova, Ouliana, DiBerto, Jeffrey F., Lyu, Jiankun, Krumm, Brian E., Wacker, Daniel, Robertson, Michael J., Seven, Alpay B., Nichols, David E., Shoichet, Brian K., Skiniotis, Georgios, Roth, Bryan L.·2020·Cell

DOI 10.1016/j.cell.2020.08.024PMC PMC7593816

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Abstract

Hallucinogens like lysergic acid diethylamide (LSD), psilocybin, and substituted N-benzyl phenylalkylamines are widely used recreationally with psilocybin being considered as a therapeutic for many neuropsychiatric disorders including depression, anxiety, and substance abuse. How psychedelics mediate their actions-both therapeutic and hallucinogenic-are not understood, although activation of the 5-HT 2A serotonin receptor (HTR2A) is key. To gain molecular insights into psychedelic actions, we determined the active-state structure of HTR2A bound to 25-CN-NBOH-a prototypical hallucinogen-in complex with an engineered Gαq heterotrimer by cryoelectron microscopy (cryo-EM). We also obtained the X-ray crystal structures of HTR2A complexed with the arrestin-biased ligand LSD or the inverse agonist methiothepin. Comparisons of these structures reveal determinants responsible for HTR2A-Gαq protein interactions as well as the conformational rearrangements involved in active-state transitions. Given the potential therapeutic actions of hallucinogens, these findings could accelerate the discovery of more selective drugs for the treatment of a variety of neuropsychiatric disorders.

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Authors: Kim, K., Che, T., Panova, O., DiBerto, J. F., Lyu, J., Krumm, B. E., Wacker, D., Robertson, M. J., Seven, A. B., Nichols, D. E., Shoichet, B. K., Skiniotis, G., & Roth, B. L.
Affiliations: University of North Carolina at Chapel Hill (US)
Stanford Medicine (US)
University of California, San Francisco (US)
Corresponding author: Skiniotis, Georgios
Roth, Bryan L.
ORCID: Kim, Kuglae
Che, Tao
Panova, Ouliana
DiBerto, Jeffrey F.
Lyu, Jiankun
Wacker, Daniel
Seven, Alpay B.
Nichols, David E.
Shoichet, Brian K.
Skiniotis, Georgios
Roth, Bryan L.
Venue: Cell
Publisher: Elsevier BV
Published: 2020-09
Volume: 182
Issue: 6
Pages: 1574-1588.e19
ISSN: 0092-8674 (ISSN-L)
DOI: 10.1016/j.cell.2020.08.024
PMC: PMC7593816
OpenAlex: W3086773311
Cited by: 481
References: 91
Citations by year: 2026: 59 · 2025: 92 · 2024: 86 · 2023: 88 · 2022: 76 · 2021: 72 · 2020: 6
FWCI: 19.70
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 381 d)
Locations: Cell (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
eScholarship (California Digital Library) (submittedVersion)
OSTI OAI (U.S. Department of Energy Office of Scientific and Technical Information) (submittedVersion)
Funders: National Institute on Drug Abuse
National Institute of Mental Health
National Institutes of Health (R37DA04567, R01MH112205)
Argonne National Laboratory (DE-AC02-06CH11357)
National Institute of General Medical Sciences (AGM-12006)
National Cancer Institute (ACB-12002, P30CA016086)
Defense Advanced Research Projects Agency (HR0011-20-2-0029, R35GM122481)
Office of Science
U.S. Department of Defense
National Research Foundation of Korea (2017R1A6A3A03012547)
University of North Carolina
U.S. Department of Energy
Government of South Australia
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Social Sciences › Psychology › Clinical Psychology › Psychedelics and Drug Studies
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords: 5-HT2A receptor, hallucinogens, LSD, psilocybin, receptor-G protein complex, methiothepin, inverse agonists, neuropsychiatric disorders
MeSH terms: Protein Conformation, alpha-Helical, Animals, Hallucinogens, Humans, Ligands, Lysergic Acid Diethylamide, Methiothepin, Models, Chemical, Mutation, Recombinant Proteins, Serotonin, Gene Expression, Crystallography, X-Ray, Spodoptera, Cryoelectron Microscopy, GTP-Binding Protein alpha Subunits, Gq-G11, Receptor, Serotonin, 5-HT2A, HEK293 Cells

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Structure of a Hallucinogen-Activated Gq-Coupled 5-HT2A Serotonin Receptor

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