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

Kim, Kuglae, Che, Tao, Panova, Ouliana, DiBerto, Jeffrey F., Lyu, Jiankun, Krumm, Brian E., Wacker, Daniel, Robertson, Michael J. +5 more·2020·Cell

DOI 10.1016/j.cell.2020.08.024

Cited by (475)

Items 401–475 of 475

Reviewer #3 (Public Review): Cryo-EM structure of the bicarbonate receptor GPR30
Shota Kaneda, Airi Jo-Watanabe, Hiroaki Akasaka · 2024 · eLife
Reviewer #1 (Public Review): Cryo-EM structure of the bicarbonate receptor GPR30
Shota Kaneda, Airi Jo-Watanabe, Hiroaki Akasaka · 2024 · eLife
Reviewer #2 (Public Review): Cryo-EM structure of the bicarbonate receptor GPR30
Shota Kaneda, Airi Jo-Watanabe, Hiroaki Akasaka · 2024 · eLife
Psychedelics: a window into perceptual processing
Berit “Brit” Brogaard, Dimitria Electra Gatzia · 2024 · Oxford University Press eBooks
Letzte Geheimnisse des Roten Keulenkopfs und seiner Inhaltsstoffe werden ans Licht gebracht
Frank Petersen · 2024 · Springer eBooks
CNS Biased Agonism and the Promise of Targeting Drugs Beyond Receptors to Cellular Pathways
Laurence M. Melnick · 2024 · Springer eBooks
Unlocking the Therapeutic Potential of DMT’s: Molecular Modelling Insights into Nueropharmacological Mechanisms and Clinical Prospects
2024 · Letters in Applied NanoBioScience
Helix-8 and Carboxyl Terminal Tail Regulation of Proteinase Activated Receptor-4 (PAR4) signalling
Pierre E. Thibeault, Amr A. K. Mousa, Victor Michael Mirka, Rithwik Ramachandran · 2025 · bioRxiv (Cold Spring Harbor Laboratory)
Molecular Insight into the Interaction between Different Classes of Psychoplastogens and Serotonin 5-HT2A Receptor
David Nisenboim · 2025 · International Journal of Science and Research (IJSR)
Last secrets of ergot and its ingredients are revealed
Frank Petersen · 2025 · Springer eBooks
Divergent activation patterns of BRS3 revealed by two Chinese herb-derived agonists
Jie Li, Changyao Li, Qingtong Zhou, Wei Han, Mingzhu Fang, Youwei Xu, Yiting Mai, Yao Zhang, Jiahua Cui, H. Eric Xu et al. · 2025 · Acta Pharmaceutica Sinica B
Effects of three tryptamines: alpha-methyltryptamine, 5-methoxy-alpha-methyltryptamine, and 5-methoxy-N,N-diisopropyltryptamine on acute toxicity, locomotor activity, and hallucinogenic behavior in mice
Kaixi Li, Nan Li, Yuanyuan Chen, Xiangyu Li, Yanling Qiao, Dan Wang, Bin Di, Peng Xu · 2025 · Behavioural Pharmacology
Binding pose depth modulates photoswitchable ligands’ efficacy at the 5-HT2A receptor
Verena Weber, Giacomo Salvadori, Federico Natale, Hubert Gerwe, Michael W. Decker, Paolo Carloni, Giulia Rossetti · 2026 · Communications Chemistry
Psychedelics’ Intoxicating Impact and Behavioural Dynamics
Afshan Zeeshan Wasti · 2025 · Pharmaceutical science.
Psychedelic-Assisted Therapy for Anorexia Nervosa
Olga Stefańska, Maksymilian Matuszewski · 2024 · Journal of Student Research
Psychedelics for the Treatment of Substance Use Disorder
Berta Fumàs, David Pubill, Raúl López‐Arnau, Núria Nadal‐Gratacós · 2025 · Pharmaceutical science.
A Comparative Neurophenomenology of the Psychedelic State and Autism: Predictive Processing as a Unifying Lens
William Roseby, Catriona Osborn Moar · 2025 · Psychoactives
Structural insights into the G-protein subtype selectivity revealed by human sphingosine-1-phosphate receptor 3–G q complexes
Momono Yamauchi, Dohyun Im, Shintaro Maeda, Tatsuya Ikuta, Masayasu Toyomoto, Hidetsugu Asada, Yukihiko Sugita, Jun-ichi Kishikawa, Takeshi Noda, Takayuki Kato et al. · 2025 · Proceedings of the National Academy of Sciences
Association of Hallucinogen Use With Psychosocial Outcomes: Secondary Analysis of the Spinal Cord Injury Model Systems Database
Kayleigh Crane, Angela Hanks Philippus, Jennifer L. Coker, Jesse L. Kowalski, Kimberley R. Monden · 2025 · Topics in Spinal Cord Injury Rehabilitation
To Be Biased or Not to Be: A Play for G-Protein Coupled Receptors
Nikitas G. Liolitsas, Evangelia Pantazaka, Εvangelia Papadimitriou · 2025 · International Journal of Translational Medicine
Acute Blockade of the Serotonin Transporter With Low Doses of Escitalopram Does Not Alter the Behavioural Responses to Acute Psilocybin
Nina Kleditzsch, James J Gattuso, Anthony John Hannan, Thibault Renoir · 2025 · European Journal of Neuroscience
Cryo-EM structure of the bicarbonate receptor GPR30
Shota Kaneda, Airi Jo‐Watanabe, Hiroaki Akasaka, Hidetaka S. Oshima, Takehiko Yokomizo, Wataru Shihoya, Osamu Nureki · 2025 · eLife
Role of Neuronal Cholecystokinin Receptor: An Emerging Therapeutic Target for Ameliorating Neurological Diseases
Fengwen Huang, Stephen Temitayo Bello · 2025 · Molecular Neurobiology
Molecular insights into ago-allosteric modulation at cysteinyl leukotriene receptor 2
Mu Li, Xiaoling Bao, Wanbiao Chen, Yusheng Guo, Xiaomin Mao, Miaofang Xiao, Siqi Liu, Jiawei Li, Limin Zhao, Tiancai Chang et al. · 2025 · Nature Communications
Bioproduction platform using a novel cane toad (Rhinella marina) N-methyltransferase for psychedelic-inspired drug discovery
Xue Chen, Jing Li, Lisa X Yu, D. Dhananjaya, Francesca Maule, Sarah G. Cook, Limei Chang, Jonathan Gallant, David Press, Jaideep S Bains et al. · 2023 · Research Square
‘Shrooms for the Blues: Psilocybin to alleviate difficult-to-treat depression
Zoe Graham · 2022 · Journal of High School Science
De Novo Drug Design for Antipsychotics: A Case Study with Llama 3.2 1B
Harshit, Mayank Bhasin · 2025 · Lecture notes in social networks
A structural overview of G-protein-coupled receptors in neurological disorders
Oindrilla Dutta Gupta, Indranil Chakraborty, Kuntal Pal · 2026 · Acta Pharmacologica Sinica
Structural analysis reveals that water molecules mediate self-activation of GPR99
Miaofang Xiao, Xiaoling Bao, Yusheng Guo, Jiawei Li, Tiancai Chang, Fumei Zhong, Xiaomin Mao, Mu Li, Siqi Liu, Wanbiao Chen et al. · 2026 · Communications Biology
Antidepressant-Like Effects of n-Butylidenephthalide Using In Vivo and In Silico Approaches
Maria L. González-Rivera, María del Carmen Juárez-Vázquez, Athzirys Alejandra Melecio-Hernández, Diana Casique‐Aguirre, Gabriela Josefina López-González, Ramsés Maximiliano Ramírez-Martínez, Andrea Ayala-Torres, Yurisleidys Quesada-Mendiola, Juan Ramón Zapata‐Morales, Ángel Josabad Alonso‐Castro · 2026 · Pharmaceuticals
Targeting serotonin 5-HT2A receptors in the treatment of aggression: From antipsychotics to psychedelics
Simona Scheggi, Giulia Braccagni, Caterina Branca, Marco Bortolato · 2026 · Aggression and Violent Behavior
Rewiring Receptor Activation: Mechanistic Insights into Toggle Switch Modulation by 25CN-NBx Compounds
Vito F. Palmisano, Micaela Vidal−Sánchez, Juan José Nogueira · 2026 · ACS Chemical Neuroscience
Structural and dynamic insights into agonist recognition and function of the thromboxane A2 receptor
Pawel Krawinski, Donna Matzov, Aoife Ryder, Kanhaya Lal, Dmitry S. Karlov, Georges Chalhoub, Eamon P. Mulvaney, B. Therese Kinsella, Peter James McCormick, Martin Caffrey et al. · 2026 · Nature Communications
Trip killers: Addressing a critical knowledge gap in psychedelic research
Brian William O’Mahony, Colm Harrington, Andrew Harkin, Níall Lally · 2026 · Journal of Psychopharmacology
Advances in Target Identification and Drug Development for Depression
Kaixuan Hu, Xinmin Wang, Wentong Yu, Qiyue Liu, Yan Cheng, Yuting Song, Li Liang, Wei Liu, Junping Zhang, Shan Chang et al. · 2026 · Current Drug Targets
Structural insight into ligand binding and activation of the orphan GPCR Mas1
Yumu Zhang, Qiuying Wang, Heng Liu, Hong Shan, Yimin Gu, Jiaqi Yang, Yuan Gao, Kai Wu, Dehua Yang, H. Eric Xu · 2026 · The EMBO Journal
Optimizing cognitive enhancement through dopamine transporter modulation
Marco Niello, Predrag Kalaba, Anita Cybulska-Kłosowicz, Michael Kirchhofer, Iva Spreitzer, Markus Spreitzer, Judith Wackerlig, Michele Santoni, Claudia Sagheddu, Simone B. Sartori et al. · 2026 · Neuropharmacology
Decoding the structure of GPR151 via NELiS
Yumeng Wang, Luyu Fan, Qianqian Song, Yaning Li, Jiayu Jin, Qiaoyu Zhao, Weijie Gu, Xiangyi Shi, Dianfan Li, Yao Cong et al. · 2026 · Proceedings of the National Academy of Sciences
Cryo-EM structure of the bicarbonate receptor GPR30
Shota Kaneda, Airi Jo‐Watanabe, Hiroaki Akasaka, Hidetaka S. Oshima, Takehiko Yokomizo, Wataru Shihoya, Osamu Nureki · 2026 · eLife
LSD persistently disrupts affective pain processing
Jared Plotkin, Elaine Zhu, Mélanie Druart, Qiaosheng Zhang, Eric Hu, Deven Cathcart, Nellie Jun, Leo Kwok, Tanya Sippy, Jing Wang · 2026 · bioRxiv (Cold Spring Harbor Laboratory)
Multiscale Simulation Approaches to Probe Lipid Interactions of G Protein-Coupled Receptors
Durba Sengupta, Shalmali Kharche, Aditya Manoj, Amit Naglekar, Amitabha Chattopadhyay · 2026 · Methods in molecular biology
Enhancing structure-based drug‒target interaction prediction via electron-density map-informed conformation optimization
Rui Li, Qinyu Chu, X He, Jian Zhang, Xi Cheng · 2026 · Acta Pharmaceutica Sinica B
Antidepressant effect of psychedelic compounds and mechanisms underlying the G protein-coupled receptors activation psychedelics: Antidepressant action and GPCR signaling
Amanda Gollo Bertollo, Vinícius Alexandre Wippel, Maiqueli Eduarda Dama Mingoti, Rui Daniel Prediger, Zuleide Maria Ignácio · 2026 · European Journal of Pharmacology
Analyses of orphan GPCRs’ function in the pathogenesis of sepsis and their small-molecule therapeutics
Yibing Wang, Yining Lin · 2026 · Biochemical Pharmacology
MFCC–DFT mapping of ligand recognition at the 5-HT 2A receptor: energetic analysis of the interactions between serotonin, psychedelics, and antipsychotics
Washington Sales Clemente, Katyanna Sales Bezerra, E. G. C. Matias, J J de Oliveira, Umberto Laino Fulco · 2026 · Physical Chemistry Chemical Physics
Evaluation of Neurotoxicity of NBOH Derivatives
Rodrigo Foss da Silva, Lennon Machado Alves, Fernanda Mocellin Conte, Bruno Pereira dos Santos, Rodrigo Ligabue‐Braun, Solange Cristina García, Tiago Franco de Oliveira, Hecson Jesser Segat, Silvana Peterini Boeira, Dieniffer Espinosa Janner et al. · 2026 · Pharmaceuticals
In silico characterization of Desmodium gangeticum compounds as dual modulators of MAO-B and 5-HT2A in Parkinson’s disease: an integrated approach combining molecular docking, ADMET profiling, MM-GBSA, QSAR modeling, and molecular dynamics simulation
Oluwabusayo Esther Akinma, O. S. Akinola, Ifeoluwa Deborah OJO, Akinyode Isaac Olopoda, Ifedayo David Akerele, Bright Bayonle Akinyemi, Folashade Ayodeji, Olusola Olalekan Elekofehinti · 2026 · In Silico Pharmacology
Design of a new psychedelic quipazine analog with therapeutic efficacy and potentially fewer side effects
Jason Younkin, Ajay H. Bansode, Somdatta Saha, Archana Paymode, Jessica L. Maltman, Charles B. Jones, Justin M. Silverman, Belle Buzzi, Alaina M. Jaster, Michael Fiorillo et al. · 2026 · Science Signaling
Striatal Dopamine D2 Receptors Contribute to N-Ethylpentylone-Induced Arousal in Mice
Cheng-Teng Fan, Jingya Wang, Hong Qian, Shang-Qi Tang, Zhi-Gang Zhong, Yu‐Rong Zhang, Shui-Qing Zheng, Mei‐Hong Qiu, Yu-Lan Rao, Zhi-ru Xu · 2026 · Neurochemical Research
Reviewer #3 (Public review): Cryo-EM structure of the bicarbonate receptor GPR30
2026 · eLife
Reviewer #2 (Public review): Cryo-EM structure of the bicarbonate receptor GPR30
2026 · eLife
Membrane Mimetic-Thermal Proteome Profiling Reveals Broad, Sequence-Independent Membrane Protein Stabilization by Cholesteryl Hemisuccinate
Ashim Bhattacharya, Shamus Clunie, Frank Antony, Yilun Chen, Hiroyuki Aoki, Mohan Babu, Franck Duong · 2026 · bioRxiv (Cold Spring Harbor Laboratory)
G Protein-Mediated Allosteric Modulation of Ligand Binding in Class A GPCRs: Receptor–Ligand–Transducer Ensembles in Disease and Drug Discovery
Yukiko Kurihara, Hiroki Kurihara · 2026 · Pharmaceuticals
A signaling signature distinguishes hallucinogenic from non-hallucinogenic psychedelics
Sandra M. Martin-Guerrero, Marco Taddei-Tardon, Jessica L. Maltman, Sritanvi Potukanuma, Javier González‐Maeso, Pedro R. Cutillas, Juan F. López‐Giménez · 2026 · Translational Psychiatry
Deconstruction of lysergic acid diethylamide
Andrian G. Basargin, Andras Domokos, Joseph J. Hennessey, Isak K. Aarrestad, Rohini Sambyal, Yara A. Khatib, Johanna Krüger, Lee E. Dunlap, Samuel J. Carter, Isabella A. Rebek et al. · 2026 · Proceedings of the National Academy of Sciences
Next-Generation Psychedelic Drug Development
Lindsay P. Cameron, Matthew W. Johnson, Kevin Sean Murnane, Mark M. Rasenick, Charles David Nichols · 2026 · ACS Chemical Neuroscience
Bias from within: intracellular allosterism and the ICL2 hub
Yang Zhou, Alan Long, Joshua D. Gross, Larry S. Barak, Alem W. Kahsai · 2026 · Trends in Pharmacological Sciences
Mechanistic Basis for 5-HT2AR Over 5-HT2BR Activation
Lingjie Tang, Xin Ji, Yumeng Wang, Dongmei Cao, Huiqiong Li, Licong He, Jianjun Cheng, Sheng Wang · 2026 · Nature Communications
Structure-based design of subtype-selective psychedelic analogs
Huiqiong Li, Lingjie Tang, Jinfeng Zhang, Bing Meng, Dongmei Cao, Yujin Chen, Jing Hua Yu, Huan Wang, Zhi‐Jie Liu, Sheng Wang et al. · 2026 · Nature Communications
Deciphering the allosteric landscape of 5-HT2 receptors: integrated molecular dynamics and fragment molecular orbital analyses of activation mechanisms
Paweł Śliwa, Karina Pakosz, Aleksandra Banach · 2026 · Pharmacological Reports
On the Structural Precision Required for Ligand-Specific Elastic Network Dynamics of AI Co-Folded GPCR Structures
Benjamin R. Cummins, Christina G. Fragel, Joyita Faruk · 2026 · Receptors
Structural Basis for Angiotensin II Type I Receptor G Protein-biased Signaling
刘静涵, Meredith A. Skiba, Andrew Kruse · 2026 · bioRxiv (Cold Spring Harbor Laboratory)
Gi Signaling Does Not Differentiate Hallucinogenic from Nonhallucinogenic 5-HT2A Receptor Agonists
Cassandra J. Hatzipantelis, David E. Olson · 2026 · ACS Chemical Neuroscience
mechanoLight: A genetically encoded fluorescent biosensor for visualizing 5-HT2AR mechanotransduction in live cells
In-Yeop Baek, Hyunbin Kim, 권두완, Hahnbeom Park, Jihye Seong · 2026 · Proceedings of the National Academy of Sciences
QSAR Modeling and Fragment Contribution Analysis of N-Benzyltryptamines at Human 5-HT2 Receptor Subtypes
Vladimir V. Đorđević, Iva Binić, Jovana Petrović, Jelena Stojanov, Žarko J. Mitić, Aleksandar M. Veselinović · 2026 · Molecules
Exploratory Comparison of EEG Spectral Profiles Across Pilocarpine-Induced Epilepsy and Acute LSD and Zolpidem Conditions in Mice
Darlene Kim · 2026 · American journal of student research.
BindingDB Entry 50018939: Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT
BindingDB · 2024 · UC San Diego
BindingDB Entry 50019553: Design, Synthesis, Molecular Docking, and Biological Evaluation of Novel Pimavanserin-Based Analogues as Potential Serotonin 5-HT
BindingDB · 2024 · UC San Diego
BindingDB Entry 50021828: Synthesis and in vitro evaluation of novel amino-phenylmethylene-imidazolone 5-HT2A receptor antagonists.
BindingDB · 2025 · UC San Diego
BindingDB Entry 50019575: Discovery of Novel Oleamide Analogues as Brain-Penetrant Positive Allosteric Serotonin 5-HT
BindingDB · 2024 · UC San Diego
BindingDB Entry 50021727: Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT2 Receptor Agonist.
BindingDB · 2025 · UC San Diego
BindingDB Entry 50016203: Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HT
BindingDB · 2023 · UC San Diego
BindingDB Entry 50016734: Discovery of Highly Potent Serotonin 5-HT
BindingDB · 2023 · UC San Diego
Quantum Chemical Topology and Energetic Analysis of Psychedelic and Non-Psychedelic Ligands in Coordination-Sphere Models of the Human 5-HT2A Receptor
Anaid Flores, Imelda Lizeth Lazcano Carrasco, Mayra Lozano-Espinosa, Luis Antonio Soriano-Agueda, Carlos Zepactonal Gómez-Castro, Marco Franco‐Pérez · 2026 · Research Square
Mechanism-guided generative chemistry yields distinct agonist-like and antagonist-like ligand populations for the serotonin 5-HT2A receptor
Precious Ayorinde Akinnusi · 2026 · Scientific Reports