ArticleCell2020
Cryo-EM Structure of the Human Cannabinoid Receptor CB2-G
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Article in Cell, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 133 papers.
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133 citing papers in PubMed, 246 citations in OpenAlex.
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- The Endocannabinoid System in the Development and Treatment of Obesity: Searching for New Ideas.International journal of molecular sciences · 2025Review
73 more citing papers are in PubMed but not listed here.
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Authors and funding
17 authors at 5 institutions in 2 countries.
Changrui XingDepartment of Pharmaceutical Sciences, Computational Chemical Genomics Screen Center, School of Pharmacy, and NIDA National Center of Excellence for Computational Drug Abuse Research, University of Pittsburgh, Pittsburgh, PA 15261, USA; Drug Discovery Institute and Departments of Computational Biology and of Structural Biology, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Youwen ZhuangCAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of the Chinese Academy of Sciences, Beijing 100049, China; Center for Cancer and Cell Biology, Program for Structural Biology, Van Andel Institute, Grand Rapids, MI 49503, USA.
Ting-Hai XuCenter for Cancer and Cell Biology, Program for Structural Biology, Van Andel Institute, Grand Rapids, MI 49503, USA.
Zhiwei FengDepartment of Pharmaceutical Sciences, Computational Chemical Genomics Screen Center, School of Pharmacy, and NIDA National Center of Excellence for Computational Drug Abuse Research, University of Pittsburgh, Pittsburgh, PA 15261, USA; Drug Discovery Institute and Departments of Computational Biology and of Structural Biology, University of Pittsburgh, Pittsburgh, PA 15261, USA.
X Edward ZhouCenter for Cancer and Cell Biology, Program for Structural Biology, Van Andel Institute, Grand Rapids, MI 49503, USA.
Maozi ChenDepartment of Pharmaceutical Sciences, Computational Chemical Genomics Screen Center, School of Pharmacy, and NIDA National Center of Excellence for Computational Drug Abuse Research, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Lei WangLaboratory for GPCR Biology, Department of Pharmacology and Chemical Biology, School of Medicine, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Xing MengDavid Van Andel Advanced Cryo-Electron Microscopy Suite, Van Andel Research Institute, Grand Rapids, MI 49503, USA.
Ying XueDepartment of Pharmaceutical Sciences, Computational Chemical Genomics Screen Center, School of Pharmacy, and NIDA National Center of Excellence for Computational Drug Abuse Research, University of Pittsburgh, Pittsburgh, PA 15261, USA; Department of Pharmacy and Therapeutics, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Junmei WangDepartment of Pharmaceutical Sciences, Computational Chemical Genomics Screen Center, School of Pharmacy, and NIDA National Center of Excellence for Computational Drug Abuse Research, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Heng LiuLaboratory for GPCR Biology, Department of Pharmacology and Chemical Biology, School of Medicine, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Terence Francis McGuireDepartment of Pharmaceutical Sciences, Computational Chemical Genomics Screen Center, School of Pharmacy, and NIDA National Center of Excellence for Computational Drug Abuse Research, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Gongpu ZhaoDavid Van Andel Advanced Cryo-Electron Microscopy Suite, Van Andel Research Institute, Grand Rapids, MI 49503, USA.
Karsten MelcherCenter for Cancer and Cell Biology, Program for Structural Biology, Van Andel Institute, Grand Rapids, MI 49503, USA.
Cheng ZhangLaboratory for GPCR Biology, Department of Pharmacology and Chemical Biology, School of Medicine, University of Pittsburgh, Pittsburgh, PA 15261, USA. Electronic address: chengzh@pitt.edu.
H Eric XuCAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. Electronic address: eric.xu@simm.ac.cn.
Xiang-Qun XieDepartment of Pharmaceutical Sciences, Computational Chemical Genomics Screen Center, School of Pharmacy, and NIDA National Center of Excellence for Computational Drug Abuse Research, University of Pittsburgh, Pittsburgh, PA 15261, USA; Drug Discovery Institute and Departments of Computational Biology and of Structural Biology, University of Pittsburgh, Pittsburgh, PA 15261, USA. Electronic address: xix15@pitt.edu.
University of Pittsburgh · USVan Andel Institute · USDiscovery Institute · USChinese Academy of Sciences · CNShanghai Institute of Materia Medica · CN
Funding
NIDA Center of Excellence OF Computational Drug Abuse Research (CDAR)P30DA035778 · NIDA · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI BAHAR, IVET, XIE, XIANG-QUN · 2014 to 2018
$5.4MStructure, pharmacology and signaling of G protein-coupled receptors (GPCRs) in inflammationR35GM128641 · NIGMS · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI CHENG ZHANG · 2018 to 2026
$3.5MStructure/Function of the CB2 Receptor Binding and G-protein Recognition PocketsR01DA025612 · NIDA · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI XIE, XIANG-QUN · 2010 to 2014
$1.7MStructural and Functional Studies of Rhodopsin and G-Protein Coupled Receptor KinasesR01GM127710 · NIGMS · VAN ANDEL RESEARCH INSTITUTE · PI MELCHER, KARSTEN · 2018 to 2020
$1.1MNIDA NIH HHS P30 DA035778NIDA NIH HHS R01 DA025612NIGMS NIH HHS R01 GM127710NIGMS NIH HHS R35 GM128641
Abstract
Drugs selectively targeting CB2 hold promise for treating neurodegenerative disorders, inflammation, and pain while avoiding psychotropic side effects mediated by CB1. The mechanisms underlying CB2 activation and signaling are poorly understood but critical for drug design. Here we report the cryo-EM structure of the human CB2-G
Indexed as
Signal TransductionAnimalsBinding SitesCannabinoid Receptor AgonistsCannabinoid Receptor AntagonistsCHO CellsCricetinaeCricetulusCryoelectron MicroscopyGTP-Binding Protein alpha Subunits, Gi-GoHumansMolecular Docking SimulationProtein BindingReceptor, Cannabinoid, CB2Sf9 CellsSpodopteraCannabinoid Receptor AgonistsCannabinoid Receptor AntagonistsGTP-Binding Protein alpha Subunits, Gi-GoReceptor, Cannabinoid, CB23D Structure of Cannabinoid Receptor CB2Activation Mechanisms of CB2 and CB1Agonist-bound CB2- Gi Signaling ComplexCB2 AgonistCB2 Coupling Specificity for GiCB2 Drug DiscoveryCB2 Inverse AgonistCryo-EM structureGi Coupling VersatilityResidual Energy Contribution
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