ArticleBiochemistry2011
Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands.
Article in Biochemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
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Who cites it
34 citing papers in PubMed, 78 citations in OpenAlex.
- Mixed squaramide thioesters as phosphate group analogues for non-competitive antagonists of the phospholipid-sensing G protein-coupled receptor GPR55.RSC chemical biology · 2026Article
- Neuroprotective Role of Cannabinoid CBMolecular neurobiology · 2026Article
- Structural basis for lipid-mediated activation of G protein-coupled receptor GPR55.Nature communications · 2025Article
- Structural insight into GPR55 ligand recognition and G-protein coupling.Cell research · 2025Article
- The Benzoxazole Heterocycle: A Comprehensive Review of the Most Recent Medicinal Chemistry Developments of Antiproliferative, Brain-Penetrant, and Anti-inflammatory Agents.Topics in current chemistry (Cham) · 2024Review
- Article
- Microglial Cannabinoid CBInternational journal of molecular sciences · 2023Review
- Interacting binding insights and conformational consequences of the differential activity of cannabidiol with two endocannabinoid-activated G-protein-coupled receptors.Frontiers in pharmacology · 2022Article
- GPR55 Antagonist CID16020046 Protects against Atherosclerosis Development in Mice by Inhibiting Monocyte Adhesion and Mac-1 Expression.International journal of molecular sciences · 2021Article
- Peptide targeting of lysophosphatidylinositol-sensing GPR55 for osteoclastogenesis tuning.Cell communication and signaling : CCS · 2021Article
- GPR55 Receptor Activation by theInternational journal of molecular sciences · 2021Article
- Distinctive Evidence Involved in the Role of Endocannabinoid Signalling in Parkinson's Disease: A Perspective on Associated Therapeutic Interventions.International journal of molecular sciences · 2020Review
- GPR55-Mediated Effects in Colon Cancer Cell Lines.Medical cannabis and cannabinoids · 2019Article
- Targeting CBMolecular neurobiology · 2019Article
- Discovery of 1,4-Naphthoquinones as a New Class of Antiproliferative Agents Targeting GPR55.ACS medicinal chemistry letters · 2019Article
- Design, synthesis and biological evaluation of GPR55 agonists.Bioorganic & medicinal chemistry · 2017Article
- Cannabinoid Receptor Interacting Protein 1a Competition with β-Arrestin for CB1 Receptor Binding Sites.Molecular pharmacology · 2017Article
- Identification of Crucial Amino Acid Residues Involved in Agonist Signaling at the GPR55 Receptor.Biochemistry · 2017Article
- Peptide-guided targeting of GPR55 for anti-cancer therapy.Oncotarget · 2017Article
- Identifying ligands at orphan GPCRs: current status using structure-based approaches.British journal of pharmacology · 2016Review
Corrections and comments
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Authors and funding
14 authors at 5 institutions in 1 country.
Funding
Abstract
Marijuana is the most widely abused illegal drug, and its spectrum of effects suggests that several receptors are responsible for the activity. Two cannabinoid receptor subtypes, CB1 and CB2, have been identified, but the complex pharmacological properties of exogenous cannabinoids and endocannabinoids are not fully explained by their signaling. The orphan receptor GPR55 binds a subset of CB1 and CB2 ligands and has been proposed as a cannabinoid receptor. This designation, however, is controversial as a result of recent studies in which lysophosphatidylinositol (LPI) was identified as a GPR55 agonist. Defining a biological role for GPR55 requires GPR55 selective ligands that have been unavailable. From a β-arrestin, high-throughput, high-content screen of 300000 compounds run in collaboration with the Molecular Libraries Probe Production Centers Network initiative (PubChem AID1965), we identified potent GPR55 selective agonists. By modeling of the GPR55 activated state, we compared the GPR55 binding conformations of three of the novel agonists obtained from the screen, CID1792197, CID1172084, and CID2440433 (PubChem Compound IDs), with that of LPI. Our modeling indicates the molecular shapes and electrostatic potential distributions of these agonists mimic those of LPI; the GPR55 binding site accommodates ligands that have inverted-L or T shapes with long, thin profiles that can fit vertically deep in the receptor binding pocket while their broad head regions occupy a horizontal binding pocket near the GPR55 extracellular loops. Our results will allow the optimization and design of second-generation GPR55 ligands and provide a means for distinguishing GPR55 selective ligands from those interacting with cannabinoid receptors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.