ArticleThe Journal of biological chemistry2012
Molecular characterization of oxysterol binding to the Epstein-Barr virus-induced gene 2 (GPR183).
Article in The Journal of biological chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 48 citations in OpenAlex.
- International Union of Basic and Clinical Pharmacology. CXXII. Applying an objective evaluation to the status of class A orphan G protein-coupled receptors.Pharmacological reviews · 2026Review
- Structure-based screening and a conformational biosensor identify a GPR183 inverse agonist and an activation switch.Nature communications · 2026Article
- G-protein coupled receptor 183 (GPR183) inhibits visceral metastasis of non-small cell lung cancer.Clinical & experimental metastasis · 2025Article
- First report on chemometrics-driven multilayered lead prioritization in addressing oxysterol-mediated overexpression of G protein-coupled receptor 183.Molecular diversity · 2024Article
- Sexual Dimorphism in the Immunometabolic Role of Gpr183 in Mice.Journal of the Endocrine Society · 2024Article
- 25-Hydroxycholesterol in health and diseases.Journal of lipid research · 2024Review
- Ligand entry pathways control the chemical space recognized by GPR183.Chemical science · 2023Article
- Identification of the niche and mobilization mechanism for tissue-protective multipotential bone marrow ILC progenitors.Science advances · 2022Article
- Potential Biomarker Identification by RNA-Seq Analysis in Antibiotic-Related Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS): A Pilot Study.Toxicological sciences : an official journal of the Society of Toxicology · 2022Article
- EBI2 is a negative modulator of brown adipose tissue energy expenditure in mice and human brown adipocytes.Communications biology · 2022Article
- ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production.Frontiers in immunology · 2022Article
- Evidence that specific interactions play a role in the cholesterol sensitivity of G protein-coupled receptors.Biochimica et biophysica acta. Biomembranes · 2021Article
- Review
- Early Growth Response Gene Upregulation in Epstein-Barr Virus (EBV)-Associated Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS).Biomolecules · 2020Review
- Article
- GPR183 Regulates Interferons, Autophagy, and Bacterial Growth DuringFrontiers in immunology · 2020Article
- Epstein-Barr Virus Induced Gene-2 Upregulation Identifies a Particular Subtype of Chronic Fatigue Syndrome/Myalgic Encephalomyelitis.Frontiers in pediatrics · 2019Review
- Biased agonism and allosteric modulation of G protein-coupled receptor 183 - a 7TM receptor also known as Epstein-Barr virus-induced gene 2.British journal of pharmacology · 2017Article
- Membrane cholesterol access into a G-protein-coupled receptor.Nature communications · 2017Article
- Article
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Authors and funding
10 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Oxysterols are oxygenated cholesterol derivates that are emerging as a physiologically important group of molecules. Although they regulate a range of cellular processes, only few oxysterol-binding effector proteins have been identified, and the knowledge of their binding mode is limited. Recently, the family of G protein-coupled seven transmembrane-spanning receptors (7TM receptors) was added to this group. Specifically, the Epstein-Barr virus-induced gene 2 (EBI2 or GPR183) was shown to be activated by several oxysterols, most potently by 7α,25-dihydroxycholesterol (7α,25-OHC). Nothing is known about the binding mode, however. Using mutational analysis, we identify here four key residues for 7α,25-OHC binding: Arg-87 in TM-II (position II:20/2.60), Tyr-112 and Tyr-116 (positions III:09/3.33 and III:13/3.37) in TM-III, and Tyr-260 in TM-VI (position VI:16/6.51). Substituting these residues with Ala and/or Phe results in a severe decrease in agonist binding and receptor activation. Docking simulations suggest that Tyr-116 interacts with the 3β-OH group in the agonist, Tyr-260 with the 7α-OH group, and Arg-87, either directly or indirectly, with the 25-OH group, although nearby residues likely also contribute. In addition, Tyr-112 is involved in 7α,25-OHC binding but via hydrophobic interactions. Finally, we show that II:20/2.60 constitutes an important residue for ligand binding in receptors carrying a positively charged residue at this position. This group is dominated by lipid- and nucleotide-activated receptors, here exemplified by the CysLTs, P2Y12, and P2Y14. In conclusion, we present the first molecular characterization of oxysterol binding to a 7TM receptor and identify position II:20/2.60 as a generally important residue for ligand binding in certain 7TM receptors.
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