ArticleBritish journal of pharmacology2013
Identification and profiling of CXCR3-CXCR4 chemokine receptor heteromer complexes.
Article in British journal of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed, 64 citations in OpenAlex.
- Pharmacological modulation of CXCL12/CXCR4/ACKR3 for brain disorders - an overview.Cell communication and signaling : CCS · 2026Review
- A Spatiotemporal Model of CXCL10 as a Master Regulator of Immune Evasion and Metastasis in Osteosarcoma.International journal of molecular sciences · 2025Review
- CXCR3 inhibitors for therapeutic interventions: current status and perspectives.Frontiers in pharmacology · 2025Review
- Chemokinergic and Dopaminergic Signalling Collaborates through the Heteromer Formed by CCR9 and Dopamine Receptor D5 Increasing the Migratory Speed of Effector CD4International journal of molecular sciences · 2024Article
- Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET.International journal of molecular sciences · 2024Article
- The β2-adrenergic receptor associates with CXCR4 multimers in human cancer cells.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- G protein activation via chemokine (C-X-C motif) receptor 4 and αFEBS letters · 2023Article
- NanoBCell reports methods · 2023Article
- Development of tolerance to chemokine receptor antagonists: current paradigms and the need for further investigation.Frontiers in immunology · 2023Review
- GPCR heteromers: An overview of their classification, function and physiological relevance.Frontiers in endocrinology · 2022Review
- Prestimulation of CD2 confers resistance to HIV-1 latent infection in blood resting CD4 T cells.iScience · 2021Article
- Profiling novel pharmacology of receptor complexes using Receptor-HIT.Biochemical Society transactions · 2021Review
- Investigation of Receptor Heteromers Using NanoBRET Ligand Binding.International journal of molecular sciences · 2021Article
- Plasticity of seven-transmembrane-helix receptor heteromers in human vascular smooth muscle cells.PloS one · 2021Article
- Regulation of the thrombin/protease-activated receptor 1 axis by chemokine (CThe Journal of biological chemistry · 2020Article
- Kinetic Analysis of the Early Signaling Steps of the Human Chemokine Receptor CXCR4.Molecular pharmacology · 2020Article
- Characterization of heteromeric complexes between chemokine (C-X-C motif) receptor 4 and αBiochemical and biophysical research communications · 2020Article
- CRISPR-Mediated Protein Tagging with Nanoluciferase to Investigate Native Chemokine Receptor Function and Conformational Changes.Cell chemical biology · 2020Article
- The orphan receptor GPR88 blunts the signaling of opioid receptors and multiple striatal GPCRs.eLife · 2020Article
- High CXCR3 on Leukemic Cells DistinguishesJournal of immunology research · 2020Article
Corrections and comments
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Authors and funding
14 authors at 6 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe C-X-C chemokine receptors 3 (CXCR3) and C-X-C chemokine receptors 4 (CXCR4) are involved in various autoimmune diseases and cancers. Small antagonists have previously been shown to cross-inhibit chemokine binding to CXCR4, CC chemokine receptors 2 (CCR2) and 5 (CCR5) heteromers. We investigated whether CXCR3 and CXCR4 can form heteromeric complexes and the binding characteristics of chemokines and small ligand compounds to these chemokine receptor heteromers. EXPERIMENTAL APPROACH: CXCR3-CXCR4 heteromers were identified in HEK293T cells using co-immunoprecipitation, time-resolved fluorescence resonance energy transfer, saturation BRET and the GPCR-heteromer identification technology (HIT) approach. Equilibrium competition binding and dissociation experiments were performed to detect negative binding cooperativity. KEY
resultsWe provide evidence that chemokine receptors CXCR3 and CXCR4 form heteromeric complexes in HEK293T cells. Chemokine binding was mutually exclusive on membranes co-expressing CXCR3 and CXCR4 as revealed by equilibrium competition binding and dissociation experiments. The small CXCR3 agonist VUF10661 impaired binding of CXCL12 to CXCR4, whereas small antagonists were unable to cross-inhibit chemokine binding to the other chemokine receptor. In contrast, negative binding cooperativity between CXCR3 and CXCR4 chemokines was not observed in intact cells. However, using the GPCR-HIT approach, we have evidence for specific β-arrestin2 recruitment to CXCR3-CXCR4 heteromers in response to agonist stimulation. CONCLUSIONS AND IMPLICATIONS: This study indicates that heteromeric CXCR3-CXCR4 complexes may act as functional units in living cells, which potentially open up novel therapeutic opportunities.
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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.