ArticleScience (New York, N.Y.)2010
Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Article in Science (New York, N.Y.), 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 878 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
878 citing papers in PubMed, 1,753 citations in OpenAlex.
- CXCR4 reduces aldosterone synthesis via regulating CYP11B2 expression.Genes & diseases · 2026Article
- Improved Method for Predicting GPCR-GPCR Interaction Pairs.Proteins · 2026Article
- The chemokine receptor-like fourth extracellular loop of the apelin receptor differentially regulates apelin and elabela binding and signalling.British journal of pharmacology · 2026Article
- Cloud-based ligand-guided virtual screening with deep-learning-enhanced docking identifies a micromolar CXCR4 antagonist.Molecular diversity · 2026Article
- Co-receptor usage in distinct phylogenetic clusters of HIV-1 CRF01_AE is associated with differential immune reconstitution after antiretroviral therapy.Microbiology spectrum · 2026Article
- De novo design of miniproteins targeting GPCRs.Nature · 2026Article
- Decoding Waldenström Macroglobulinemia Through Genomics, Epigenomics and Cellular Interactions.International journal of molecular sciences · 2026Review
- Mechanistic and therapeutic insights into class A GPCR dimers in neuropsychiatric disorders.npj drug discovery · 2026Review
- Computational Insights into the Activation Mechanism of CXCR4: Implications for the Design of Small Molecule Agonists.Journal of the American Chemical Society · 2026Article
- Elevated conformational dynamics makes ACKR3 activation-prone and G protein-incompetent.bioRxiv : the preprint server for biology · 2026Article
- Structure basis for C-C chemokine receptor 4 modulation by orthosteric and allosteric antagonists.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Chirobiophore: A Novel Framework for Quantifying Biochirality in Macromolecular Systems.Biomolecules · 2026Article
- Surface Plasmon Resonance as a Potential Diagnostic Tool for the Detection of CXC Chemokine Receptor 4 (CXCR4) on Extracellular Vesicles.Biosensors · 2026Article
- Advances in Therapeutic Antibody Discovery and Development Targeting G Protein-Coupled Receptors.Pharmacology research & perspectives · 2026Review
- Cycling molecular assemblies for Golgi imaging and disruption.Nature communications · 2026Article
- CXCR4: A Promising Novel Strategy for Lung Cancer Treatment.Biomolecules · 2026Review
- Molecular basis of antagonism of the dimeric human arginine vasopressin receptor 1A.Nature communications · 2026Article
- Analysis of common differential gene expression between rheumatoid arthritis and ulcerative colitis.PloS one · 2026Article
- Identification of Immune-Related Genes in Predicting the Progression of Colitis-Associated Colorectal Cancer: An Integrated Bioinformatics and Experimental Validation Study.Journal of inflammation research · 2026Article
- Computational identification of natural CXCR4-binding candidates relevant to endometriosis and ovarian cancer progression.PloS one · 2026Article
818 more citing papers are in PubMed but not listed here.
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Authors and funding
15 authors at 1 institution in 1 country.
Funding
Abstract
Chemokine receptors are critical regulators of cell migration in the context of immune surveillance, inflammation, and development. The G protein-coupled chemokine receptor CXCR4 is specifically implicated in cancer metastasis and HIV-1 infection. Here we report five independent crystal structures of CXCR4 bound to an antagonist small molecule IT1t and a cyclic peptide CVX15 at 2.5 to 3.2 angstrom resolution. All structures reveal a consistent homodimer with an interface including helices V and VI that may be involved in regulating signaling. The location and shape of the ligand-binding sites differ from other G protein-coupled receptors and are closer to the extracellular surface. These structures provide new clues about the interactions between CXCR4 and its natural ligand CXCL12, and with the HIV-1 glycoprotein gp120.
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What OpenQuestion holds
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.