ArticleScientific reports2016
Discovery and characterization of novel small-molecule CXCR4 receptor agonists and antagonists.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 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
35 citing papers in PubMed, 68 citations in OpenAlex.
- SOD1 regulates CXCR4 transcription in cortical neurons for establishment of cerebral ischemic tolerance.Journal of advanced research · 2026Article
- Computational Insights into the Activation Mechanism of CXCR4: Implications for the Design of Small Molecule Agonists.Journal of the American Chemical Society · 2026Article
- Optimization of next-generation CXCR4 ligands for radiotheranostic applications.Frontiers in pharmacology · 2026Review
- Dual targeting of CXCR4 and EZH2 in endometriosis.iScience · 2025Article
- CXCR4 orchestrates the TOX-programmed exhausted phenotype of CD8Cell genomics · 2024Article
- Article
- Development of VLA4 and CXCR4 Antagonists for the Mobilization of Hematopoietic Stem and Progenitor Cells.Biomolecules · 2024Review
- Glucocorticoids paradoxically promote steroid resistance in B cell acute lymphoblastic leukemia through CXCR4/PLC signaling.Nature communications · 2024Article
- Triazolothiadiazine derivative positively modulates CXCR4 signaling and improves diabetic wound healing.Biochemical pharmacology · 2023Article
- Helix encoder: a compound-protein interaction prediction model specifically designed for class A GPCRs.Frontiers in bioinformatics · 2023Article
- Effects of Small Molecule Ligands on ACKR3 Receptors.Molecular pharmacology · 2022Article
- Recovery from the Neuroparalysis Caused by theToxins · 2022Article
- Machine intelligence-driven framework for optimized hit selection in virtual screening.Journal of cheminformatics · 2022Article
- Latrotoxin-Induced Neuromuscular Junction Degeneration Reveals Urocortin 2 as a Critical Contributor to Motor Axon Terminal Regeneration.International journal of molecular sciences · 2022Article
- An agonist of the CXCR4 receptor is therapeutic for the neuroparalysis induced by Bungarus snakes envenoming.Clinical and translational medicine · 2022Article
- Targeting ACE2 for COVID-19 Therapy: Opportunities and Challenges.American journal of respiratory cell and molecular biology · 2021Review
- An agonist of the CXCR4 receptor accelerates the recovery from the peripheral neuroparalysis induced by Taipan snake envenomation.PLoS neglected tropical diseases · 2020Article
- Discovery of novel aminopiperidinyl amide CXCR4 modulators through virtual screening and rational drug design.European journal of medicinal chemistry · 2020Article
- Kinetic Analysis of the Early Signaling Steps of the Human Chemokine Receptor CXCR4.Molecular pharmacology · 2020Article
- Neutrophil Signaling That Challenges Dogmata of G Protein-Coupled Receptor Regulated Functions.ACS pharmacology & translational science · 2020Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
The chemokine CXCL12 (SDF-1) and its cognate receptor CXCR4 are involved in a large number of physiological processes including HIV-1 infectivity, inflammation, tumorigenesis, stem cell migration, and autoimmune diseases. While previous efforts have identified a number of CXCR4 antagonists, there have been no small molecule agonists reported. Herein, we describe the identification of a novel series of CXCR4 modulators, including the first small molecules to display agonist behavior against this receptor, using a combination of structure- and ligand-based virtual screening. These agonists produce robust calcium mobilization in human melanoma cell lines which can be blocked by the CXCR4-selective antagonist AMD3100. We also demonstrate the ability of these new agonists to induce receptor internalization, ERK activation, and chemotaxis, all hallmarks of CXCR4 activation. Our results describe a new series of biologically relevant small molecules that will enable further study of the CXCR4 receptor and may contribute to the development of new therapeutics.
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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.