ArticleCell chemical biology2019
Characterization, Dynamics, and Mechanism of CXCR4 Antagonists on a Constitutively Active Mutant.
Article in Cell chemical biology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
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Who cites it
15 citing papers in PubMed, 29 citations in OpenAlex.
- Elevated conformational dynamics makes ACKR3 activation-prone and G protein-incompetent.bioRxiv : the preprint server for biology · 2026Article
- Activity-restoring mutations in the histamine HProtein science : a publication of the Protein Society · 2026Article
- Article
- Inhibiting CXCR4 reduces immunosuppressive effects of myeloid cells in breast cancer immunotherapy.Scientific reports · 2025Article
- Identifying and Assessing Putative Allosteric Sites and Modulators for CXCR4 Predicted through Network Modeling and Site Identification by Ligand Competitive Saturation.The journal of physical chemistry. B · 2024Article
- Crosstalk between purinergic receptor P2YCellular and molecular life sciences : CMLS · 2024Article
- Biological and mutational analyses of CXCR4-antagonist interactions and design of new antagonistic analogs.Bioscience reports · 2023Article
- CXCR4 as a novel target in immunology: moving away from typical antagonists.Future drug discovery · 2022Review
- Predicting target-ligand interactions with graph convolutional networks for interpretable pharmaceutical discovery.Scientific reports · 2022Article
- Statistical Analysis of Protein-Ligand Interaction Patterns in Nuclear Receptor RORγ.Frontiers in molecular biosciences · 2022Article
- Wnt/β-Catenin Signaling Regulates CXCR4 Expression and [Diagnostics (Basel, Switzerland) · 2021Article
- The N-terminal length and side-chain composition of CXCL13 affect crystallization, structure and functional activity.Acta crystallographica. Section D, Structural biology · 2020Article
- Factor H-Inspired Design of Peptide Biomarkers of the Complement C3d Protein.ACS medicinal chemistry letters · 2020Article
- High-Throughput Screening of a Functional Human CXCL12-CXCR4 Signaling Axis in a Genetically ModifiedFrontiers in molecular biosciences · 2020Article
- Chemokine receptor CXCR4 oligomerization is disrupted selectively by the antagonist ligand IT1t.The Journal of biological chemistryArticle
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
16 authors at 4 institutions in 2 countries.
Funding
Abstract
The G protein-coupled receptor (GPCR) CXCR4 is a co-receptor for HIV and is involved in cancers and autoimmune diseases. We characterized five purine or quinazoline core polyamine pharmacophores used for targeting CXCR4 dysregulation in diseases. All were neutral antagonists for wild-type CXCR4 and two were biased antagonists with effects on β-arrestin-2 only at high concentrations. These compounds displayed various activities for a constitutively active mutant (CAM). We use the IT1t-CXCR4 crystal structure and molecular dynamics (MD) simulations to develop two hypotheses for the activation of the N119
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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.