ArticleBiochemical and biophysical research communications2013
A synthetic bivalent ligand of CXCR4 inhibits HIV infection.
Article in Biochemical and biophysical research communications, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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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.
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Who cites it
21 citing papers in PubMed, 34 citations in OpenAlex.
- Optimization of next-generation CXCR4 ligands for radiotheranostic applications.Frontiers in pharmacology · 2026Review
- Preclinical evaluation of CXCR4 peptides for targeted radionuclide therapy in glioblastoma.EJNMMI radiopharmacy and chemistry · 2024Article
- Biological and mutational analyses of CXCR4-antagonist interactions and design of new antagonistic analogs.Bioscience reports · 2023Article
- CXCR4 Recognition by L- and D-Peptides Containing the Full-Length V3 Loop of HIV-1 gp120.Viruses · 2023Article
- HIV-1 gp120-CXCR4 recognition probed with synthetic nanomolar affinity D-peptides containing fragments of gp120 V3 loop.European journal of medicinal chemistry · 2022Article
- Mechanistic insight into the impact of a bivalent ligand on the structure and dynamics of a GPCR oligomer.Computational and structural biotechnology journal · 2022Article
- D-Peptide-Based Probe for CXCR4-Targeted Molecular Imaging and Radionuclide Therapy.Pharmaceutics · 2021Article
- Role of CXCR4 in the progression and therapy of acute leukaemia.Cell proliferation · 2021Review
- Discoveries and developments of CXCR4-targeted HIV-1 entry inhibitors.Experimental biology and medicine (Maywood, N.J.) · 2020Review
- High affinity CXCR4 inhibitors generated by linking low affinity peptides.European journal of medicinal chemistry · 2019Article
- Design and evaluation of a CXCR4 targeting peptide 4DV3 as an HIV entry inhibitor and a ligand for targeted drug delivery.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2019Article
- Peptide Assembly on the Membrane Determines the HIV-1 Inhibitory Activity of Dual-Targeting Fusion Inhibitor Peptides.Scientific reports · 2019Article
- Novel Bivalent and D-Peptide Ligands of CXCR4 Mobilize Hematopoietic Progenitor Cells to the Blood in C3H/HeJ Mice.Cell transplantation · 2018Article
- A Direct in Vivo Comparison of the Melanocortin Monovalent Agonist Ac-His-DPhe-Arg-Trp-NHACS chemical neuroscience · 2017Article
- Design, synthesis, and biological characterization of novel PEG-linked dimeric modulators for CXCR4.Bioorganic & medicinal chemistry · 2016Article
- An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.Journal of medicinal chemistry · 2016Article
- Drug delivery strategies and systems for HIV/AIDS pre-exposure prophylaxis and treatment.Journal of controlled release : official journal of the Controlled Release Society · 2015Review
- Chemokine-Derived Peptides: Novel Antimicrobial and Antineoplasic Agents.International journal of molecular sciences · 2015Review
- Targeting strategies for delivery of anti-HIV drugs.Journal of controlled release : official journal of the Controlled Release Society · 2014Review
- Nanoparticle ligand presentation for targeting solid tumors.AAPS PharmSciTech · 2014Review
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
Abstract
G-protein-coupled receptors (GPCRs) are cell membrane protein receptors that transduce signals across the cell membrane and are important targets for therapeutic interventions. As members of the GPCR superfamily, chemokine receptors such as CXCR4 play critical roles in normal physiology as well as the pathology of many human diseases including cancer, inflammation, autoimmune diseases, and human immunodeficiency virus (HIV) infection. Here we report the discovery and study of a novel peptide ligand of CXCR4 using d-amino acids and bivalent ligand approach. This peptide, DV1-K-(DV3), shows very high affinity for CXCR4 with an IC50 of 4 nM in anti-CXCR4 monoclonal antibody (mAb) 12G5 competitive assay, which is more potent than full length natural ligand SDF-1α, even though the peptide is less than half of the number of residues of SDF-1α. This peptide can block the calcium influx stimulated by SDF-1α and inhibit cancer cell migration in vitro via CXCR4, thus functioning as a CXCR4 antagonist. Furthermore, DV1-K-(DV3) peptide displayed anti-HIV activity by inhibiting HIV-1 infection mediated by CXCR4. With its high receptor affinity and stability from D-amino acids, this peptide may be a new probe of CXCR4 functions in physiology and pathology and promising lead for therapeutic development.
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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.