ArticleActa pharmaceutica Sinica. B2021
An optimized derivative of an endogenous CXCR4 antagonist prevents atopic dermatitis and airway inflammation.
Article in Acta pharmaceutica Sinica. B, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed, 49 citations in OpenAlex.
- A CXCR4 targeting peptide delivered by silica nanoparticles eliminates migrating cancer stem cells in pancreatic ductal adenocarcinoma.Scientific reports · 2026Article
- An endogenous human peptide derived from αNaunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Chemokine ligand-receptor interactions as potential therapeutic targets for atopic dermatitis: from basic to clinical research.Frontiers in allergy · 2026Review
- CXCR4 inhibition alleviates prostatic inflammation and pelvic pain via suppressing Th17 cell differentiation and oxidative stress in EAP mice.International journal of biological sciences · 2026Article
- Targeting the CXCL12/CXCR4 pathway by an optimized derivative or EPI-X4 preserves chondrocyte function and offers a novel therapeutic approach in rheumatic diseases.Arthritis research & therapy · 2025Article
- ButyrylatedActa pharmaceutica Sinica. B · 2025Article
- A Computational Perspective to Intermolecular Interactions and the Role of the Solvent on Regulating Protein Properties.Chemical reviews · 2025Review
- Is Zebrafish a Good Model for the Alpha-Gal Syndrome?FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2025Review
- CXCR4 Inhibition Enhances the Efficacy of CD19 Monoclonal Antibody-Mediated Extermination of B-Cell Lymphoma.International journal of molecular sciences · 2025Article
- A naturally occurring 22-amino acid fragment of human hemoglobin A inhibits autophagy and HIV-1.Cellular and molecular life sciences : CMLS · 2024Article
- An Optimized Peptide Antagonist of CXCR4 Limits Survival of BCR-ABL1-Transformed Cells in Philadelphia-Chromosome-Positive B-Cell Acute Lymphoblastic Leukemia.International journal of molecular sciences · 2024Article
- Dupilumab-associated head and neck dermatitis shows a pronounced type 22 immune signature mediated by oligoclonally expanded T cells.Nature communications · 2024Article
- Confinement and Polarity Effects on the Peptide Packing Density on Mesoporous Silica Nanoparticles.Langmuir : the ACS journal of surfaces and colloids · 2024Article
- MDIC3: Matrix decomposition to infer cell-cell communication.Patterns (New York, N.Y.) · 2024Article
- Relationship between dietary protein, serum albumin, and mortality in asthmatic populations: a cohort study.Frontiers in immunology · 2024Article
- The story of clobenpropit and CXCR4: can be an effective drug in cancer and autoimmune diseases?Frontiers in pharmacology · 2024Review
- Development of N-Terminally Modified Variants of the CXCR4-Antagonistic Peptide EPI-X4 for Enhanced Plasma Stability.Journal of medicinal chemistry · 2023Article
- Post-acute immunological and behavioral sequelae in mice after Omicron infection.bioRxiv : the preprint server for biology · 2023Article
- Peptide Bispecifics Inhibiting HIV-1 Infection by an Orthogonal Chemical and Supramolecular Strategy.Bioconjugate chemistry · 2023Article
- Development of a New Class of CXCR4-Targeting Radioligands Based on the Endogenous Antagonist EPI-X4 for Oncological Applications.Journal of medicinal chemistry · 2023Article
Corrections and comments
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Authors and funding
19 authors at 7 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Aberrant CXCR4/CXCL12 signaling is involved in many pathophysiological processes such as cancer and inflammatory diseases. A natural fragment of serum albumin, named EPI-X4, has previously been identified as endogenous peptide antagonist and inverse agonist of CXCR4 and is a promising compound for the development of improved analogues for the therapy of CXCR4-associated diseases. To generate optimized EPI-X4 derivatives we here performed molecular docking analysis to identify key interaction motifs of EPI-X4/CXCR4. Subsequent rational drug design allowed to increase the anti-CXCR4 activity of EPI-X4. The EPI-X4 derivative JM#21 bound CXCR4 and suppressed CXCR4-tropic HIV-1 infection more efficiently than the clinically approved small molecule CXCR4 antagonist AMD3100. EPI-X4 JM#21 did not exert toxic effects in zebrafish embryos and suppressed allergen-induced infiltration of eosinophils and other immune cells into the airways of animals in an asthma mouse model. Moreover, topical administration of the optimized EPI-X4 derivative efficiently prevented inflammation of the skin in a mouse model of atopic dermatitis. Thus, rationally designed EPI-X4 JM#21 is a novel potent antagonist of CXCR4 and the first CXCR4 inhibitor with therapeutic efficacy in atopic dermatitis. Further clinical development of this new class of CXCR4 antagonists for the therapy of atopic dermatitis, asthma and other CXCR4-associated diseases is highly warranted.
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