ArticlePloS one2015
The fucosylation inhibitor, 2-fluorofucose, inhibits vaso-occlusion, leukocyte-endothelium interactions and NF-ĸB activation in transgenic sickle mice.
Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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The trial behind it
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Who cites it
19 citing papers in PubMed, 32 citations in OpenAlex.
- Fucosylation enhances CD34⁺ hematopoietic stem cell homing and longevity via E-selectin-mediated adhesion and signaling.BMC cancer · 2026Article
- Blockade of the Notch Pathway by Inhibition of Fucosylation Ameliorates Chondrocyte Inflammation and Extracellular Matrix Degradation.Journal of inflammation research · 2025Article
- Review
- 2-Fluorofucose Attenuates Hydrogen Peroxide-Induced Oxidative Stress in HepG2 Cells via Nrf2/keap1 and NF-κB Signaling Pathways.Life (Basel, Switzerland) · 2022Article
- Glucose metabolism and glycosylation link the gut microbiota to autoimmune diseases.Frontiers in immunology · 2022Review
- Inhibition of fucosylation by 2-fluorofucose attenuated acetaminophen-induced liver injuryFrontiers in pharmacology · 2022Article
- First-In-Human, First-In-Class, Phase I Trial of the Fucosylation Inhibitor SGN-2FF in Patients with Advanced Solid Tumors.The oncologist · 2021Article
- Synthetic Fluorinated l-Fucose Analogs Inhibit Proliferation of Cancer Cells and Primary Endothelial Cells.ACS chemical biology · 2020Article
- Repurposing pyridoxamine for therapeutic intervention of intravascular cell-cell interactions in mouse models of sickle cell disease.Haematologica · 2020Article
- The multifaceted role of ischemia/reperfusion in sickle cell anemia.The Journal of clinical investigation · 2020Review
- Bioisosteres of Carbohydrate Functional Groups in Glycomimetic Design.Biomimetics (Basel, Switzerland) · 2019Review
- Glycosylation in the Tumor Microenvironment: Implications for Tumor Angiogenesis and Metastasis.Cells · 2019Review
- Critical role of C5a in sickle cell disease.American journal of hematology · 2019Article
- Therapeutic strategies for sickle cell disease: towards a multi-agent approach.Nature reviews. Drug discovery · 2019Review
- Inhibition of fucosylation by 2-fluorofucose suppresses human liver cancer HepG2 cell proliferation and migration as well as tumor formation.Scientific reports · 2017Article
- Microfluidic on-chip biomimicry for 3D cell culture: a fit-for-purpose investigation from the end user standpoint.Future science OA · 2017Review
- Base-modified UDP-sugars reduce cell surface levels of P-selectin glycoprotein 1 (PSGL-1) on IL-1β-stimulated human monocytes.Glycobiology · 2016Article
- Designing sugar mimetics: non-natural pyranosides as innovative chemical tools.Current opinion in chemical biology · 2016Review
- Advances in cell surface glycoengineering reveal biological function.Glycobiology · 2016Review
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
2-Fluorofucose (2FF) blocks the fucosylation and the tethering of sialyl-Lewisx tetrasaccharide and structural variants on leukocytes and red blood cells to P- and E-selectins on activated endothelial cell surfaces. Because P- and E-selectin are required for vaso-occlusion in murine sickle cell disease (SCD), we investigated whether 2FF would inhibit vaso-occlusion in SCD mice. Microvascular stasis was measured in subcutaneous venules in NY1DD and HbSS-Townes SCD mice with dorsal skin-fold chambers after infusion of hemoglobin or exposure to hypoxia/reoxygenation. 2FF in drinking water or administered by gavage inhibited stasis in sickle mice in a dose-responsive manner. Significant inhibitory effects on stasis were seen 1 day post-treatment. 2FF treatment of SCD mice also significantly reduced leukocyte rolling and adhesion along the vessel walls of SCD mice and the static adhesion of neutrophils and sickle red blood cells isolated from 2FF-treated SCD mice to resting and activated endothelial cells. Total white blood cell counts increased in response to 2FF. NF-ĸB activation and VCAM-1 and E-selectin expression were inhibited in the livers of SCD mice consistent with an overall decrease in vascular inflammation and ischemia-reperfusion physiology. Pretreatment with 2FF completely eliminated heme-induced lethality in HbSS-Townes mice, consistent with the observed anti-inflammatory and anti-adhesive properties of 2FF in SCD mice. These data suggest that 2FF may be beneficial for preventing or treating vaso-occlusive crises in SCD patients.
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