ArticleJournal of the American Chemical Society2013
Selective tumor cell targeting by the disaccharide moiety of bleomycin.
Article in Journal of the American Chemical Society, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 56 papers.
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Who cites it
56 citing papers in PubMed, 244 citations in OpenAlex.
- Carbamate-Bearing Carbohydrates: Natural Occurrence, Pharmacological Relevance, and Chemical Synthesis.ACS omega · 2026Review
- Formation and cellular uptake of Bleomycin saccharide decorated molecular spherical nucleic acids evaluated by time-resolved fluorescence spectroscopy.Photochemical & photobiological sciences : Official journal of the European Photochemistry Association and the European Society for Photobiology · 2026Article
- A Simple Colorimetric Assay of Bleomycin-Mediated DNA Cleavage Utilizing Double-Stranded DNA-Modified Gold Nanoparticles.Chembiochem : a European journal of chemical biology · 2023Article
- Synthesis of Four Orthogonally Protected Rare l-Hexose Thioglycosides from d-Mannose by C-5 and C-4 Epimerization.Molecules (Basel, Switzerland) · 2022Article
- Review
- Assembly of Bleomycin Saccharide-Decorated Spherical Nucleic Acids.Bioconjugate chemistry · 2022Article
- GDP-Mannose 3,5-Epimerase: A View on Structure, Mechanism, and Industrial Potential.Frontiers in molecular biosciences · 2021Review
- Cancer nanotechnology: Enhancing tumor cell response to chemotherapy for hepatocellular carcinoma therapy.Asian journal of pharmaceutical sciences · 2019Review
- Characterization of the First Bacterial and Thermostable GDP-Mannose 3,5-Epimerase.International journal of molecular sciences · 2019Article
- Synthesis and Properties of Low-Molecular-Weight PEI-Based Lipopolymers for Delivery of DNA.Polymers · 2018Article
- Aptamer-Modified Magnetic Nanosensitizer for In Vivo MR Imaging of HER2-Expressing Cancer.Nanoscale research letters · 2018Article
- The Interaction of the Metallo-Glycopeptide Anti-Tumour Drug Bleomycin with DNA.International journal of molecular sciences · 2018Review
- Review
- Potential Applications of Nanotechnology in Urological Cancer.Frontiers in pharmacology · 2018Review
- Human Albumin Fragments Nanoparticles as PTX Carrier for Improved Anti-cancer Efficacy.Frontiers in pharmacology · 2018Article
- Structural changes of Zn(II)bleomycin complexes when bound to DNA hairpins containing the 5'-GT-3' and 5'-GC-3' binding sites studied through NMR spectroscopy.Magnetochemistry (Basel, Switzerland) · 2018Article
- Design, synthesis, and biological evaluation of new thiazolo[5,4-MedChemComm · 2017Article
- The DNA sequence specificity of bleomycin cleavage in a systematically altered DNA sequence.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2017Article
- NC1404, a novel derivative of Bleomycin with modified sugar moiety obtained during the preparation of Boningmycin.The Journal of antibiotics · 2017Article
- SLC2A8 (GLUT8) is a mammalian trehalose transporter required for trehalose-induced autophagy.Scientific reports · 2016Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
Abstract
In a recent study, the well-documented tumor targeting properties of the antitumor agent bleomycin (BLM) were studied in cell culture using microbubbles that had been derivatized with multiple copies of BLM. It was shown that BLM selectively targeted MCF-7 human breast carcinoma cells but not the "normal" breast cell line MCF-10A. Furthermore, it was found that the BLM analogue deglycobleomycin, which lacks the disaccharide moiety of BLM, did not target either cell line, indicating that the BLM disaccharide moiety is necessary for tumor selectivity. Not resolved in the earlier study were the issues of whether the BLM disaccharide moiety alone is sufficient for tumor cell targeting and the possible cellular uptake of the disaccharide. In the present study, we conjugated BLM, deglycoBLM, and BLM disaccharide to the cyanine dye Cy5**. It was found that the BLM and BLM disaccharide conjugates, but not the deglycoBLM conjugate, bound selectively to MCF-7 cells and were internalized. The same was also true for the prostate cancer cell line DU-145 (but not for normal PZ-HPV-7 prostate cells) and for the pancreatic cancer cell line BxPC-3 (but not for normal SVR A221a pancreas cells). The targeting efficiency of the disaccharide was only slightly less than that of BLM in MCF-7 and DU-145 cells and comparable to that of BLM in BxPC-3 cells. These results establish that the BLM disaccharide is both necessary and sufficient for tumor cell targeting, a finding with obvious implications for the design of novel tumor imaging and therapeutic agents.
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Registered trials
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