A novel molecular agent for glioma angiogenesis imaging.

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  • Additional Information
    • Source:
      Publisher: Lippincott Williams & Wilkins Country of Publication: England NLM ID: 8201017 Publication Model: Print Cited Medium: Internet ISSN: 1473-5628 (Electronic) Linking ISSN: 01433636 NLM ISO Abbreviation: Nucl Med Commun Subsets: MEDLINE
    • Publication Information:
      Publication: London : Lippincott Williams & Wilkins
      Original Publication: London : Chapman and Hall in association with the British Nuclear Medicine Society, c1980-
    • Subject Terms:
      Endostatins*/pharmacokinetics; Glioma/*blood supply ; Neovascularization, Pathologic/*diagnostic imaging ; Positron-Emission Tomography/*methods; Animals ; Cell Line, Tumor ; Fluorine Radioisotopes ; Glioma/diagnostic imaging ; Humans ; Isotope Labeling ; Mice ; Tissue Distribution
    • Abstract:
      Background: Gliomas are rich in blood vessels and are the most primary and malignant type of brain tumor affecting the central nervous system. A few fluorine-18 (F)-labeled imaging agents can be used for imaging of tumor angiogenesis. In the current study, F-labeled recombinant human endostatin (rh-endostatin) was developed and evaluated as a probe for PET imaging of tumor angiogenesis.
      Materials and Methods: F-fluorobenzoyl-endostatin (F-FB-endostatin) was synthesized from radiolabeling of rh-endostatin with N-succinimidyl-4-F-fluorobenzoate produced by a facile module-assisted radiosynthesis procedure. Blocking studies were used to measure the relative affinities of F-FB-endostatin to human glioblastoma U87MG cells in tumor tissues rich with vessels. In addition, biodistribution, metabolic stability, and small-animal PET imaging studies were carried out with F-FB-endostatin using Institute of Cancer Research and U87MG tumor-bearing mice.
      Results: Noninvasive small-animal PET imaging indicated that F-FB-endostatin showed rapid and good tumor uptake. The probe was rapidly cleared from the blood and most organs, resulting in excellent tumor-to-normal tissue contrasts. Tumor uptake and rapid clearance were further confirmed with biodistribution studies. Metabolite assays showed that the probe was highly stable, making it suitable for in-vivo applications.
      Conclusion: F-FB-endostatin shows promising in-vivo properties. Therefore, the promising properties of F-FB-endostatin indicate that this probe can be a powerful tool to evaluate the antiangiogenic therapy for gliomas and thus warrants further investigation as a novel PET probe for imaging of tumor angiogenesis.
    • Accession Number:
      0 (Endostatins)
      0 (Fluorine Radioisotopes)
      GZ5I74KB8G (Fluorine-18)
    • Publication Date:
      Date Created: 20170902 Date Completed: 20180604 Latest Revision: 20190101
    • Publication Date:
      20240829
    • Accession Number:
      10.1097/MNM.0000000000000735
    • Accession Number:
      28863122