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An aminoacridine derivative for radionuclide therapy: DNA binding properties studied in a novel cell-free in vitro assay

  • Authors:
    • Erika Bohl Kullberg
    • Bo Stenerlöw
    • Senait Ghirmai
    • Hans Lundqvist
    • Per-Uno Malmström
    • Anna Orlova
    • Vladimir Tolmachev
    • Lars Gedda

  • View Affiliations

  • Published online on: November 1, 2005     https://doi.org/10.3892/ijo.27.5.1355
  • Pages: 1355-1360
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Abstract

Radiolabelled DNA-binding compounds can be used to increase the efficiency of radionuclide cancer therapy of disseminated disease. In this work, the aminoacridine compound N-[3-(acridine-9-ylamino)-propyl]-3-iodobenzamide (A3) labelled with the Auger-emitting nuclide 125I using Chloramine-T was studied. Optimal labelling conditions of 125I-A3 were investigated and the interaction with DNA was studied using a novel cell-free in vitro assay with naked human genomic DNA in agarose plugs. This novel assay showed to be simple and reliable. The results verify that 125I-A3 specifically binds DNA with low dissociation and is potent in causing double-strand breaks, yielding 1.0-1.4 breaks per decay. In conclusion, 125I-A3 is a most suitable DNA-binding compound for future therapeutic studies of Auger-electron emitters like 125I.

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November 2005
Volume 27 Issue 5

Print ISSN: 1019-6439
Online ISSN:1791-2423

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  • Journal Metrics
  • Impact Factor: 4.5
  • Ranked Oncology
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  • CiteScore: 9.6
  • CiteScore Rank: Q1: #66/404 Oncology
  • Source Normalized Impact per Paper (SNIP): 0.88
  • SCImago Journal Rank (SJR): 1.099
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Spandidos Publications style
Kullberg EB, Stenerlöw B, Ghirmai S, Lundqvist H, Malmström P, Orlova A, Tolmachev V and Gedda L: An aminoacridine derivative for radionuclide therapy: DNA binding properties studied in a novel cell-free in vitro assay. Int J Oncol 27: 1355-1360, 2005.
APA
Kullberg, E.B., Stenerlöw, B., Ghirmai, S., Lundqvist, H., Malmström, P., Orlova, A. ... Gedda, L. (2005). An aminoacridine derivative for radionuclide therapy: DNA binding properties studied in a novel cell-free in vitro assay. International Journal of Oncology, 27, 1355-1360. https://doi.org/10.3892/ijo.27.5.1355
MLA
Kullberg, E. B., Stenerlöw, B., Ghirmai, S., Lundqvist, H., Malmström, P., Orlova, A., Tolmachev, V., Gedda, L."An aminoacridine derivative for radionuclide therapy: DNA binding properties studied in a novel cell-free in vitro assay". International Journal of Oncology 27.5 (2005): 1355-1360.
Chicago
Kullberg, E. B., Stenerlöw, B., Ghirmai, S., Lundqvist, H., Malmström, P., Orlova, A., Tolmachev, V., Gedda, L."An aminoacridine derivative for radionuclide therapy: DNA binding properties studied in a novel cell-free in vitro assay". International Journal of Oncology 27, no. 5 (2005): 1355-1360. https://doi.org/10.3892/ijo.27.5.1355