An aminoacridine derivative for radionuclide therapy: DNA binding properties studied in a novel cell-free in vitro assay
2005 (English)In: International Journal of Oncology, ISSN 1019-6439, Vol. 27, no 5, 1355-60 p.Article in journal (Refereed) Published
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.
Place, publisher, year, edition, pages
2005. Vol. 27, no 5, 1355-60 p.
Medical and Health Sciences
IdentifiersURN: urn:nbn:se:uu:diva-104630PubMedID: 16211232OAI: oai:DiVA.org:uu-104630DiVA: diva2:220025