An aminoacridine derivative for radionuclide therapy: DNA binding properties studied in a novel cell-free in vitro assay.
Int J Oncol
; 27(5): 1355-60, 2005 Nov.
Article
em En
| MEDLINE
| ID: mdl-16211232
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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Base de dados:
MEDLINE
Assunto principal:
Benzamidas
/
Acridinas
/
Adutos de DNA
Limite:
Humans
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article