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An aminoacridine de...
An aminoacridine derivative for radionuclide therapy : DNA binding properties studied in a novel cell-free in vitro assay
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- Kullberg, Erika Bohl (author)
- Uppsala universitet,Enheten för biomedicinsk strålningsvetenskap
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- Stenerlöw, Bo (author)
- Uppsala universitet,Enheten för biomedicinsk strålningsvetenskap
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- Ghirmai, Senait (author)
- Uppsala universitet,Institutionen för biokemi och organisk kemi
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- Lundqvist, Hans (author)
- Uppsala universitet,Enheten för biomedicinsk strålningsvetenskap
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- Malmström, Per-Uno (author)
- Uppsala universitet,Institutionen för kirurgiska vetenskaper
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- Orlova, Anna (author)
- Uppsala universitet,Enheten för biomedicinsk strålningsvetenskap
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- Tolmachev, Vladimir (author)
- Uppsala universitet,Enheten för biomedicinsk strålningsvetenskap
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- Gedda, Lars (author)
- Uppsala universitet,Enheten för biomedicinsk strålningsvetenskap
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(creator_code:org_t)
- 2005
- 2005
- English.
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In: International Journal of Oncology. - 1019-6439 .- 1791-2423. ; 27:5, s. 1355-60
- Related links:
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https://urn.kb.se/re...
Abstract
Subject headings
Close
- 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.
Keyword
- MEDICINE
- MEDICIN
Publication and Content Type
- ref (subject category)
- art (subject category)
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