Targeting against epidermal growth factor receptors: Cellular processing of astatinated EGF after binding to cultured carcinoma cells
2004 (English)In: Anticancer Research, ISSN 0250-7005, Vol. 24, no 6, 4035-4042 p.Article in journal (Refereed) Published
The alpha-emitting nuclide 211At is of great interest for radionuclide therapy when coupled to a tumor-targeting biomolecule, e.g. epidermal growth factor (EGF) the receptors of which are overexpressed in many malignancies. However, almost no information concerning the cellular processing of astatinated targeting agents is available.
MATERIALS AND METHODS:
We indirectly astatinated EGF ([211At]-benzoate-EGF) and studied its cellular processing in A-431 carcinoma cells in comparison with data concerning [125I]-benzoate-EGF.
The biological half-life of astatine (3.5 h) was longer than the half-life of the iodine label (1.5 h). The increase of the half-life was due to longer retention of the internalised astatine radioactivity. The maximum accumulation for the astatine label occurred later (4-6h) than that for the iodine label (2-4h), indicating a slower excretion of astatine that was confirmed in experiment with 211At/1251-benzoate-EGF.
The long retention of astatine might be advantageous for radionuclide therapy.
Place, publisher, year, edition, pages
2004. Vol. 24, no 6, 4035-4042 p.
Astatine/chemistry/metabolism/*pharmacokinetics, Carcinoma/*metabolism/radiotherapy, Cell Line; Tumor, Cell Membrane/metabolism, Epidermal Growth Factor/metabolism/*pharmacokinetics, Epithelioid Cells/metabolism/pathology, Half-Life, Humans, Iodobenzoates/metabolism/pharmacokinetics, Radiopharmaceuticals/metabolism/*pharmacokinetics, Receptor; Epidermal Growth Factor/*metabolism
Radiology, Nuclear Medicine and Medical Imaging
IdentifiersURN: urn:nbn:se:uu:diva-72882PubMedID: 15736449OAI: oai:DiVA.org:uu-72882DiVA: diva2:100793