Targeting against epidermal growth factor receptors. Cellular processing of astatinated EGF after binding to cultured carcinoma cells

Anna Orlova, Anna Sjöstrom, Ondrej Lebeda, Hans Lundqvist, Jörgen Carlsson, Vladimir Tolmachev

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

Abstract

Background: 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. Results: 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/ 125I-benzoate-EGF. Conclusion: The long retention of astatine might be advantageous for radionuclide therapy.

Original languageEnglish
Pages (from-to)4035-4041
Number of pages7
JournalAnticancer Research
Volume24
Issue number6
Publication statusPublished - Nov 2004
Externally publishedYes

Keywords

  • I-para-iodo-benzoate
  • At-para-astato-benzoate
  • A-431 cells
  • EGF
  • Intracellular retention

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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