Labelling of bio-macromolecules: Challenge in radiolabelling for radiopharmacy


Labelling of bio-macromolecules: Challenge in radiolabelling for radiopharmacy

Steinbach, J.

Over the last two decades, radiolabeled antibodies and peptides have been introduced in research and in clinical application of nuclear medicine. Such substances are utilized for tumor targeting as radiotracers and for therapeutic purposes as well. Labelling of such substances with PET radionuclides such as F-18 offers the chance of introduction the label without drastic changes of the molecular properties in conjunction with highest image quality, i.e. high diagnostic value. Radiometal-labeled bioactive substances offer both: The possibility of diagnostics and therapeutic intervention as well. However, the labelling procedure is a considerable alteration of the molecules radiopharmacological properties. This is due to the need of introducing a chelating moiety to bind the radiometals kinetically and thermodynamically inert. Beside this geometric impact, the labelling conditions are of highest importance. Whereas peptides may withstand rather drastic conditions, proteins e.g. antibodies need ambient labelling conditions such as aqueous solution, room temperature, near physiological pH. Furthermore, various proteins tend to coagulate in the presence of heavy metals as radio-copper.
The talk will present such results of scientific investigations at the Institute of Radiopharmacy during the last five years. This involves the application of established methods such as the use of [18F]SFB (N-succinimidyl-4-[18F]fluorobenzoate) for labelling of biomolecules, the development of alternative labelling agents/prosthetic groups as well as current efforts to establish methods for pre- and postlabelling with radiometals. All these investigations are directed to corresponding applications with biomolecules and bioactive compounds, respectively.

  • Invited lecture (Conferences)
    16th Biennial Congress of the György Hevesy Hungarian Society of Nuclear Medicine (MONT), 02.-04.07.2009, Debrecen, Hungary
  • Open Access Logo Abstract in refereed journal
    Nuclear Medicine Review 12(2009)1, 31
    ISSN: 1506-9680

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Publ.-Id: 12881