Publications Repository - Helmholtz-Zentrum Dresden-Rossendorf

1 Publication

Recent Progress using the Staudinger Ligation for Radiolabeling Applications

Mamat, C.; Gott, M.; Steinbach, J.


The increasing application of positron emission tomography (PET) and single photon emission computer tomography (SPECT) in radiopharmacy and nuclear medicine has stimulated the development of a multitude of novel and versatile bioorthogonal conjugation techniques. Currently, there is particular interest in radiolabeling biologically active, high molecular weight compounds like peptides, proteins or antibodies, but also for the labeling of small organic compounds. An enormous challenge in radiolabeling these biologically active molecules is that the introduction of radiohalogens like fluorine-18 as well as various radiometals proceeds under harsh conditions, which could destroy the biomolecule.
The Staudinger Ligation is one of the most powerful bioorthogonal conjugation techniques. The reaction proceeds over wide temperature and pH ranges; an amide (peptide) bond is formed as the ligation unit, which minimizes distortion of the structure; no isomers are obtained; and the reaction proceeds without any metal catalyst. Due to this adaptability, this robust ligation type is a perfect candidate with a high potential for various applications in the field of radiopharmacy for the labeling of biomolecules under mild conditions.
This review summarizes recent research concerning the implementation of the Staudinger Ligation for radiolabeling applications.

Keywords: fluorine-18; Staudinger Ligation; click chemistry; bioorthogonal

Involved research facilities

  • PET-Center



Years: 2023 2022 2021 2020 2019 2018 2017 2016 2015