Radiolabelling small and biomolecules for tracking and monitoring

Martin R. Edelmann

Research output: Contribution to journalReview articlepeer-review

12 Citations (SciVal)


Radiolabelling small molecules with beta-emitters has been intensively explored in the last decades and novel concepts for the introduction of radionuclides continue to be reported regularly. New catalysts that induce carbon/hydrogen activation are able to incorporate isotopes such as deuterium or tritium into small molecules. However, these established labelling approaches have limited applicability for nucleic acid-based drugs, therapeutic antibodies, or peptides, which are typical of the molecules now being investigated as novel therapeutic modalities. These target molecules are usually larger (significantly >1 kDa), mostly multiply charged, and often poorly soluble in organic solvents. However, in preclinical research they often require radiolabelling in order to track and monitor drug candidates in metabolism, biotransformation, or pharmacokinetic studies. Currently, the most established approach to introduce a tritium atom into an oligonucleotide is based on a multistep synthesis, which leads to a low specific activity with a high level of waste and high costs. The most common way of tritiating peptides is using appropriate precursors. The conjugation of a radiolabelled prosthetic compound to a functional group within a protein sequence is a commonly applied way to introduce a radionuclide or a fluorescent tag into large molecules. This review highlights the state-of-the-art in different radiolabelling approaches for oligonucleotides, peptides, and proteins, as well as a critical assessment of the impact of the label on the properties of the modified molecules. Furthermore, applications of radiolabelled antibodies in biodistribution studies of immune complexes and imaging of brain targets are reported.

Original languageEnglish
Pages (from-to)32383-32400
Number of pages18
JournalRSC Advances
Issue number50
Early online date11 Nov 2022
Publication statusPublished - 31 Dec 2022

Bibliographical note

Funding Information:
I thank Dr Ian S. Blagbrough and Prof Stephen M. Husbands from the University of Bath as well as Dr Michael B. Otteneder and Dr Filippo Sladojevich from Roche for their helpful comments and for their interest in these studies.

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)


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