A review of approaches to 18F radiolabelling affinity peptides and proteins. (1st June 2018)

• Record Type: Journal Article
• Authors: Morris, O.; Fairclough, M.; Grigg, J.; Prenant, C.; McMahon, A.
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 62:Number 1(2019)
• Page Start: 4
• Page End: 23
• Publication Date: 2018-06-01
• Subjects: proteins and peptides -- radiolabelling -- monoclonal antibodies -- affibody -- nanobody -- automation; Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3634
• Languages: English
• ISSNs: 0362-4803

Abstract

Abstract : Affinity peptide and protein‐ (APP) based radiotracers are an increasingly popular class of radiotracer in positron emission tomography (PET), which was once dominated by the use of small molecule radiotracers. Radiolabelled monoclonal antibodies (mAbs) are important examples of APPs, yet a preference for smaller APPs, which exhibit fast pharmacokinetics and permit rapid PET aided diagnosis, has become apparent. 18 F exhibits favourable physical characteristics for APP radiolabelling and has been described as an ideal PET radionuclide. Notwithstanding, 18 F radiolabelling of APP is challenging, and this is echoed in the literature where a number of diverse approaches have been adopted. This review seeks to assess and compare the approaches taken to 18 F APP radiolabelling with the intention of highlighting trends within this expanding field. Generic themes have emerged in the literature, namely the use of mild radiolabelling conditions, a preference of site‐specific methodologies with an impetus for short, automated procedures which produce high‐yielding [ 18 F]APPs. Abstract : Once a field dominated by small molecule radiotracers, position emission tomography (PET) has seen a shift towards the use of radiolabelled affinity peptide and proteins (APP). Monoclonal antibodies are important examples, yet a preference for smaller APPs, exhibiting faster pharmacokinetics, has become apparent. This review article seeks to assess and compare the diverse approaches taken to radiolabel this emerging class with 18 F, with the intention of highlighting trends within this expanding field.