Earley, D.F.; Guillou, A.; van der Born, D.; Poot, A.J.; Holland, J.P. Microfluidic Preparation of 89Zr-Radiolabelled Proteins by Flow Photochemistry. Molecules2021, 26, 764.
Earley, D.F.; Guillou, A.; van der Born, D.; Poot, A.J.; Holland, J.P. Microfluidic Preparation of 89Zr-Radiolabelled Proteins by Flow Photochemistry. Molecules 2021, 26, 764.
89Zr-radiolabelled proteins functionalised with desferrioxamine B are a cornerstone of diagnostic positron emission tomography. In the clinical setting, 89Zr-labelled proteins are produced manually. Here, we explore the potential of using a microfluidic photochemical flow reactor to prepare 89Zr-radiolabelled proteins. The light-induced functionalisation and 89Zr-radiolabelling of human serum albumin ([89Zr]ZrDFO-PEG3-Et-azepin-HSA) was achieved by flow photochemistry with a decay-corrected radiochemical yield (RCY) of 31.2±1.3% (n = 3) and radiochemical purity >90%. In comparison, a manual batch photoreactor synthesis produced the same radiotracer in a decay-corrected RCY of 59.6±3.6% (n = 3) with an equivalent RCP >90%. The results indicate that photoradiolabelling in flow is a feasible platform for the automated production of protein-based 89Zr-radiotracers, but further refinement of the apparatus, and optimisation of the method is required before the flow process is competitive with manual reactions.
Flow Chemistry; Photochemistry; Radiochemistry; Protein Conjugation.
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