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- W926751322 abstract "573 Objectives Peptides radiolabeled with radioisotopes such as fluorine-18 ([18F]) have proven to be promising tools for studying diseases such as cancer using positron emission tomography (PET). 18F-radiolabeling can be challenging, as it must be performed in a quick and efficient manner in order to accommodate for the short half-life of fluorine-18 (109 minutes). Microfluidic flow chemistry devices allow for faster chemistry, while permitting rapid and easy control of reaction temperatures, pressures, and flow rates. We therefore propose a strategy for convenient microfluidic flow chemistry [18F]-peptide radiolabeling. Methods An Advion NanoTek® microfluidic device was used to radiolabel a model peptide, Tyr-Gly-Gly-Phe-Lys (YGGFL). We have demonstrated the radiolabeling of YGGFL using N-succidimidyl-4-[18F]-fluorobenzoate ([18F]SFB). Peptides were assembled on Rink Amide resin using standard F-moc chemistry, and cleaved off of resin prior to radiolabeling. Synthesis was conducted using a 2-step reaction in Discovery Mode of the NanoTek® device. Pump 1 contained YGGFL peptide, pump 2 held [18F]SFB, and pump 3 held base to adjust pH as necessary for coupling. Radiolabeling was shown with temperatures from 30-50°C, flow rates from 30-60 μL/min, pump 1: pump 3 ratio of 0.4-0.5, and pump 2: reaction 1 ratio of 0.5-1. Results 18F radiolabeling of a model peptide, YGGFL was achieved in 20% purity within 5 min. Notably, [18F]SFB showed little to no hydrolysis for up to 22 reactions, over a period of 6 hours. Conclusions Rapid, automated peptide radiolabeling with [18F]SFB was readily achieved on a microfluidic device. Our work demonstrates an alternative approach to radiolabeling of peptides, and shows promise as a new technique for this common synthesis. Future efforts towards optimization of [18F]SFB peptide radiolabeling, along with a complete production of [18F]-labeled peptides from [18F]fluoride, are currently underway. Research Support Office of Science, United States Department of Energy grant DE-SC000206" @default.
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- W926751322 date "2012-05-01" @default.
- W926751322 modified "2023-09-24" @default.
- W926751322 title "Fluorine-18 radiolabeling of peptides using a microfluidic flow chemistry device" @default.
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