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Issue 15, 2019, Issue in Progress
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Fully automated peptide radiolabeling from [18F]fluoride

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Abstract

The biological properties of receptor-targeted peptides have made them popular diagnostic imaging and therapeutic agents. Typically, the synthesis of fluorine-18 radiolabeled receptor-targeted peptides for positron emission tomography (PET) imaging is a time consuming, complex, multi-step synthetic process that is highly variable based on the peptide. The complexity associated with the radiolabeling route and lack of robust automated protocols can hinder translation into the clinic. A fully automated batch production to radiolabel three peptides (YGGFL, cRGDyK, and Pyr-QKLGNQWAVGHLM) from fluorine-18 using the ELIXYS FLEX/CHEM® radiosynthesizer in a two-step process is described. First, the prosthetic group, 6-[18F]fluoronicotinyl-2,3,5,6-tetrafluorophenyl ester ([18F]FPy-TFP) was synthesized and subsequently attached to the peptide. The [18F]FPy-peptides were synthesized in 13–26% decay corrected yields from fluorine-18 with high molar activity 1–5 Ci μmol−1 and radiochemical purity of >99% in an overall synthesis time of 97 ± 3 minutes.

Graphical abstract: Fully automated peptide radiolabeling from [18F]fluoride

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Publication details

The article was received on 24 Dec 2018, accepted on 26 Feb 2019 and first published on 15 Mar 2019


Article type: Paper
DOI: 10.1039/C8RA10541C
RSC Adv., 2019,9, 8638-8649
  • Open access: Creative Commons BY-NC license
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    Fully automated peptide radiolabeling from [18F]fluoride

    R. A. Davis, C. Drake, R. C. Ippisch, M. Moore and Julie L. Sutcliffe, RSC Adv., 2019, 9, 8638
    DOI: 10.1039/C8RA10541C

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