Fully automated peptide radiolabeling from [ 18 F]fluoride

Ryan A. Davis, Chris Drake, Robin C. Ippisch, Melissa Moore, Julie Sutcliffe

Research output: Contribution to journalArticlepeer-review

4 Scopus citations

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-[ 18 F]fluoronicotinyl-2,3,5,6-tetrafluorophenyl ester ([ 18 F]FPy-TFP) was synthesized and subsequently attached to the peptide. The [ 18 F]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.

Original languageEnglish (US)
Pages (from-to)8638-8649
Number of pages12
JournalRSC Advances
Volume9
Issue number15
DOIs
StatePublished - Jan 1 2019

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)

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