Development and Preliminary Evaluation of TFIB, a New Bimodal Prosthetic Group for Bioactive Molecule Labeling

作者：Billaud Emilie M F; Vidal Aurelien; Vincenot Amelie; Besse Sophie; Bouchon Bernadette; Debiton Eric; Miot Noirault Elisabeth; Miladi Imen; Rbah Vidal Latifa; Auzeloux Philippe; Chezal Jean Michel^*

来源：ACS Medicinal Chemistry Letters, 2015, 6(2): 168-172.

DOI：10.1021/ml500423v

• Bioconjugation
• prosthetic group
• radiochemistry
• radiofluorination
• radioiodination
• molecular imaging

The new readily available prosthetic group, tetrafluorophenyl 4-fluoro-3-iodobenzoate (TFIB), designed for both molecular imaging and targeted radionuclide therapy purposes was radiolabeled either with fluorine or iodine radionuclides with excellent radiochemical yields and purities. These radiolabeled tags were conjugated to N,N-diethylethylenediamine to give melanin-targeting radiotracers [I-125]9 and [F-18]9, which were successfully evaluated by PET and gamma scintigraphic imaging in B16F0 pigmented melanoma-bearing C57BL/6J mice. Then, radiolabeled [I-125]/[F-18]TFIB was used to tag tumor-targeting peptides (i.e., PEG(3)[c(RGDyK)](2) and NDP-MSH targeting alpha(v)beta(3) integrin and MC1R receptors, respectively) in mild conditions and with good radiochemical yields (47-83% d.c.) and purities (>99%). The resulting radiolabeled peptides were assessed both in vitro and by PET imaging in animal models.

• 出版日期2015-2