title: Development and Preliminary Evaluation of TFIB, a New Bimodal Prosthetic Group for Bioactive Molecule Labeling.
abstract: 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 [ (125) I]9 and [ (18) F]9, which were successfully evaluated by PET and gamma scintigraphic imaging in B16F0 pigmented melanoma-bearing C57BL/6J mice. Then, radiolabeled [ (125) I]/[ (18) F]TFIB was used to tag tumor-targeting peptides (i.e., PEG3[c(RGDyK)]2 and NDP-MSH targeting αvβ3 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.
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France.
authors.forename: Emilie M F
authors.initials: EM
authors.lastname: Billaud
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France.
authors.forename: Aurélien
authors.initials: A
authors.lastname: Vidal
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France.
authors.forename: Amélie
authors.initials: A
authors.lastname: Vincenot
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France.
authors.forename: Sophie
authors.initials: S
authors.lastname: Besse
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France.
authors.forename: Bernadette
authors.initials: B
authors.lastname: Bouchon
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France.
authors.forename: Eric
authors.initials: E
authors.lastname: Debiton
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France.
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Miot-Noirault
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France.
authors.forename: Imen
authors.initials: I
authors.lastname: Miladi
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France.
authors.forename: Latifa
authors.initials: L
authors.lastname: Rbah-Vidal
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France ; Centre Jean Perrin , F-63011 Clermont-Ferrand, France.
authors.forename: Philippe
authors.initials: P
authors.lastname: Auzeloux
authors.affiliation: Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France ; Centre Jean Perrin , F-63011 Clermont-Ferrand, France.
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Chezal
keywords: Bioconjugation; molecular imaging; prosthetic group; radiochemistry; radiofluorination; radioiodination