Billaud Emilie M F, Vidal Aurélien, Vincenot Amélie, Besse Sophie, Bouchon Bernadette, Debiton Eric, Miot-Noirault Elisabeth, Miladi Imen, Rbah-Vidal Latifa, Auzeloux Philippe, Chezal Jean-Michel
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.
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.
ACS Med Chem Lett. 2014 Nov 24;6(2):168-72. doi: 10.1021/ml500423v. eCollection 2015 Feb 12.
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.
一种新型的易于获得的用于分子成像和靶向放射性核素治疗的辅基，四氟苯基 4-氟-3-碘苯甲酸酯（TFIB），用氟或碘放射性核素进行放射性标记，获得了优异的放射化学产率和纯度。这些放射性标记物与 N,N-二乙基亚乙二胺偶联，得到靶向黑色素的放射性示踪剂[（125）I]9 和[（18）F]9，通过正电子发射断层扫描（PET）和γ闪烁成像在荷 B16F0 色素性黑色素瘤的 C57BL/6J 小鼠中对其进行了成功评估。然后，放射性标记的[（125）I]/[（18）F]TFIB 在温和条件下用于标记肿瘤靶向肽（即分别靶向αvβ3 整合素和 MC1R 受体的 PEG3[c(RGDyK)]2 和 NDP-MSH），并获得了良好的放射化学产率（47 - 83% d.c.）和纯度（>99%）。对所得的放射性标记肽进行了体外评估以及在动物模型中的 PET 成像评估。
