Protein-based ¹⁸F-PET tracers offer new possibilities in early disease detection and personalized medicine. Their development relies heavily on the availability and effectiveness of ¹⁸F-prosthetic groups. We prepared and evaluated a novel arginine-selective prosthetic group, 4-[¹⁸F]fluorophenylglyoxal ([¹⁸F]FPG). [¹⁸F]FPG was radiosynthesized by a one-pot, two-step procedure with a non-decay-corrected (n.d.c.) isolated radiochemical yield (RCY) of 41 ± 8% (n = 10). [¹⁸F]FPG constitutes a generic tool for ¹⁸F-labeling of various proteins, including human serum albumin (HSA), ubiquitin, interleukin-2, and interleukin-4 in ∼30–60% n.d.c. isolated RCYs. [¹⁸F]FPG conjugation with arginine residues is highly selective, even in the presence of a large excess of lysine, cysteine, and histidine. [¹⁸F]FPG protein conjugates are able to preserve the binding affinity of the native proteins while also demonstrating excellent in vivo stability. The [¹⁸F]FPG-HSA conjugate has prolonged blood retention, which can be applied as a potential blood pool PET imaging agent. Thus, [¹⁸F]FPG is an arginine-selective bioconjugation reagent that can be effectively used for the development of ¹⁸F-labeled protein radiopharmaceuticals.

中文翻译：

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用于有效 18F 标记天然蛋白质的精氨酸选择性生物缀合试剂

基于蛋白质的¹⁸ F-PET 示踪剂为早期疾病检测和个性化医疗提供了新的可能性。它们的发展在很大程度上依赖于^{18 个}F 假肢组的可用性和有效性。我们制备并评估了一种新型精氨酸选择性辅基，4-[ ¹⁸ F]氟苯基乙二醛（[ ¹⁸ F]FPG）。 [ ¹⁸ F]FPG 通过一锅两步程序进行放射合成，非衰变校正 (ndc) 分离放射化学产率 (RCY) 为 41 ± 8% ( n = 10)。 [ ^{18 F]FPG 构成了对各种蛋白质进行18} F 标记的通用工具，包括人血清白蛋白 (HSA)、泛素、白细胞介素 2 和白细胞介素 4（在约 30–60% ndc 分离的 RCY 中）。 [ ¹⁸ F]FPG 与精氨酸残基的缀合具有高度选择性，即使存在大量过量的赖氨酸、半胱氨酸和组氨酸。 [ ¹⁸ F]FPG 蛋白缀合物能够保留天然蛋白的结合亲和力，同时还表现出优异的体内稳定性。 [ ¹⁸ F]FPG-HSA缀合物具有延长的血液保留时间，可作为潜在的血池PET显像剂。因此，[ ¹⁸ F]FPG是一种精氨酸选择性生物缀合试剂，可有效用于开发¹⁸ F标记的蛋白质放射性药物。