Chen Junyi, Xu Mengxin, Li Zhu, Kong Ziren, Cai Jie, Wang Chunhong, Mu Bo-Shuai, Cui Xi-Yang, Zhang Zizhu, Liu Tong, Liu Zhibo
Beijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing, 100871, China.
Changping Laboratory, Beijing, 102206, China.
Angew Chem Int Ed Engl. 2025 Jan 2;64(1):e202413249. doi: 10.1002/anie.202413249. Epub 2024 Nov 6.
Trifluoroborate boronophenylalanine (BBPA) is a boron amino acid analog of 4-boronophenylalanine (BPA) but with a trifluoroborate group (-BF ) instead of a carboxyl group (-COOH). Clinical studies have shown that F-labeled BBPA ([F]BBPA) can produce high-contrast tumor images in positron emission tomography (PET). Beyond PET imaging, BBPA is a theranostic agent for boron neutron capture therapy (BNCT). Because BBPA possesses an identical chemical structure to BNCT and PET, it can potentially predict the boron concentration for BNCT using [F]BBPA-PET. The synthesis of BBPA was achieved by selectively fluorinating the α-aminoborate compound, taking advantage of the varying rates of solvolysis of the B-F bond. The study showcased the high-contrast [F]BBPA-PET imaging in various tumor models, highlighting its broad applicability for both [F]BBPA-PET and BBPA-BNCT. [F]BBPA-PET tumor uptake remains consistent across various doses, including those used in BNCT. This enables accurate estimation of the boron concentration in tumors using [F]BBPA-PET. With its dual boron structure, BBPA increases boron concentration in tumor cells and tumor tissues compared to BPA. Thus, less boron carrier is needed. This study introduces a new theranostic boron carrier that enhances boron accumulation in tumors, predicts boron concentration, and enhances the accuracy and effectiveness of BNCT.
三氟硼酸硼代苯丙氨酸（BBPA）是4-硼代苯丙氨酸（BPA）的硼氨基酸类似物，但含有三氟硼酸基团（-BF）而非羧基（-COOH）。临床研究表明，氟标记的BBPA（[F]BBPA）在正电子发射断层扫描（PET）中可产生高对比度的肿瘤图像。除PET成像外，BBPA还是一种用于硼中子俘获疗法（BNCT）的诊疗剂。由于BBPA与BNCT和PET具有相同的化学结构，它有可能利用[F]BBPA-PET预测BNCT的硼浓度。BBPA的合成是通过选择性地氟化α-氨基硼化合物实现的，这利用了B-F键不同的溶剂解速率。该研究展示了[F]BBPA-PET在各种肿瘤模型中的高对比度成像，突出了其在[F]BBPA-PET和BBPA-BNCT中的广泛适用性。[F]BBPA-PET肿瘤摄取在包括BNCT中使用的各种剂量下均保持一致。这使得能够使用[F]BBPA-PET准确估计肿瘤中的硼浓度。与BPA相比，BBPA具有双硼结构，可增加肿瘤细胞和肿瘤组织中的硼浓度。因此，所需的硼载体更少。本研究引入了一种新的诊疗硼载体，可增强硼在肿瘤中的积累，预测硼浓度，并提高BNCT的准确性和有效性。
