用于单光子发射计算机断层扫描成像示踪剂靶向 EphA2 的新型 [铟]铟-联硼酸双环多胺-EphA2-230-1 抗体。
Novel [ In]In-BnDTPA-EphA2-230-1 Antibody for Single-Photon Emission Computed Tomography Imaging Tracer Targeting of EphA2.
作者信息
Furukawa Takenori, Kimura Hiroyuki, Sasaki Minon, Yamada Takumu, Iwasawa Takumi, Yagi Yusuke, Kato Kazunori, Yasui Hiroyuki
机构信息
Department of Analytical and Bioinorganic Chemistry, Division of Analytical and Physical Science, Kyoto Pharmaceutical University, 5 Nakauchi-cho, Misasagi, Yamashina-ku, Kyoto 607-8414, Japan.
Department of Biomedical Engineering, Faculty of Science and Engineering, Toyo University, 2100 Nakanodai, Kujirai, Kawagoe, Saitama 350-0815, Japan.
出版信息
ACS Omega. 2023 Feb 9;8(7):7030-7035. doi: 10.1021/acsomega.2c07849. eCollection 2023 Feb 21.
Erythropoietin-producing hepatocellular receptor A2 (EphA2) is overexpressed in cancer cells and causes abnormal cell proliferation. Therefore, it has attracted attention as a target for diagnostic agents. In this study, the EphA2-230-1 monoclonal antibody (EphA2-230-1) was labeled with [In]In and evaluated as an imaging tracer for single-photon emission computed tomography (SPECT) of EphA2. EphA2-230-1 was conjugated with 2-(4-isothiocyanatobenzyl)-diethylenetriaminepentaacetic acid (p-SCN-BnDTPA) and then labeled with [In]In. [In]In-BnDTPA-EphA2-230-1 was evaluated in cell-binding, biodistribution, and SPECT/computed tomography (CT) studies. The cellular uptake ratio of [In]In-BnDTPA-EphA2-230-1 was 14.0 ± 2.1%/mg protein at 4 h in the cell-binding study. In the biodistribution study, a high uptake of [In]In-BnDTPA-EphA2-230-1 was observed in tumor tissue (14.6 ± 3.2% injected dose/g at 72 h). The superior accumulation of [In]In-BnDTPA-EphA2-230-1 in tumors was also confirmed using SPECT/CT. Therefore, [In]In-BnDTPA-EphA2-230-1 has potential as a SPECT imaging tracer for EphA2.
促红细胞生成素产生肝细胞受体A2（EphA2）在癌细胞中过度表达并导致细胞异常增殖。因此，它作为诊断剂的靶点已引起关注。在本研究中，EphA2-230-1单克隆抗体（EphA2-230-1）用[铟]铟标记，并作为EphA2单光子发射计算机断层扫描（SPECT）的成像示踪剂进行评估。EphA2-230-1与2-（4-异硫氰酸苄基）-二亚乙基三胺五乙酸（p-SCN-BnDTPA）偶联，然后用[铟]铟标记。[铟]铟-BnDTPA-EphA2-230-1在细胞结合、生物分布和SPECT/计算机断层扫描（CT）研究中进行了评估。在细胞结合研究中，4小时时[铟]铟-BnDTPA-EphA2-230-1的细胞摄取率为14.0±2.1%/mg蛋白。在生物分布研究中，在肿瘤组织中观察到[铟]铟-BnDTPA-EphA2-230-1的高摄取（72小时时为14.6±3.2%注射剂量/g）。使用SPECT/CT也证实了[铟]铟-BnDTPA-EphA2-230-1在肿瘤中的优越蓄积。因此，[铟]铟-BnDTPA-EphA2-230-1有潜力作为EphA2的SPECT成像示踪剂。
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