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[68Ga]Ga-PG2-2FAPI:一种DPro-Gly修饰的二进制FAPI探头,增强了瘤吸收和保留
Qing Ruan1,2, Yuhao Jiang1,2, Zuojie Li1,2
1Key Laboratory of Beam Technology of the Ministry of Education, School of Physics and Astronomy, Beijing Normal University, Beijing 100875, P.R. China.
Molecular pharmaceutics
|February 6, 2026
概括
一种新的纤维细胞激活蛋白 (FAP) 向连接体,DOTA-PG2-2FAPI,显示出增强的结合亲和力和高特异性用于瘤成像. 这种针对FAP的探测器显示出使用PET成像检测广谱癌症的巨大潜力.
科学领域:
- 生物医学成像技术 生物医学成像技术
- 放射化学 放射化学是指辐射化学.
- 分子成像学分子成像学
背景情况:
- 纤维细胞激活蛋白 (FAP) 是瘤微环境中的一个关键生物标志物.
- 开发针对FAP的向成像剂对于癌症诊断和治疗至关重要.
研究的目的:
- 设计和合成一种新的FAP向性联体,DOTA-PG2-2FAPI.
- 评估FAP准探针的结合亲和力,稳定性和体外/体内表现.
主要方法:
- 用分子对接来评估结合亲和力.
- 用68Ga的DOTA-PG2-2FAPI的合成和放射性标记
- 在FAP表达细胞中的体外细胞吸收研究.
- 在瘤携带小鼠模型中的活体正子发射断层扫描 (PET) 成像.
主要成果:
- 与单体FAPI-46相比,DOTA-PG2-2FAPI对FAP的结合亲和力显著更高 (IC50 = 6.65 nM).
- 标有Ga的探头 (Ga-PG2-2FAPI) 显示出极好的放射化学纯度 (>95%),稳定性和水友性.
- 在FAP阳性瘤中观察到高细胞吸收和瘤积累,迅速积累和持续保留.
- 在多种瘤模型中实现了特定的PET成像,证明了广谱的潜力.
结论:
- DOTA-PG2-2FAPI是一种高效的FAP向剂,具有卓越的结合亲和力.
- 68标记Ga的探针适用于敏感和特定的瘤成像.
- 这种针对FAP的探针显示出作为临床应用的广谱诊断剂的显著前景.
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