基于小分子的放射性追踪剂的合成和临床前评估,用于对PD-L1表达和动态的PET成像
Gaochao Lv1,2, Nan Zhang3,4, Junyi Zhu3,4
1NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, 214063, China. lvgaochao@jsinm.org.
European journal of nuclear medicine and molecular imaging
|April 22, 2025
概括
两种新的小分子放射追踪器[18F]LG-2和[18F]LG-3被开发用于正电子发射断层扫描 (PET) 成像. [18F]LG-3在癌症治疗过程中有效监控编程死亡干1 (PD-L1) 表达和动态.
科学领域:
- 放射化学 放射化学是指辐射化学.
- 分子成像学分子成像学
- 在瘤学瘤学.
背景情况:
- 小分子放射标志物为正电子发射断层扫描 (PET) 成像提供了优势.
- 在实体中对编程死亡配体1 (PD-L1) 表达的非侵入性监测对于治疗评估至关重要.
研究的目的:
- 开发新的小分子放射追踪器,以评估PD-L1的表达和动态.
- 在临床前模型中评估这些标记物的疗效.
主要方法:
- 使用点击化学设计和合成[18F]LG-2和[18F]LG-3.
- 在体外细胞吸收测试以确定PD-L1的特异性.
- 在携带瘤的小鼠体内PET成像,以评估PD-L1表达和治疗反应.
主要成果:
- 这两种标记物都成功被放射性标记,产量很好.
- 与[18F]LG-2相比,[18F]LG-3被证明与PD-L1具有特定的结合,并且在肝脏和肠道中具有较低的非目标吸收.
- 使用[18F]LG-3的PET成像显示了与PD-L1水平的强烈相关性,并在化疗和免疫治疗期间准确监测PD-L1动态.
结论:
- [18F]LG-3是一种有前途的小分子放射追踪器,用于评估PD-L1表达.
- 这种追踪器可以在癌症治疗期间动态监测PD-L1状态.
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