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基于皮里丁的新型纤维细胞激活蛋白向标志物:设计,合成和PET成像评估瘤的成像

Ziyue Yu¹, Yong Huang², Zeng Jiang¹

¹Beijing Institute of Brain Disorders, Laboratory of Brain Disorders, Ministry of Science and Technology, Collaborative Innovation Center for Brain Disorders, Capital Medical University, Beijing 100069, China.

Journal of medicinal chemistry

|November 7, 2025

概括

与较旧的类型相比,新的基于氨酸的FAP抑制剂显示了瘤向和保留的改善. 这些新型放射性药物,如[68Ga]1f,为增强癌症PET成像和治疗提供了希望.

科学领域:

放射性药物化学放射性药物化学
分子成像学分子成像学
在瘤学瘤学.

背景情况:

纤维细胞激活蛋白 (FAP) 是癌症诊断和治疗的关键目标.
现有的林基FAP抑制剂面临着瘤保留和目标外吸收的挑战.
新型的脚手架设计对于开发改进的FAP向药剂至关重要.

研究的目的:

设计和合成新型的烯氨酸 - - 皮里迪尔 - - 葡萄糖 - - 胺衍生物作为FAP抑制剂.
评估这些新化合物的体外和体内性能,用于针对FAP的应用.
为了确定临床PET成像和放射性连接体治疗的有前途的候选人.

主要方法:

设计新型FAP抑制剂的脚手架跳跃方法.
合成和表征氨酸 - - 皮里迪尔 - - 葡萄糖 - - 胺衍生物 (1a-i化合物).
在A549-FAP瘤模型中使用放射性标记化合物 ([68Ga]1b, [68Ga]1f, [68Ga]1h/1i) 的体外亲和度测定和体内PET成像研究.

主要成果:

多聚衍生物1h和1i显示出高的FAP亲和力 (IC50:0.51和0.27nM).
与[68Ga]FAP-46.6相比,[68Ga]1b显示瘤吸收增加和器官吸收减少.
[68Ga]1f表现出优异的瘤保留率 (在4h时7.84%的ID/g) 和高的目标与背景比率.
[68Ga]1h/1i显示高瘤吸收,但也增加了非目标积累.
[68Ga]1f显示出有利的水友性和稳定性,证实了FAP的特定向.

结论:

fenilalanine-pyridyl-glycyl-prolamide 架构代表了基于林的 FAP 抑制剂的可行替代品.
[68Ga]1f是临床PET成像的一个有希望的候选人,因为它具有有利的特性.
[68Ga]1h/1i 需要进一步研究放射性干治疗的应用.
这项研究为开发先进的针对FAP的放射性药物提供了新的方向.

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