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开发Ga-标记的exendin{}9-39) 衍生物用于胰岛素瘤的PET成像

Tuo Li¹, Linlin Li¹, Yaping Luo¹

¹Department of Nuclear Medicine, State Key Laboratory of Common Mechanism Research for Major Diseases, Chinese Academy of Medical Sciences and Peking Union Medical College Hospital, Beijing 100730, China.

Bioconjugate chemistry

|November 8, 2025

概括

研究人员开发了一种新的加-68标记的标记物,[68Ga]Ga-E09,用于成像葡萄糖类-1受体 (GLP-1R) 阳性瘤. 与以前的药物相比,这种更安全的对抗剂追踪剂显示出优越的瘤吸收和结合亲和力.

科学领域:

核医学就是核医学.
放射性药物化学放射性药物化学
分子成像学分子成像学

背景情况:

葡萄糖类-1受体 (GLP-1R) 在胰岛素瘤中高度表达,使其成为诊断成像的关键标.
目前的GLP-1R激素追踪剂可能会导致低血糖症等不良影响,特别是在儿科患者中.

研究的目的:

设计和开发新的,更安全的GLP-1R抗剂放射标记物,以改善胰岛素瘤成像.
用计算和实验方法评估这些新型追踪器的性能.

主要方法:

利用分子动力学 (MD) 模拟和MM/GBSA计算来预测NOTA结合的exendin(9-39) 衍生物的结合亲缘关系.
合成和表征了三个具有对抗性质的68Ga标记衍生物 (E09,E12,E27).
使用表面等离子体共振 (SPR) 验证的结合亲和度,并通过PET成像评估体内性能.

主要成果:

MD模拟准确地预测了结合亲缘关系,排名E09>E12>E27.
[68Ga]Ga-E09在PET成像中表现出明显更高的瘤吸收 (SUVmax: 3.99) 与E12 (SUVmax: 0.75) 和E27 (无法检测) 相比.
所有的放射性标记物都表现出极好的放射性化学产量 (>95%) 和血稳定性 (>91%完好).

结论:

计算查和实验验证的结合对于开发新型放射性追踪剂是有效的.
[68Ga]Ga-E09显示出卓越的结合亲和力,瘤吸收和成像特征,将其定位为胰岛素瘤成像的有希望的候选人.
这种新型的抗体追踪剂为患者提供了一个潜在的更安全的替代方案,特别是儿童,接受GLP-1R向成像.

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