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新型化纳米体PET标记器用于TIM3表达的临床前研究

Dongye Zheng^1,2,3, Yong Huang⁴, Chengze Li⁴

¹Department of Biomedical Engineering, College of Future Technology, Peking University, Beijing 100871, China.

Molecular pharmaceutics

|September 5, 2025

概括

研究人员开发了一种新型PET标记物[18F]AlF-RESCA-HVCR2N2,用于非侵入性检测T细胞免疫球蛋白和粘素域-3 (TIM3) 表达. 通过可视化TIM3阳性瘤,该追踪器显示出指导癌症免疫疗法的前景.

科学领域:

免疫学
癌症学
放射化学

背景情况:

T细胞免疫球蛋白和粘素域-3 (TIM3) 是一种抑制抗瘤反应的关键免疫检查点蛋白.
在晚期癌症中,双重阻断TIM3和PD1可增强免疫力,但缺乏非侵入性TIM3检测.

研究的目的:

开发和描述一种用于非侵入性TIM3检测的新型正电子发射断层扫描 (PET) 标记器.
评估标记物的特异性,亲和力和体内表现,以量化TIM3表达.

主要方法:

开发了一种新的PET追踪器,[18F]AlF-RESCA-HVCR2N2,使用TIM3特定的纳米体和[18F]AlF放射化学.
在体外评估的标志物特异性和亲和力 (Kd = 4. 644 nM).
在瘤模型中使用PET成像来可视化表达TIM3的病变,并进行动态成像和动态分析.

主要成果:

[18F]AlF-RESCA-HVCR2N2追踪剂对TIM3具有很高的特异性和亲和力.
在体内成功可视化TIM3表达瘤.
观察到有利的药理动力学和PET信号与TIM3表达之间的相关性.

结论:

[18F]AlF-RESCA-HVCR2N2是TIM3表达的非侵入性量化的一个有前途的工具.
这种标记物可以帮助患者分层和监测TIM3向免疫疗法.
这项研究促进了针对TIM3的癌症治疗策略的进步.

关键词:

PET成像技术在RESCA 时间3 一个纳米体放射性化

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Positron Emission Tomography

Positron Emission Tomography

Positron emission tomography (PET) is a medical imaging technique involving radiopharmaceuticals — substances that emit short-lived radiation. Although the first PET scanner was introduced in 1961, it took 15 more years before radiopharmaceuticals were combined with the technique and revolutionized its potential.
One of the main requirements of a PET scan is a positron-emitting radioisotope, which is produced in a cyclotron and then attached to a substance used by the part of the body...