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¹⁸ F-标记的阿米多胺醇类似物用于可视化瘤中的STING表达

Jianyang Fang¹, Jingru Zhang¹, Lingxin Meng¹

¹State Key Laboratory of Vaccines for Infectious Diseases, Center for Molecular Imaging and Translational Medicine, Xiang An Biomedicine Laboratory School of Public Health, Xiamen University, 4221-116 Xiang'An South Rd, Xiamen 361102, China.

Molecular pharmaceutics

|March 6, 2024

概括

研究人员开发了[18F]AlF-ABI,这是一种用于可视化刺激干扰素基因 (STING) 的新型PET成像剂. 这种新的探测器显示了与STING相关的癌症治疗的前景,通过在瘤微环境中实现可视化.

科学领域:

免疫学免疫学免疫学
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:

干扰素基因刺激器 (STING) 对I型干扰素的产生和瘤排斥至关重要.
在瘤微环境中可视化STING对于向治疗至关重要.
有效的STING成像探针的有限可用性阻碍了治疗开发.

研究的目的:

开发和评估一种新的18F标记的PET成像剂用于STING.
评估[18F]AlF-ABI在临床前瘤模型中可视化STING的疗效.

主要方法:

[18F]AlF-ABI的合成,18F标记的阿米多胺醇衍生物.
使用体外和体外测定方法进行探针结合亲和性和特异性的表征.
在携带瘤的B16F10和CT26小鼠中进行正子发射断层扫描 (PET) 成像.

主要成果:

[18F]AlF-ABI的合成具有很高的放射性化学产量 (>38%) 和纯度 (>97%).
探测器证明了对STING的纳米分子结合亲和力 (KD = 35.6 nM).
观察到[18F]AlF-ABI的显著瘤吸收,B16F10的积累比CT26瘤高,与STING表达相关.

结论:

[18F]AlF-ABI是一种有前途的新型PET成像剂用于STING.
该探头可以在瘤微环境中可视化STING.
[18F]AlF-ABI在指导针对STING的癌症治疗方面有潜在的应用.

关键词:

在PET成像中使用PET成像.氨基胺醇类似物一个单质的单质分子.干扰素基因的刺激剂.瘤微环境是一个微环境.

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