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合理设计和药物调节的F-标记生物素/FAPI-结合的异构分子

Xuedong Chen¹, Dongsheng Xia¹, Xueyuan Zeng¹

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.

Journal of medicinal chemistry

|May 10, 2024

概括

结合纤维细胞激活蛋白 (FAP) 和生物素受体 (BR) 向的新型双重向放射性连接体显示,增强瘤吸收和保留,以改善癌症诊断. 双特异性[18F]AlF-NSFBP4标记物对临床翻译具有前景.

科学领域:

在瘤学瘤学.
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:

癌症异质性需要先进的诊断策略.
异构体放射连体通过吸引多个生物标志物提供了改进的瘤向.
纤维细胞激活蛋白 (FAP) 和生物素受体 (BR) 是瘤诊断中的关键标.

研究的目的:

开发新的18F标记生物素/FAPI结合的异性双价放射性连接体.
为了评估这些双重准标记物的体外和体内性能.
评估这些药物在增强瘤成像和保留方面的潜力.

主要方法:

新型异体双价放射性连接体的合成和18F标记 ([18F]AlF-NSFB, [18F]AlF-NSFBP2, [18F]AlF-NSFBP4).
在体外和体外对生物性质的评估,包括瘤吸收和保留.
在A549和HT1080-FAP瘤携带的小鼠模型中进行正子发射断层扫描 (PET) 成像.

主要成果:

与FAP向单体相比,生物/FAPI合的异构体显示出明显更高的瘤吸收和长时间的保留.
开发的追踪器 ([18F]AlF-NSFB, [18F]AlF-NSFBP2, [18F]AlF-NSFBP4) 显示出有效的双重准能力.
[18F]AlF-NSFBP4作为两种特异性标记物表现出卓越的性能.

结论:

针对FAP和BR的异构体放射连体提供了优越的瘤向和保留.
生物素和链接器修饰对放射性体的药理动力学产生积极影响.
[18F]AlF-NSFBP4在癌症诊断中的临床翻译方面显示出显著的希望.

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